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N Thiolated Beta Lactams
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Book Synopsis N-Thiolated B-lactam Antibiotics by : J. Michelle Leslie
Download or read book N-Thiolated B-lactam Antibiotics written by J. Michelle Leslie and published by . This book was released on 2006 with total page pages. Available in PDF, EPUB and Kindle. Book excerpt: ABSTRACT: N-Thiolated beta-lactams are a new class of anti-MRSA and anti-Bacillus agents that have recently been reported by our laboratories. From previous studies performed in our laboratories, it is believed that the N-thiolated beta-lactams exert their antimicrobial activity through a unique mode of action that is completely unlike that of classical beta-lactam antibiotics. In the first chapter of this dissertation, a review of previously prepared N-thiolated beta-lactam analogues and their mode of action is presented. In the second chapter, the synthesis of seven different C3-oxygenated derivatives is described. These analogues were tested for antibacterial activity against Staphylococcus aureus, nine different strains of MRSA, and seven different species of Bacillus. The results of the antibacterial testing will be discussed in relation to the differences in the structures of the analogues. In chapter 3, the design and synthesis of two new, functionalized caprolactone monomers are presented. These monomers were subsequently cooligomerized with epsilon-caprolactone, as described in chapter 4. N-thiolated beta-lactams were attached to the functionalized oligomers. These antibiotic containing oligomers were then screened for activity against MSSA, MRSA, and Bacillus. The results of these biological tests and their implications for future experiments are discussed.
Book Synopsis N-thiolated [beta]-lactams by : Timothy Edward Long
Download or read book N-thiolated [beta]-lactams written by Timothy Edward Long and published by . This book was released on 2003 with total page pages. Available in PDF, EPUB and Kindle. Book excerpt: ABSTRACT: The lipophilic nature of these molecules, which lack the polar side chain functionality of all other microbially-active Beta-lactams, suggests the compounds do not target the penicillin binding proteins within bacterial membranes. The most active members of this Beta-lactam class appear to be those bearing an aryl (Ar) substituent at C4 of the ring. The synthesis and structure-activity relationship of these analogues is discussed in Chapter III. Moreover, microscopy and 3H pulse-labeling studies, which are described in Chapter IV, demonstrate that N-methylthio beta-lactams appear to be inhibitors of protein biosynthesis.
Book Synopsis β-Lactams: Unique Structures of Distinction for Novel Molecules by : Bimal K. Banik
Download or read book β-Lactams: Unique Structures of Distinction for Novel Molecules written by Bimal K. Banik and published by Springer. This book was released on 2012-09-28 with total page 233 pages. Available in PDF, EPUB and Kindle. Book excerpt: I. Ojima • E. S. Zuniga • J. D. Seitz: Advances in the Use of Enantiopure β-Lactams for the Synthesis of Biologically Active Compounds of Medicinal Interests.- I. Fernández • Miguel A. Sierra: β -Lactams from Fischer Carbene Complexes: Scope, Limitations, and Reaction Mechanism.- Bablee Mandal • Basudeb Basu: Synthesis of β-Lactams Through Alkyne–Nitrone Cycloadditions.- T. T. Tidwell: Preparation of Bis-β-Lactams by Ketene–Imine Cycloadditions.- Edward Turos: The Chemistry and Biology of N-Thiolated β-Lactams.- Indrani Banik • Bimal K. Banik: Synthesis of β-Lactams and Their Chemical Manipulations Via Microwave-Induced Reactions.
Book Synopsis N-thiolated [Beta]-lactams by : Bart Allan Heldreth
Download or read book N-thiolated [Beta]-lactams written by Bart Allan Heldreth and published by . This book was released on 2004 with total page pages. Available in PDF, EPUB and Kindle. Book excerpt: And Chapters 5 and 6 demonstrate a novel mode of action and biological target for these drugs using techniques which include target identification, metabolic effects, and reactivity kinetics.
