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Medicinal Chemistry of Steroids

Medicinal Chemistry of Steroids

Author: F. J. Zeelen

Publisher: Elsevier Science Limited

ISBN: UOM:39015019394280

Category: Medical

Page: 357

View: 293

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The many new and fascinating data which have been gathered in the period 1985-1990 have made molecular endocrinology into a mature discipline stimulating creative chemists to design innovative drugs. Within a few years, the primary structures of all the steroid receptor proteins and most of the steroid-converting enzymes have been determined and detailed studies of their mechanism of action at a molecular level have become possible. Medicinal chemists have developed steroidal affinity probes to examine the binding sites of enzymes and receptors, and these investigations were supplemented with studies of modified enzymes and receptors prepared with the aid of site-directed mutagenesis. In view of these rapid scientific developments, the author deemed it appropriate to review the present knowledge of the medicinal chemistry of the steroids. In this book, the discussion is supported by the addition of some chapters which summarize the available data on the biological counterparts of the steroids, the steroid-converting enzymes and the steroid receptors.

Chemistry and Biological Activity of Steroids

Chemistry and Biological Activity of Steroids

Author: Jorge António Ribeiro Salvador

Publisher: BoD – Books on Demand

ISBN: 9781789855159

Category: Science

Page: 142

View: 852

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The steroid scaffold continues to be the structural basis of new drugs for a variety of targets and diseases. Indeed, steroids interact with enzymes and receptors in a strikingly specific manner. Chemistry and Biological Activity of Steroids aims to provide an updated overview of recent advances in the medicinal chemistry of steroids. Novel synthetic methods in the steroids field, including steroid biotransformations, new steroids able to tackle steroid receptors, and steroid enzymes with clinical relevance, are critically reviewed in this book. Furthermore, the diverse physiopathological roles of oxysterols and their therapeutic value are also discussed.

Steroid Dimers

Steroid Dimers

Author: Satyajit Sarker

Publisher: John Wiley & Sons

ISBN: 9781119972846

Category: Science

Page: 392

View: 296

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Steroid dimers are an important group of compounds produced by various marine organisms, and also synthesized in the laboratories. This group of compounds possesses various pharmacological and biological properties, and can also be used to create “molecular umbrellas” for drug delivery. Steroid Dimers: Chemistry and Applications in Drug Design and Delivery provides an up-to-date overview on the chemistry and applications of steroid dimers of natural and synthetic origins. The book includes easy-to-follow synthetic protocols for various classes of important dimeric steroids, source details, valuable spectroscopic data and depiction of unique structural features of natural steroidal dimers, and the Structure-Activity-Relationships (SARs) of some pharmacologically active dimeric steroids. Topics covered include: introduction to steroid dimers synthesis and chemistry of noncyclic and cyclic steroid dimers naturally occurring steroid dimers – cephalostatins, ritterazines and crellastatins biological and pharmacological functions of steroid dimers and their application in drug design and discovery steroid dimers as “molecular umbrellas” for drug delivery Steroid Dimers: Chemistry and Applications in Drug Design and Delivery is an essential guide to this important class of natural and synthetic compounds for researchers and students of natural products chemistry and biochemistry, synthetic organic and medicinal chemistry, and drug design, discovery and delivery.

Medicinal Chemistry

Medicinal Chemistry

Author: Thomas Nogrady

Publisher: Oxford University Press

ISBN: 0195104552

Category: Medical

Page: 649

View: 822

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Fully updated, this textbook takes a receptor-based, target-centred approach, presenting concepts central to the study of drug action in a logical, mechanistic way, grounded on molecular & biochemical principles.

Progress in Medicinal Chemistry

Progress in Medicinal Chemistry

Author:

Publisher: Elsevier

ISBN: 0080862764

Category: Medical

Page: 359

View: 364

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The six reviews in this volume cover once again a most comprehensive range of topics. The anti-malarial activity of the 8-aminoquinolines is examined, with an eye to the development of a single, broad-spectrum drug. Chelation, important in removal of toxic metals from the body, is reviewed for tripositive elements. A new and promising approach to total parenteral nutrition is described. Our indebtedness to the plant origins of many modern drugs is noted in the context of new chemicals. Heterosteroids and receptor-specific opioid peptides constitute two further topics, each case highlighting the wide range of relevant biologically active compounds. Yet another volume challenging the staggering diversity of the field of medicinal chemistry.

