Imidazole Based Drug Discovery

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Imidazole-Based Drug Discovery

Author : Shikha Agarwal
Publisher : Elsevier
ISBN 13 : 0323903630
Total Pages : 374 pages
Book Rating : 4.3/5 (239 download)

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Book Synopsis Imidazole-Based Drug Discovery by : Shikha Agarwal

Download or read book Imidazole-Based Drug Discovery written by Shikha Agarwal and published by Elsevier. This book was released on 2021-12-02 with total page 374 pages. Available in PDF, EPUB and Kindle. Book excerpt: Imidazole-Based Drug Discovery covers all categories of imidazole and its derivatives, synthesis, pharmacological applications and drug-based studies. Imidazole scaffolds act as a channel between organic synthesis and medicinal chemistry and compel researchers to explore new drug candidates. This book provides detailed coverage of several greener synthetic protocols and pharmacological applications of imidazole derivatives that are useful to researchers working on designing more promising clinical lead compounds with this scaffold. It also includes information on past decades of research on the synthesis and biological applications of imidazole derivatives. This is an ideal resource for researchers in organic chemistry both in academic and industrial settings, as well as postgraduates in chemistry and medicinal chemistry. Reviews the most current developments and future perspectives of imidazole on different disease therapies to achieve the ultimate goal of disease eradication Discusses the role of imidazole in contemporary science, technological innovation, drug development, critical challenges and future research directions Covers emerging trends on different eco-benign pathways to synthesize imidazole derivatives for the development of simpler synthetic protocols

Studies Towards the Total Synthesis of Imidazole-containing Natural Products

Author : Lawton Anthony II Seal
Publisher :
ISBN 13 :
Total Pages : 114 pages
Book Rating : 4.:/5 (132 download)

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Book Synopsis Studies Towards the Total Synthesis of Imidazole-containing Natural Products by : Lawton Anthony II Seal

Download or read book Studies Towards the Total Synthesis of Imidazole-containing Natural Products written by Lawton Anthony II Seal and published by . This book was released on 2019 with total page 114 pages. Available in PDF, EPUB and Kindle. Book excerpt: Nature has inspired man in all aspects of life, chemistry included. The first antibiotic ever discovered came from nature, and since then, chemists have been probing nature for insights to guide drug discovery and development. Alkaloids are a class of naturally occurring molecules which contain nitrogen atoms and can be found in all forms of life. Imidazole is common structural unit found in many natural molecules, from the simple amino acid histamine to more complex structures like the marine sponge derived alkaloid palau'amine. Many imidazole-containing natural products are biologically active, such as inhibiting the growth of tumors, possessing antibacterial properties, and influencing signaling pathways of cells like an inflammatory response. Access to large quantities of these molecules would aid medical science in drug discovery and design, potentially impacting the overall quality of life for all. It is therefore essential for the chemical community to pursue the synthesis of natural products not only to gain more knowledge in the overall science, allowing for better isolation,characterization, and synthesis of molecules, but also to better the quality of life and health as a whole.Chapter 1 of this dissertation describes the isolation and characterization of spiroleucettadine and terrazoanthines A-C. It further describes, in detail, the unsuccessful attempts to synthesis spiroleucettadine, which prompted its structural revision, and the only reported synthesis of the revised structure.Chapter 2 focuses on our approach to the total synthesis of spiroleucettadine. Initially our strategy centered on employing a novel reaction discovered in our lab to help facilitate the construction of the spirocyclic center. However, we later found this route to not be viable,leading to a significant revision in our strategy.In chapter 3 describe our approach to total synthesis of terrazoanthines A-C. Besides its purification and structural assignment,there are no reports pertaining to this molecule in the literature. Of the 3 molecules, only one of them possesses multiple stereochemical centers. However, upon further examination of the core structure we proposed a concise synthetic route leading to not only all 3 molecule, all possible stereoisomers through the construction of a key symmetric intermediate.In chapter 4 we discuss the oxidative chemistry of tetrahydrobenzimidazole. The two oxidants used were dimethyldioxarine and oxaziridine. The results show the choice of oxidant, N-protecting group,and the functionalization at the C2-position can greatly affect the outcome of the reactions, leading to additions, cyclizations, and ring openings.