Book Synopsis The Combinatorial Index by : Barry A. Bunin
Download or read book The Combinatorial Index written by Barry A. Bunin and published by Elsevier. This book was released on 1998-04-15 with total page 341 pages. Available in PDF, EPUB and Kindle. Book excerpt: With the explosion of combinatorial solid-phase methods, access to information has become one of the main barriers facing a synthetic chemist who is contemplating a combinatorial approach to a medicinal chemistry problem. The Combinatorial Index is an answer to that problem. This compendium of methods from the primary literature provides quick and convenient access to reliable synthetic transformations as well as information on linkers and analytical methods. Each synthetic procedure is preceded by a section entitled"Points of Interest,"which highlights the strengths and weaknesses of the various studies. The index also covers the use of solution-based synthesis for the generation of molecular diversity. - Organized for rapid retrieval of published information on classes of synthetic transformations, linkers, and analytical methods - Serves as a laboratory manual for bench chemists - Includes a chapter on linkers to assist in choice of linking strategy - Discusses strengths and limitations of the various methods - Contains a structural index showing functional group transformations in solid-phase synthesis
Download or read book Memorendum 1964 Abr. 14 written by and published by . This book was released on 1960 with total page pages. Available in PDF, EPUB and Kindle. Book excerpt:
Book Synopsis Mode of Action and Structure-activity Studies of N-alkylthio Beta-lactams and N-alkylthio-2-oxazolidinones, and Synthesis of Second-generation Disulfide Inhibitors of Beta-Ketoacyl-Acyl Carrer Protein Synthase III (FabH) as Potent Antibacterial Agents by : Kevin David Revell
Download or read book Mode of Action and Structure-activity Studies of N-alkylthio Beta-lactams and N-alkylthio-2-oxazolidinones, and Synthesis of Second-generation Disulfide Inhibitors of Beta-Ketoacyl-Acyl Carrer Protein Synthase III (FabH) as Potent Antibacterial Agents written by Kevin David Revell and published by . This book was released on 2006 with total page pages. Available in PDF, EPUB and Kindle. Book excerpt: ABSTRACT: Work in the Turos group over the past five years has focused on the development of N-alkylthio beta-lactams, which show antibacterial activity against Staphylococcus (including MRSA), Bacillus, and others. These compounds do not function in the manner of the traditional beta-lactam antibiotics, but were thought to undergo an intracellular thiol-transfer to coenzyme A. In expanding the SAR of these novel compounds, it was found that N-alkylthio-2-oxazolidinones also exhibit antibacterial activity. Although CoA acts as the thiol-redox buffer in the genera most susceptible to the N-alkylthio beta-lactams, studies on Coenzyme A disulfide reductase (CoADR) show that the redox buffer is not affected by these compounds. However, the recent finding that fatty acid synthesis is affected by the N-alkylthio beta-lactams led to the discovery that these compounds act as prodrugs, and that the asymmetric CoA disulfides produced by in vivo thiol transfer are potent inhibitors of beta-ketoacyl-acyl carrier protein synthase III (FabH) through a novel thiol-disulfide exchange with the active site cysteine. Lactams 2a and 2g were also found to be potent inhibitors of this enzyme. In an effort to produce a CoA mixed-disulfide mimic which could cross the cell membrane, a series of simple aryl-alkyl disulfides were synthesized and tested against E. coli, S. aureus, and B. subtilis. Several of these compounds were found to be very potent antibacterials both in vitro and in vivo, with MICs less than 0.125 micrograms/mL. Comparison of the activities of these disulfides with those of acyl-CoA analogs and CoA mixed disulfides support the assertion that FabH is indeed the cellular target of these potent new compounds.
Book Synopsis The Chemistry of [beta]-lactams by : Michael I. Page
Download or read book The Chemistry of [beta]-lactams written by Michael I. Page and published by Springer Science & Business Media. This book was released on 1992 with total page 380 pages. Available in PDF, EPUB and Kindle. Book excerpt: This volume provides a review of developments in the chemistry of beta-lactams, particularly in the synthesis, reactivity and mechanisms of reaction, including novel beta-lactam structures and non-beta-lactam analogues.
Book Synopsis Beta-lactams: Natural and Synthetic by : Maghar S. Manhas
Download or read book Beta-lactams: Natural and Synthetic written by Maghar S. Manhas and published by John Wiley & Sons. This book was released on 1971 with total page 264 pages. Available in PDF, EPUB and Kindle. Book excerpt:
Book Synopsis Studies on Antibacterial Activities of N-thiolated Beta-lactams and Their Polymeric Nanoparticles Against Mrsa by : Jeung-Yeop Shim
Download or read book Studies on Antibacterial Activities of N-thiolated Beta-lactams and Their Polymeric Nanoparticles Against Mrsa written by Jeung-Yeop Shim and published by . This book was released on 2003 with total page pages. Available in PDF, EPUB and Kindle. Book excerpt: These results led to the idea about examining a fO-lactam conjugated polymer as a possible pro-drug delivery method, which is the focus of Chapter 3. To synthesize the initial drug-polymer candidate, microemulsion polymerization of an acrylate-substituted lactam was done in aqueous solution to form hydrophilic polymeric nanoparticles containing the highly water-insoluble solid antibiotic, N-methylthio fO-lactam. This method has advantages over the conventional emulsion polymerization methods because a solid co-monomer (fO-lactam drug) can be utilized. SEM studies show that these polymeric nanoparticles have a microspherical morphology with nano-sizes of 40-150 nm. The N-thiolated fO-lactam containing nanoparticles display potent anti-MRSA activity at much lower drug amounts compared with free lactam drug, penicillin G or vancomycin.