Drug Design

Drug Design

Author: E. J. Ariëns

Publisher: Elsevier

ISBN: 9781483216058

Category: Medical

Page: 520

View: 257

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Drug Design, Volume III covers the mode of action of biologically active compounds. The book discusses microbial transformations that have been used in the preparation of drugs or closely related substances; the use of linear free energy parameters and other experimental constants in structure-activity studies; and the mode of action of anticoagulants structurally and functionally related to vitamin K. The text also describes the design of beta-blocking drugs, biologically active acridines, local anesthetics, and insect chemosterilants. The molecular approach for designing inhibitors to enzymes involved in blood clotting is also considered. Chemists, pharmacologists, and people involved in drug design.

Spectroscopic Data of Steroid Glycosides

Spectroscopic Data of Steroid Glycosides

Author: Anwer Basha

Publisher: Springer Science & Business Media

ISBN: 9780387395722

Category: Science

Page: 706

View: 782

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Spectroscopic Data of Steroid Glycosides serves as an essential reference guide containing spectroscopic, physical and biological activity data of over 3500 steroid glycosides, offering the structures and the data of the naturally occurring glycosides of steroids. All compounds are arranged according to the structure of the aglycone, and, in its own class, according to the increasing molecular weight, making Spectroscopic Data of Steroid Glycosides extremely useful for the structure elucidation of new natural products, particularly glycosides. Spectroscopic Data of Steroid Glycosides offers a practical desk reference for all scientists and students interested in steroid glycosides and their biological and medicinal importance. The following data of the steroid glycosides, as available in published literature, are included: - Name of the compound, Chemical name of compound and its structure, - Source, name of the genus, species, authors, family of the biological source from which the glycoside has been isolated, - Melting point, - Specific rotation, - Molecule weight, - Molecular formula, - UV spectral data : maxima, e or log e , solvent, - IR peaks in cm-1 with medium in which the spectrum was taken e.g. KBr, nujol, etc, - Proton magnetic resonance (PMR) chemical shifts, multiplicity of the peaks, coupling constants with assignments, - 13C-NMR (CMR) chemical shifts with assignments, - Mass spectral data with the technique used (e.g. Electron Impact (E.I.), Fast Atom Bombardment (FAB), positive ion or negative ion mode or any other technique, - CD or ORD data, - Biological Activity, - Full reference from which data have been taken.

Molecular Library Synthesis Using Natural Products

Molecular Library Synthesis Using Natural Products

Author: Vasily A. Ignatenko

Publisher:

ISBN: OCLC:1164806448

Category:

Page: 380

View: 912

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Triterpenoids are a broad and structurally diverse class of natural products primarily derived from the plant kingdom. The triterpenoid family consists of nearly thirty thousand members with over two hundred unique carbocyclic skeletons. Consequently, triterpenoids are known to have a wide array of biological activities, including antifungal, anti-inflammatory, anti-cancer, as well as anti-viral and anti-bacterial properties. Considerable efforts in drug discovery have focused on the isolation and structural elucidation of novel triterpenoid molecules from the plant sources. Moreover, semisynthetic triterpenoids, created by further manipulation of the exterior functional groups, have been shown to enhance the potency of their natural precursors. In this regard, the increase in structural complexity of triterpenoid-like molecular libraries through alteration of the carbocyclic core skeleton of the parent natural product can be viewed as a promising tool to study the chemical biology and medicinal chemistry of this natural product family. This work represents a general synthetic strategy for remodeling of a triterpenoid skeleton based on the reactivity patterns of lanosterol, and application of the devised strategy to pentacyclic triterpenoid bryonolic acid. Lanosterol was chosen because of the unsaturated B/C ring fusion, which can undergo iterative allylic oxidation/oxidative cleavage to produce transannular polyketones. These polyketones, in turn, can form distinct molecular skeletons via regio- and stereoselective aldol addition and Norrish-Yang photocyclization. The main advantage of this approach is that instead of relying on reaction development and catalysis to impart stereochemical and regiochemical selectivity, the inherent complexity of the natural product-derived substrates drives stereoselective and regioselective reactions. The central finding described herein is that the subtle changes in the parent triterpenoid, which is subjected to the devised diversification strategy, imparts dramatic effects on the resultant products. Consequently, the devised diversification strategy can be applied to many members of this natural product family with significantly different composition of the resultant molecular library

Frontiers in Medicinal Chemistry , Volume (4)

Frontiers in Medicinal Chemistry , Volume (4)

Author: Atta-ur Rahman

Publisher: Bentham Science Publishers

ISBN: 9781608052073

Category: Medical

Page: 866

View: 807

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""Frontiers in Medicinal Chemistry" is an Ebook series devoted to the review of areas of important topical interest to medicinal chemists and others in allied disciplines. "Frontiers in Medicinal Chemistry" covers all the areas of medicinal chemistry, incl"