Advanced Drug Design And Development: A Medicinal Chemistry Approach

Author : P N Kourounakis
Publisher : CRC Press
ISBN 13 : 1134995296
Total Pages : 199 pages
Book Rating : 4.1/5 (349 download)

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Book Synopsis Advanced Drug Design And Development: A Medicinal Chemistry Approach by : P N Kourounakis

Download or read book Advanced Drug Design And Development: A Medicinal Chemistry Approach written by P N Kourounakis and published by CRC Press. This book was released on 1994-03-31 with total page 199 pages. Available in PDF, EPUB and Kindle. Book excerpt: Reporting the rapidly growing field of rational drug design, this work is composed from a selected, topical range of chapters written by specialists in each field.

Bioactive Heterocycles

Author :
Publisher :
ISBN 13 :
Total Pages : pages
Book Rating : 4.:/5 (123 download)

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Book Synopsis Bioactive Heterocycles by :

Download or read book Bioactive Heterocycles written by and published by . This book was released on with total page pages. Available in PDF, EPUB and Kindle. Book excerpt:

Imidazole and Benzimidazole Synthesis

Author : M. R. Grimmett
Publisher : Academic Press
ISBN 13 : 9780080534459
Total Pages : 265 pages
Book Rating : 4.5/5 (344 download)

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Book Synopsis Imidazole and Benzimidazole Synthesis by : M. R. Grimmett

Download or read book Imidazole and Benzimidazole Synthesis written by M. R. Grimmett and published by Academic Press. This book was released on 1997-06-02 with total page 265 pages. Available in PDF, EPUB and Kindle. Book excerpt: Imidazole and Benzimidazole Synthesis is a comprehensive survey of the known methods of syntheses and ring modification. It brings together the multitude of synthesis of the imidazole ring in a systemic way interms of specific bond formation, and recommends the most attractive synthetic approaches. It also collects non-ring-synthetic approaches to classes of compounds such as nitro-, halogeno-, and amino-imidazoles, and covers the synthesis of N-substituted compounds and preparations of specific isomers. The only book in print dealing specifically with this topic Comprehensive survey of the known methods of synthesis and ring modification Recommends the most attractive synthetic approaches

Heterocyclic Chemistry in Drug Discovery

Author : Jie Jack Li
Publisher : John Wiley & Sons
ISBN 13 : 1118354435
Total Pages : 688 pages
Book Rating : 4.1/5 (183 download)

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Book Synopsis Heterocyclic Chemistry in Drug Discovery by : Jie Jack Li

Download or read book Heterocyclic Chemistry in Drug Discovery written by Jie Jack Li and published by John Wiley & Sons. This book was released on 2013-04-26 with total page 688 pages. Available in PDF, EPUB and Kindle. Book excerpt: Enables researchers to fully realize the potential to discover new pharmaceuticals among heterocyclic compounds Integrating heterocyclic chemistry and drug discovery, this innovative text enables readers to understand how and why these two fields go hand in hand in the effective practice of medicinal chemistry. Contributions from international leaders in the field review more than 100 years of findings, explaining their relevance to contemporary drug discovery practice. Moreover, these authors have provided plenty of practical guidance and tips based on their own academic and industrial laboratory experience, helping readers avoid common pitfalls. Heterocyclic Chemistry in Drug Discovery is ideal for readers who want to fully realize the almost limitless potential to discover new and effective pharmaceuticals among heterocyclic compounds, the largest and most varied family of organic compounds. The book features: Several case studies illustrating the role and application of 3, 4, 5, and 6+ heterocyclic ring systems in drug discovery Step-by-step descriptions of synthetic methods and practical techniques Examination of the physical properties for each heterocycle, including NMR data and quantum calculations Detailed explanations of the complexity and intricacies of reactivity and stability for each class of heterocycles Heterocyclic Chemistry in Drug Discovery is recommended as a textbook for organic and medicinal chemistry courses, particularly those emphasizing heterocyclic chemistry. The text also serves as a guide for medicinal and process chemists in the pharmaceutical industry, offering them new insights and new paths to explore for effective drug discovery.

