Essentials of medicinal chemistry (Korolkovas, Andrejus; Burckhalter

Dec 1, 1977 - Essentials of Medicinal Chemistry, Second Edition (Korolkovas, Andrejus). Journal of Chemical Education. Kumli. 1989 66 (6), p A173...
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Essentials of Medicinal Chemistry Andrejus Korolkouas, University of Sa0 Paulo and Joseph H. Burckholter, University of Michigan. John Wiley & Sons, New York, 1976.vi 697 pp. Figs. andta-

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Chemistry

Claude H. Yoder, Fred H. Suydorn, and Fred A. Snouely, Franklin and Marshall College. Harcourt Brace Jovanovich, Inc., New York, 1975. Figs. and tables. 19 X 24 em. xvi 678 pp. $13.96.

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The authors indicate that they are directing this general textbook to the needs of science majors and "serious students whose field of interest lies eIsewhere."kF courses for these groups have tended to diverge in philosophy, level, and style in recent years, textbook efforts aimed at both groups tend to find suitability for one or the other. It is difficult to mesh the need for demonstration of applicability and relevance in a broad hut limited mathematical context, with the need for quantitative rigor and preparation for advanced Levels of chemistry. Motivation strategies differ as well. Yoder, Suydam, and Snavely do not bridge this gap. The teat does merit consideration for the scientists' course, where there are some clear virtues. T h e text is solid. T h e arrangement is logical and ordered. Part One "The Structure and Composition of Matter" consists of ten chapters and 270 pages. It begins with atomic theory, develops the periodicity concept and electronic canfwration of the eiements. Ionic and covalent bonding models are developed with emphasis on correlation with periodic properties. Enthalpy, Entropy and Free Energy are introduced as concepts in connection with gases, and thermodynamics is used extensively from that point forward in the text. "The Reactions of Matter." Part Two is welldcme. Folluwing an rlrmentary and uninspired chapter on kinetics, the conwpt ol equilibrium is devrloprd qualitatively, then c&related to thermodynamic parameters, and quantitatively applied in much detail. ~~~~

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Part Three is "The Chemistry of the Elements." I t begins with a straightforward development of nuclear phenomena, then concludes with an interesting consideration of the birth and evolution of the universe and concomitant formation of the elements. This is perhaps the best single section af the The teat has some significant omissions. While organic chemistry is incorporated through the text, the overall coverage is less extensive than in many general texts. Biochemistry is given short shrift indeed. Descriptive inorganic chemistry is not developed in the later chapters to the extent that it might have been. The importance of chemistry in dealing with complex issues of our times is not emphasized, and this severely limits the text's applicability, in particular for courses for non-science students. With thermodynamics holding such a central place, it could have been straightforward to present a searching analysis of our present energy dilemma. This was not done. In style the book is not scintillating nor likely to strike high student intarest, hut it is well organized and thorough. The editing is first-rate and the drawings are good with the exceptions of a few organic structures (p. 152, 586). The cost is reasonable for a full-year text. For the instructar who wishes to emphasize chemical principles, particularly thermodynamic concepts and periodic properties, this text will serve well. The many and varied problems will he useful in such courses, as will the detailed data tahles of the appendix. I do not find the text useful for the "serious student whose field of interest lies elsewhere"-to say nothing of his or her classmates. James L. Pyla

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Miami University Oxford. Ohio 45056

These two experienced authors on medicinal chemistry topics have produced a textbook designed to provide a chemical insight into a number of biomedical areas. The hook emphasizes the application of principles from basic chemistry, biological science, and medicinal chemistry to the study of pharmacology. In contrast to the classical approach to medicinal chemistry, in depth descriptions of preparative chemical methods, nomenclature, and historical sketches have not been included. The principles of pharmacentics, biopharmaceutin, pharmacokineties and drug metabolism are also left for rhr mwt part toother texts. The hmk israrefully edwd and the Cornat conswent throuahm~t.A typ~rnlihaptrr is divided into three sections: introduction, classification, and mechanism of action. The introduction sections review pertinent hiological and chemical background information in a readable and understandable style. The classification sections, which are more descriptive in nature, present the drugs covered in the chapter by pharmacological or ehemical class. These sections include well drawn structures and figures as well as tahles of drugs giving official,proprietary and chemical names, and chemical structure. Each chapter ends with a one or two page well written, concise description of currently proposed mechanisms of drug action. Suggested reading lists at the end of the chapters provide useful leading referen=. Some of the references cited, however, are for journals or books found only in large medical library collections. The contents include 42 chapters separated into eight parts roughly based on pharmacological classification. Part One (3 chapters) is en excellent distillation of KOrokolvas' previous effort, "Essentials of MOlecular Pharmacology: Background for Drug Design." These chapters describe underlying chemical principles of drug action which can he applied to the specific drug classes discussed in the remainder of the book. Part Two (8 chapters) covers drugs acting on the (Continued on page A498J