Book Synopsis Examination of Potential Anti-Tumor Activity of N-Thiolated B-Lactam Antibiotics in Nude Mice Bearing Human Breast Tumors by :
Download or read book Examination of Potential Anti-Tumor Activity of N-Thiolated B-Lactam Antibiotics in Nude Mice Bearing Human Breast Tumors written by and published by . This book was released on 2006 with total page 136 pages. Available in PDF, EPUB and Kindle. Book excerpt: Activation of the cellular apoptotic program is a current strategy for the prevention and treatment of human cancer including breast cancer. Because of the ease of synthesis and structural manipulation, small molecules with apoptosis-inducing ability have great potential to be developed into chemotherapeutic drugs. The beta-lactam antibiotics have for the past 60 years played an essential role in treating bacterial infections without causing toxic side effects in the host. We hypothesized that active N-thiolated beta-lactams can damage DNA and induce apoptosis in human breast cancer cells in nude mice. In this final report. we have first evaluated potencies of many novel synthetic beta-lactams to inhibit proliferation and induce apoptosis in human cancer cell. We then determined whether several of these beta-lactam, L1, HY2, HY14, HY15 and SC4, could damage breast tumor cell DNA and inhibit breast tumor growth in vivo. We have found that these beta-lactams inhibited growth of implanted MDA-MB-231 breast tumors in a concentration-dependent manner, associated with their DNA-damaging activities. Our studies have provided strong support for proof-of-concept of the potential use of these N-thiolated beta-lactams in breast cancer prevention and treatment.
Book Synopsis Examination Pf Potential Anti-Tumor Activity of N-Thiolated B-Lactam Antibiotics in Nude Mice Bearing Human Breast Tumors by :
Download or read book Examination Pf Potential Anti-Tumor Activity of N-Thiolated B-Lactam Antibiotics in Nude Mice Bearing Human Breast Tumors written by and published by . This book was released on 2005 with total page 85 pages. Available in PDF, EPUB and Kindle. Book excerpt: Activation of the cellular apoptotic program is a current strategy for the prevention and treatment of human cancer including breast cancer. Because of the ease of synthesis and structural manipulation, small molecules with apoptosis-inducing ability have great potential to be developed into chemotherapeutic drugs. The beta-lactam antibiotics have for the past 60 years played an essential role in treating bacterial infections without causing toxic side effects in the host. We hypothesized that active N-thiolated b-lactams can damage DNA and induce apoptosis in human breast cancer cells in nude mice. In this summary report, we have first evaluated potencies of several novel synthetic beta-lactams to inhibit proliferation and induce apoptosis in human cancer cells. We then determined whether one of these b-lactams, HY14, could inhibit breast tumor growth in vivo. We have found that HY14 inhibited growth of implanted MDA-MB-231 breast tumors in a concentrationdependent manner, associated with its DNA-damaging activity. We are currently testing more novel beta-lactams in nude mice bearing human breast tumors. Our studies have provided strong support for proof-of-concept of the potential use of these Nthiolated beta-lactams in breast cancer prevention and treatment.