Privileged Scaffolds in Medicinal Chemistry

Author : Stefan Bräse
Publisher : Royal Society of Chemistry
ISBN 13 : 1782620303
Total Pages : 486 pages
Book Rating : 4.7/5 (826 download)

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Book Synopsis Privileged Scaffolds in Medicinal Chemistry by : Stefan Bräse

Download or read book Privileged Scaffolds in Medicinal Chemistry written by Stefan Bräse and published by Royal Society of Chemistry. This book was released on 2015-11-20 with total page 486 pages. Available in PDF, EPUB and Kindle. Book excerpt: This book addresses the various classes of privileged scaffolds and covers the history of their discovery and use.

Drug-like Properties: Concepts, Structure Design and Methods

Author : Li Di
Publisher : Elsevier
ISBN 13 : 0080557619
Total Pages : 549 pages
Book Rating : 4.0/5 (85 download)

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Book Synopsis Drug-like Properties: Concepts, Structure Design and Methods by : Li Di

Download or read book Drug-like Properties: Concepts, Structure Design and Methods written by Li Di and published by Elsevier. This book was released on 2010-07-26 with total page 549 pages. Available in PDF, EPUB and Kindle. Book excerpt: Of the thousands of novel compounds that a drug discovery project team invents and that bind to the therapeutic target, typically only a fraction of these have sufficient ADME/Tox properties to become a drug product. Understanding ADME/Tox is critical for all drug researchers, owing to its increasing importance in advancing high quality candidates to clinical studies and the processes of drug discovery. If the properties are weak, the candidate will have a high risk of failure or be less desirable as a drug product. This book is a tool and resource for scientists engaged in, or preparing for, the selection and optimization process. The authors describe how properties affect in vivo pharmacological activity and impact in vitro assays. Individual drug-like properties are discussed from a practical point of view, such as solubility, permeability and metabolic stability, with regard to fundamental understanding, applications of property data in drug discovery and examples of structural modifications that have achieved improved property performance. The authors also review various methods for the screening (high throughput), diagnosis (medium throughput) and in-depth (low throughput) analysis of drug properties. Serves as an essential working handbook aimed at scientists and students in medicinal chemistry Provides practical, step-by-step guidance on property fundamentals, effects, structure-property relationships, and structure modification strategies Discusses improvements in pharmacokinetics from a practical chemist's standpoint

Privileged Scaffolds in Drug Discovery

Author : Bin Yu
Publisher : Elsevier
ISBN 13 : 044318612X
Total Pages : 988 pages
Book Rating : 4.4/5 (431 download)

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Book Synopsis Privileged Scaffolds in Drug Discovery by : Bin Yu

Download or read book Privileged Scaffolds in Drug Discovery written by Bin Yu and published by Elsevier. This book was released on 2023-07-19 with total page 988 pages. Available in PDF, EPUB and Kindle. Book excerpt: Privileged Scaffolds in Drug Discovery is the most complete and up-to-date work in the area. Covering a wide range of privileged structures, it is a perfect reference for scientists involved in targeted drug development. The editors recruited epserts from several prestigious Chinese institutions to cover the areas of antiviral drugs, chalcone, pyrimidine, (benz)imidazoles, natural product-derived privileged scaffolds, N-Sulfonyl carboxamides, kinase inhibitors, antitumor molecules, antineurodegenerative drugs, triazoles, oxazolidinone, indole and indoline scaffolds, tigliane diterpenoids, peptide and peptide-based drugs, quassinoids, and others including pseudonatural products, macrocycles, stable peptides and peptidomimetics. The book also explores scaffolds in drug molecules approved in recent years. Privileged Scaffolds in Drug Discovery is a complete reference for researchers in drug discovery and organic synthesis, in academic and corporate settings, who are investigating privileged structures upon which to base new drugs. Researchers in medicinal chemistry and chemical biology will also find the contents of this book valuable. Provides wide coverage of privileged scaffolds in new drug discovery Includes complex and diverse natural product scaffolds Covers applications to peptides and peptide-based drugs

Chemistry and Applications of Benzimidazole and its Derivatives

Author : Maria Marinescu
Publisher : BoD – Books on Demand
ISBN 13 : 1789845521
Total Pages : 230 pages
Book Rating : 4.7/5 (898 download)

