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Journal of Medicinal Chemistry, 1996, Vol. 39, No. 5
Book Reviews
(R) electronic effects; and MR, a measure of size. It is arranged according to distance from hydrogen to aid the design of a varied series. Every chapter of the book is impressive in the wealth of detailed information provided, usually in the form of regression equations. For example the chapter on applications of the Hammett equation has 174 equations. Early QSAR results are presented and many have been re-derived to bring them up to current standards. The equations for similar biological endpoints are compared and contrasted with each other to put each in context with each other and with known biochemistry of the system. The information is put into historical context with extensive referencing starting with Ehrlich, Meyer, and Overton. These books should be studied by anyone practicing computer-assisted molecular design or interested in what can be gained by a QSAR analysis. In view of the recent emphasis on structure-based drug design, the chapter on proteins and enzymes is especially informative in that frequently the structure-activity relationships show electronic effects of substituents on a position remote from the substituent. Such effects would be difficult to discern from molecular graphics analysis and would probably be a challenge for molecular dynamics. It is only by considering hydrophobic, steric, and electronic effects on biological activity that one can understand the basis of structure-activity relationships.
isoquinolines occur in this volume. However, the section devoted to natural products specifically only occupies a page or less, no doubt frustrating natural product chemists. The contributors faced a task of significant magnitude covering a wide time span of literature (references begin in the 1920s and extend to 1990). Generally, they succeeded admirably; insight and mechanistic interpretation are frequently included. However, there are a few sections which seem to be little more than abstract services and compressed ones at that. Delays in manuscript preparation have resulted in a literature gap in book publication in the range of 5-9 years. A curious compound numbering approach was used in the section on hydroxy and thiol derivatives. Numbers appear haphazardly, making the text and diagrams difficult to coordinate. The tables of contents are concise but clearly explanatory; the seven-page index is adequate; however no author index is included. Editorial quality is highsfew typographical errors appear although some structural diagrams are more “crisp” than others. The price of this volume likely dictates that it will be found largely in libraries where it doubtless has already attracted many readers.
Yvonne Connolly Martin Pharmaceutical Products Division Abbott Laboratories Abbott Park, Illinois 60064-3500 JM950902O
Heterocyclic Compounds. Isoquinolines. Volume 38. Part 3. Edited by Gary M. Coppola and Herbert F. Schuster. John Wiley & Sons, Inc., New York. 1995. xi + 552 pp. 16 × 24 cm. ISBN 0-471-62853-7. $225.00. These handsome dark red/dark blue volumes are one of the mainstays of the literature of heterocyclic chemistry. The nearly all-inclusive scope of the series and high quality make them one of the first sources a heterocyclic chemist chooses to gain perspective on the myriad faces of this field. A well-qualified and prestigious group of contributors from both industry and academia and from far-flung sites has cooperated to produce this volume, a valuable and still pertinent compilation of the chemistry of derivatives of isoquinolinessthose bearing basic side chains (Schuster and Kathawala section) and hydroxyl groups or ethercontaining side chains and thiol derivatives (Hoshino, Hara and Umezawa section). The study of the pharmacological or biological activity of these compounds has been the motivation for much of their syntheses and characterization because of the unique activities of many isoquinolines in their own right and because of the presence of an imbedded, conformationally restricted phenethylamine or dopamine moiety in 1,2,3,4-tetrahydro derivatives. Natural product chemistry is also an important aspect of isoquinolines, and over 30 references to natural product
Stephen T. Ross SmithKline Beecham Pharmaceuticals King of Prussia, Pennsylvania 19406-0939 JM9509051
Angiotensin II Receptors Volume 1. Molecular Biology, Biochemistry, and Clinical Perspectives. Edited by Robert R. Ruffolo, Jr. CRC Press, Boca Raton, FL. 1994. 170 pp. 16 × 24 cm. ISBN 0-84938380-3. $99.50; Volume 2. Medicinal Chemistry. 1994. 225 pp. 16 × 24 cm. ISBN 0-8493-8545-3. $99.50. In the last few years our knowledge of the role of angiotensin II and of the receptors through which it operates has advanced rapidly. One important reason for this progress has been the discovery of several series of selective, nonpeptide antagonists of the AII receptors. In addition, the clinical utility of these antagonists has been demonstrated, and the past past few years have seen intensive effort in the pharmaceutical industry to discover and develop AII receptor antagonists. This two-volume set represents a comprehensive but relatively concise review of the biochemistry, pharmacology, and medicinal chemistry of the angiotensin II receptors. The material is timely and extensively referenced, and a subject index is provided. Any medicinal chemist with an interest in this area should find both volumes very readable. The chapter titles and authors of volume 1 are as follows: (1) Introduction: Angiotensin II Receptors by D. P. Brooks and R. R. Ruffolo, Jr.; (2) Angiotensin II Receptor Subclassification by R. M. Edwards and R. R. Ruffolo, Jr.; (3) Molecular Biology of Angiotensin II Receptors by D. J. Bergsma; (4) Angiotensin II Receptor Signal Transduction Mechanisms by R. M. Edwards and R. R. Ruffolo, Jr.; (5) Functions Mediated by Peripheral Angiotensin II Receptors by D. P. Brooks and R. R. Ruffolo, Jr.; (6) Functions Mediated by Angiotensin II