Book Synopsis Medical Pharmacology and Therapeutics E-Book by : Derek G. Waller
Download or read book Medical Pharmacology and Therapeutics E-Book written by Derek G. Waller and published by Elsevier Health Sciences. This book was released on 2013-08-07 with total page 741 pages. Available in PDF, EPUB and Kindle. Book excerpt: This book covers all the pharmacology you need, from basic science pharmacology and pathophysiology, through to clinical pharmacology to therapeutics, in line with the integrated approach of new medical curricula. The first section covers the basic principles, and the rest is organised by body systems. The book ends with sections on toxicity and prescribing practice. Integrates basic science pharmacology, clinical pharmacology and therapeutics Brief review of pathophysiology of major diseases Case histories and multiple choice questions (and answers) Tabular presentation of all common drugs within each class Section on further reading Kinetics chapter simplified with more practical examples Includes more on genetic issues Drug tables made more concise to make information more accessible Fully updated to reflect current clinical practice
Book Synopsis Biofilms in Infection Prevention and Control by : Steven L. Percival
Download or read book Biofilms in Infection Prevention and Control written by Steven L. Percival and published by Academic Press. This book was released on 2014-01-30 with total page 394 pages. Available in PDF, EPUB and Kindle. Book excerpt: Biofilms in Infection and Disease Control: A Healthcare Handbook outlines the scientific evidence and rationale for the prevention of infection, the role biofilms play in infection control, and the issues concerning their resistance to antimicrobials. This book provides practical guidance for healthcare and infection control professionals, as well as students, for preventing and controlling infection. Biofilms are the most common mode of bacterial growth in nature. Highly resistant to antibiotics and antimicrobials, biofilms are the source of more than 65 percent of health care associated infections (HCAI), which, according to the WHO, affect 1.4 million people annually. Biofilms are involved in 80 percent of all microbial infections in the body, including those associated with medical devices such as catheters, endotracheal tubes, joint prostheses, and heart valves. Biofilms are also the principle causes of infections of the middle-ear, dental caries, gingivitis, prostatitis and cystic fibrosis. Importantly, biofilms also significantly delay wound healing and reduce antimicrobial efficiency in at-risk or infected skin wounds. - Provides specific procedures for controlling and preventing infection - Includes case studies of HCAI, and identifies appropriate treatments - Presents national government standards for infection prevention and control - Includes extensive references and links to websites for further information
Book Synopsis Chemistry and Biology of Beta-Lactams by : Bimal Krishna Banik
Download or read book Chemistry and Biology of Beta-Lactams written by Bimal Krishna Banik and published by CRC Press. This book was released on 2024-11-07 with total page 410 pages. Available in PDF, EPUB and Kindle. Book excerpt: Due to their medicinal activity and potential use as synthetic starting materials, studies on beta-lactams have increased significantly. This unique volume takes readers on a tour de force from the concept of antibiosis to the serendipity of antibiotics, evolution of beta‐lactam development, and molecular biology of antibiotic resistance. These areas of research have culminated in a deeper understanding of microbiology, particularly in the area of bacterial cell wall synthesis and recycling. Considerable work has been performed by chemists and biologists to continue updating their findings about beta-lactam synthesis. Features: Stereoselective synthesis of monocyclic, bicyclic, and polycyclic beta-lactams Microwave, ultrasound, and solid support-mediated preparation of beta-lactams Diverse medicinal activities including anticancer activities of beta-lactams and products obtained from them Nanoparticles, artificial intelligence, and dipole moments in beta-lactam science Synthesis and mechanism of formation of polyaromatic beta-lactams
Download or read book Beta-Lactams written by Bimal K. Banik and published by Springer. This book was released on 2017-05-11 with total page 423 pages. Available in PDF, EPUB and Kindle. Book excerpt: This book presents an essential overview of beta-lactams and their medicinal value and use in the preparation of other biologically active compounds. Written by internationally respected authors, the individual chapters explore beta-lactams’ synthesis, their mechanism of formation, biological effects, and function as base materials for other heterocycles of major importance.
Book Synopsis Synthetic Beta-Lactam Antibiotic as a Selective Breast Cancer Cell Apoptosis Inducer: Significance in Breast Cancer Prevention and Treatment by :
Download or read book Synthetic Beta-Lactam Antibiotic as a Selective Breast Cancer Cell Apoptosis Inducer: Significance in Breast Cancer Prevention and Treatment written by and published by . This book was released on 2005 with total page 78 pages. Available in PDF, EPUB and Kindle. Book excerpt: Activation of the cellular apoptotic program is a current strategy for the prevention and treatment of human cancer, including breast cancer. Because of the ease of synthesis and structural manipulation, small molecules with apoptosis-inducing ability have great potential to be developed into chemotherapeutic drugs. The beta-lactam antibiotics have for the past 60 years played an essential role in treating bacterial infections without causing toxic side effects in the host. The authors hypothesized that active N-thiolated beta-lactams can target a tumor-specific protein or proteins and selectively induce apoptosis in human breast cancer cells, but not in normal cells. In this summary report, they have designed and synthesized a number of beta-lactams with selected C3 ring substituents, and evaluated the potencies of these synthetic beta-lactams to inhibit proliferation and induce apoptosis in human breast cancer cells. They also are investigating whether these N-thiolated beta-lactams can induce apoptosis selectively in breast tumor vs. normal breast cells. They will study the biochemical target of these N-thiolated beta-lactams by synthesizing and using labeled compounds. Their proposed studies should provide strong support for proof-of-concept of the potential use of these N-thiolated beta-lactams in breast cancer prevention and treatment.
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