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Book Synopsis Chemistry and Applications of Benzimidazole and its Derivatives by : Maria Marinescu

Download or read book Chemistry and Applications of Benzimidazole and its Derivatives written by Maria Marinescu and published by BoD – Books on Demand. This book was released on 2019-10-02 with total page 230 pages. Available in PDF, EPUB and Kindle. Book excerpt: Finding new strategies for synthesizing benzimidazole derivatives and functionalizing the benzimidazole core has proved to be important due to the compound's various applications in medicine, chemistry, and other areas. The multitude of benzimidazole derivatives marketed as drugs has led to intensive research in the field for the discovery of new biologically active structures. The general applications of benzimidazole derivatives in materials chemistry, electronics, technology, dyes, pigments, and agriculture open up new research horizons. This book guides the rational design of benzimidazole derivatives synthesis with certain applications. Chapters cover such topics as therapeutic use of benzimidazole in conditions like diabetes, viruses, and parasitic diseases; X-ray crystal structure of selected benzimidazole derivatives; benzimidazole compounds for cancer therapy; and others.

Strategies for Organic Drug Synthesis and Design

Author : Daniel Lednicer
Publisher : John Wiley & Sons
ISBN 13 : 9780470399590
Total Pages : 700 pages
Book Rating : 4.3/5 (995 download)

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Book Synopsis Strategies for Organic Drug Synthesis and Design by : Daniel Lednicer

Download or read book Strategies for Organic Drug Synthesis and Design written by Daniel Lednicer and published by John Wiley & Sons. This book was released on 2009-03-04 with total page 700 pages. Available in PDF, EPUB and Kindle. Book excerpt: This book examines and evaluates the strategies utilized to design and synthesize pharmaceutically active agents. Significant updates over the last 10 years since the publication of the 1st edition include synthesis of enantiomerically pure isomers, novel chemical methodologies, and new pharmaceutical agents targeted at novel biological endpoints. Written by an experienced successful author, this book meets the needs of a growing community of researchers in pharmaceutical R &D, as well as medical professionals, by providing a useful guide for designing and synthesizing pharmaceutical agents. Additionally, it is a useful text for medicinal chemistry students.

Fragment-Based Drug Discovery

Author : Steven Howard
Publisher : Royal Society of Chemistry
ISBN 13 : 1849739080
Total Pages : 314 pages
Book Rating : 4.8/5 (497 download)

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Book Synopsis Fragment-Based Drug Discovery by : Steven Howard

Download or read book Fragment-Based Drug Discovery written by Steven Howard and published by Royal Society of Chemistry. This book was released on 2015-07-03 with total page 314 pages. Available in PDF, EPUB and Kindle. Book excerpt: Fragment-based drug discovery is a rapidly evolving area of research, which has recently seen new applications in areas such as epigenetics, GPCRs and the identification of novel allosteric binding pockets. The first fragment-derived drug was recently approved for the treatment of melanoma. It is hoped that this approval is just the beginning of the many drugs yet to be discovered using this fascinating technique. This book is written from a Chemist's perspective and comprehensively assesses the impact of fragment-based drug discovery on a wide variety of areas of medicinal chemistry. It will prove to be an invaluable resource for medicinal chemists working in academia and industry, as well as anyone interested in novel drug discovery techniques.

Multicomponent Reactions towards Heterocycles

Author : Erik Van der Eycken
Publisher : John Wiley & Sons
ISBN 13 : 3527349081
Total Pages : 626 pages
Book Rating : 4.5/5 (273 download)

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Book Synopsis Multicomponent Reactions towards Heterocycles by : Erik Van der Eycken

Download or read book Multicomponent Reactions towards Heterocycles written by Erik Van der Eycken and published by John Wiley & Sons. This book was released on 2022-03-21 with total page 626 pages. Available in PDF, EPUB and Kindle. Book excerpt: Presents a wide-ranging overview of essential topics and recent advances in MCR chemistry Heterocycles are a central component in natural product chemistry, pharmaceuticals, agrochemicals, and material science. New synthetic methodologies integrating the sequencing of multicomponent reactions (MCRs) are today being used for the rapid synthesis of diversified heterocycles in just one step. Multicomponent Reactions towards Heterocycles presents an up-to-date summary MCR chemistry with a focus on the conjugation between modern synthetic methodologies and MCRs. Featuring contributions by leaders in the field, this comprehensive resource highlights applications of MCRs in natural products and intermediate synthesis, discusses current trends and future prospects in MCR chemistry, outlines novel multicomponent procedures, and more. The authors provide the practical information required for designing new reaction strategies and mechanisms, covering topics including MCR-based green synthetic methods, cyclization and cycloaddition reactions, heterocycle multicomponent syntheses in a continuous flow, catalytic alkynoyl generation, MCR synthesis of saturated heterocycles, and C–H functionalization and multicomponent reactions. Provides a thorough overview of heterocycles as input in multicomponent reactions Discusses recent advances in the field of MCR chemistry and progress in the synthesis and functionalization of heterocycles Demonstrates the use of MCRs to simplify synthetic design and achieve complexity and diversity in novel bioactive molecules Highlights examples of multicomponent polymerizations, target-oriented synthesis, and applications of MCR in medicinal chemistry Explains the methodology of using on-resin MCRs to produce heterocycle compounds Illustrating the key role of MCRs towards heterocycles in natural product synthesis, drug discovery, organic synthesis, and other applications, Multicomponent Reactions towards Heterocycles is required reading for synthetic chemists in academia and industry alike.

Biomolecular Simulations in Structure-Based Drug Discovery

Author : Francesco L. Gervasio
Publisher : John Wiley & Sons
ISBN 13 : 3527342656
Total Pages : 368 pages
Book Rating : 4.5/5 (273 download)

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Book Synopsis Biomolecular Simulations in Structure-Based Drug Discovery by : Francesco L. Gervasio

Download or read book Biomolecular Simulations in Structure-Based Drug Discovery written by Francesco L. Gervasio and published by John Wiley & Sons. This book was released on 2019-04-29 with total page 368 pages. Available in PDF, EPUB and Kindle. Book excerpt: A guide to applying the power of modern simulation tools to better drug design Biomolecular Simulations in Structure-based Drug Discovery offers an up-to-date and comprehensive review of modern simulation tools and their applications in real-life drug discovery, for better and quicker results in structure-based drug design. The authors describe common tools used in the biomolecular simulation of drugs and their targets and offer an analysis of the accuracy of the predictions. They also show how to integrate modeling with other experimental data. Filled with numerous case studies from different therapeutic fields, the book helps professionals to quickly adopt these new methods for their current projects. Experts from the pharmaceutical industry and academic institutions present real-life examples for important target classes such as GPCRs, ion channels and amyloids as well as for common challenges in structure-based drug discovery. Biomolecular Simulations in Structure-based Drug Discovery is an important resource that: -Contains a review of the current generation of biomolecular simulation tools that have the robustness and speed that allows them to be used as routine tools by non-specialists -Includes information on the novel methods and strategies for the modeling of drug-target interactions within the framework of real-life drug discovery and development -Offers numerous illustrative case studies from a wide-range of therapeutic fields -Presents an application-oriented reference that is ideal for those working in the various fields Written for medicinal chemists, professionals in the pharmaceutical industry, and pharmaceutical chemists, Biomolecular Simulations in Structure-based Drug Discovery is a comprehensive resource to modern simulation tools that complement and have the potential to complement or replace laboratory assays for better results in drug design.

Molecular Biology of the SARS-Coronavirus

Author : Sunil K. Lal
Publisher : Springer Science & Business Media
ISBN 13 : 364203683X
Total Pages : 330 pages
Book Rating : 4.6/5 (42 download)

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Book Synopsis Molecular Biology of the SARS-Coronavirus by : Sunil K. Lal

Download or read book Molecular Biology of the SARS-Coronavirus written by Sunil K. Lal and published by Springer Science & Business Media. This book was released on 2010-03-10 with total page 330 pages. Available in PDF, EPUB and Kindle. Book excerpt: SARS was the ?rst new plague of the twenty-?rst century. Within months, it spread worldwide from its “birthplace” in Guangdong Province, China, affecting over 8,000 people in 25 countries and territories across ?ve continents. SARS exposed the vulnerability of our modern globalised world to the spread of a new emerging infection. SARS (or a similar new emerging disease) could neither have spread so rapidly nor had such a great global impact even 50 years ago, and arguably, it was itself a product of our global inter-connectedness. Increasing af?uence and a demand for wild-game as exotic food led to the development of large trade of live animal and game animal markets where many species of wild and domestic animals were co-housed, providing the ideal opportunities for inter-species tra- mission of viruses and other microbes. Once such a virus jumped species and attacked humans, the increased human mobility allowed the virus the opportunity for rapid spread. An infected patient from Guangdong who stayed for one day at a hotel in Hong Kong led to the transmission of the disease to 16 other guests who travelled on to seed outbreaks of the disease in Toronto, Singapore, and Vietnam, as well as within Hong Kong itself. The virus exploited the practices used in modern intensive care of patients with severe respiratory disease and the weakness in infection control practices within our health care systems to cause outbreaks within hospitals, further amplifying the spread of the disease. Health-care itself has become a two-edged sword.

The DNA Replication-Repair Interface

Author :
Publisher : Academic Press
ISBN 13 : 0323907342
Total Pages : 454 pages
Book Rating : 4.3/5 (239 download)

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Book Synopsis The DNA Replication-Repair Interface by :

Download or read book The DNA Replication-Repair Interface written by and published by Academic Press. This book was released on 2021-11-12 with total page 454 pages. Available in PDF, EPUB and Kindle. Book excerpt: Replication-Coupled Repair, Volume 661 in the Methods in Enzymology series, highlights new advances in the field, with this new volume presenting interesting chapters on a variety of timely topics, including the Repair of replication-born DNA breaks by sister chromatid recombination, High resolution and high throughput DNA cyclization measurements to interrogate DNA bendability, A programmable detection method for genomic signatures: from disease diagnosis to genome editing, Characterization of the telomerase modulating activities of yeast DNA helicases, Eukaryotic DNA replication with purified budding yeast proteins, Single molecule studies of yeast Rad51 paralogs, Light activation and deactivation of Cas9 for DNA repair studies, and more. Other chapters explore MIDAS: Direct sequencing to map mitotic DNA synthesis and common fragile sites at high precision, Studying the DNA damage response in embryonic systems, GLASS-ChIP to map Mre11 cleavage sites in the human genome, New chemical biology approaches to trap reaction intermediates in living cells, Single-molecule imaging approaches for monitoring replication fork conflicts at genomic DNA G4 structures and R-loops in human cells, Monitoring the replication of structured DNA through heritable epigenetic change, Visualizing replication fork encounters with DNA interstrand crosslinks, and much more. Provides the authority and expertise of leading contributors from an international board of authors Presents the latest release in Methods in Enzymology series Includes the latest information on replication-coupled repair

Computation in BioInformatics

Author : S. Balamurugan
Publisher : John Wiley & Sons
ISBN 13 : 1119654718
Total Pages : 354 pages
Book Rating : 4.1/5 (196 download)

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Book Synopsis Computation in BioInformatics by : S. Balamurugan

Download or read book Computation in BioInformatics written by S. Balamurugan and published by John Wiley & Sons. This book was released on 2021-10-19 with total page 354 pages. Available in PDF, EPUB and Kindle. Book excerpt: COMPUTATION IN BIOINFORMATICS Bioinformatics is a platform between the biology and information technology and this book provides readers with an understanding of the use of bioinformatics tools in new drug design. The discovery of new solutions to pandemics is facilitated through the use of promising bioinformatics techniques and integrated approaches. This book covers a broad spectrum of the bioinformatics field, starting with the basic principles, concepts, and application areas. Also covered is the role of bioinformatics in drug design and discovery, including aspects of molecular modeling. Some of the chapters provide detailed information on bioinformatics related topics, such as silicon design, protein modeling, DNA microarray analysis, DNA-RNA barcoding, and gene sequencing, all of which are currently needed in the industry. Also included are specialized topics, such as bioinformatics in cancer detection, genomics, and proteomics. Moreover, a few chapters explain highly advanced topics, like machine learning and covalent approaches to drug design and discovery, all of which are significant in pharma and biotech research and development. Audience Researchers and engineers in computation biology, information technology, bioinformatics, drug design, biotechnology, pharmaceutical sciences.