Volume 54. Number 12, December 1977 / A497

O kOreviews

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spectrometer. These are psrtirularly useful 1,) the h i n n e r and include such topie S. the effect^ of oaramametic. imouritier. hnu OI~" determine thesignal to noise ratio, the use of vortex plugs, testing for resolution, and checking the instrument's calibration, in addition t o basic operating procedures for a simple machine such as the Varian T-60. These basic, practical discussions are welcomed as they are needed by all students and provide a "hands-on" flavor to the book. Following these chapters, there is anepilogue which, in the briefest terms, alerts the student t o the existence of decoupling, high field spectrometers, shift reagents, other nuclei, Fourier transform spectrometers, and other topics. These discussions are too spane t o provide any concrete knowledge, but do make the student aware of a larger world of nmr techniques and that is valuable. The book is not designed for, nor is it suitable for a more advanced course, such as a graduate course in magnetic resonance. One does not find discussions of nmr relaxation, the Bloch equations, decoupling, INDOR, and other fundamental topics and more elaborate techniques. My only criticism of the book, and it is minor, is that the discussion of magnetic equivalence is so brief as to require further elaboration on the part of the instructor to be understood by students new t o nmr. A discussion of the effects on the spectrum of eachanging nuclei and elementary decoupling should have been included. Auk and Dudek is worth careful consideration by those who are looking far an introductory discussion of proton high resolution nmr, particularly to supplement standard undergraduate courses. ~~~~

central nervous system including general anesthetics, hypnotics and sedatives, anticonvulsants, analgetics, antitussives, psychotherapeutic agents, skeletal muscle relaxants, antiparkinsonian agents, and stimulants. Part Three (9 chapters) includes agents which act on adrenergic and cholinergic systems, antihistamines, and local anesthetics. Part Four (3 chapters) contains a discussion of drugs acting gn the cardiovascular, hematopoietic, and renal systems. Part Five (11 chapters), the longest and most detailed section of the book, emphasizes antiinfectives, antibiotics, antineoplastic agents, and antiviral agents. The last three Parts of the book include brief discussions of vitamins (Part Six, 2 chapters), hormones (Part Seven, 3 chapters), and miscellaneous agents (Part Eight, 2 chapters). A three part index consists of a list of drugs from National Formulary XIV (19751, a list of drugs from U S . Phsnnacopeia XIX (1975), and an index of general topics. Unofficial drugs not listed in these compendia are not indexed as individual agents. The scope of this text appears to be purposefully aimed a t serving as an aid in the understanding of drugs used in therapy today. This text should prove especially valuable in a modern undergraduate pharmacy curriculum in which courses in medicinal chemistry and pharmacology have been combined. patrick S, callery School of Pharmacy University of Meryimd Baltimore, 21201

Stephen '. W. Roeder San D i e p State univerrifv San Diem. Caiifmia 92182

Symmetry Rules lor Chemical Reactions. Orbltal Topology and Elementary Processes

NMR. An Introduction to Proton Nuclear Magnetlc Resonance Spectroscopy

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Ralph G. Pearson, Northwestern University. John Wiley & Sons, New York, 1976. i r + 548 pp. 16 X 24 em. Figs. and tables. $24.50

This slender volume is designed as a companion to the usual organic chemistry text for a junior or senior year course. It would be equally suitable for the nmr portion of a course in instrumental methods. I t is intended as a more detailed introduction to prutun nmr than exist3 in the \ t a n d a d organic tcxt; it fulf~llsthispurp~,severy well. In addition to the 11911al i n t r o d u c t ~ materials r~ and discussion of first-order snectia. it covers distorted firat-order spectra and spectra that cannot h~ rxplninrd by timt-mder nnnlvsis. l ' h r I,wk does this i n a q u a l m t i w was without recourse to quantum mechanicalmethods as is appropriate to a text on this level. An adequate number of problems and illustrative spectra are included. The nicest feature of the hook. in the opinmn of the rwiewer, is the discussi~ncm w n p k preparation and operation uf the nmr

Chemists interested in reaction mechanisms will welcome this thorough and scholarly treatment of symmetry rules. Detailed paths are considered for simple and complex molecules using organic and inorganic examples. A molecular orbital approach is used. In addition to the usual treatment of paths where a t least one symmetry element persists from the reactant to the product, rules are resented based on more general topological properties. The reader is assumed t o he familiar with molecular orbital theory, group theory, and spectroscopy. The first three chapters develop the haekground needed. Selection and symmetry rules for chemical reactions are reviewed. Chapter 3 deals with molecular orbitals and shapes of simple molecules of the types XY., XZY., HXY, HgXY, and HXYz. Conjugated systemsand geometries of wardinated ligands are included also. More than half of the book deals with the

Addison Ault, Cornell College, and Gerald 0. Dudek, Harvard University. Holden-Day, Inc., San Francisco, 1976. viii 141 pp. Figs. and tables. 15 X 23 cm. $4.95, paper.

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A498 / Journal of Chemical Education

detaded mechanismv of reactions, including th,,,~ simple molecu~esc,,v,,v~ in rhaptrr :( nnd more comolex reactions. The uwal organw reactions, a5 well as thaw or organometallic rompuunds are treated. There are sprtlons on oxidalive addirmns, ligand migration, eyeliation, oxidation-reduction, and catalytic reactions. The last chapter concerns photochemical reactions. Structures of moleeules in excited states are examined in terms of the introductory material on molecular ~~~~

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The author index is four times as long as the subject index. This indicates the extensive coverage of the original literature and also the shortcomings of the subject index. The literature seems to be well covered through 1974. There are about ten references from 1975 and one from 1976. One disadvantage for the reader is the widespread use of abbreviations. Few af these appear in the index. A table would he helpful. For example, how does one learn the meaning of GVB (generalized valence bond approach) or P T (perturbation theory)? There are two index entries under g, gold complexes and group theorv. Nothing related t o nerturbation theory appeam in the index. All alrbreviat~anz are erplamrd the i m t rmr thrv are used in the trxt i t the reader mn guess where to look. This is probably the broadest and most thorough approach t o appear a n this important subject. It refleets the author's extensive background in theory and practice of reaction mechanisms. It should heln in the more ~-~~~ wideiprrad application oi thr prinriples w h ~ r bnrr shown here to apply qunr generally. Probably I'earson'u Third Crusade -,ill have even greater impact than the earlier ones-Crystal Field Theory" and "Hard and Soft Acids and Bases." ~

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Bodie Doualas

Theoretical Chemistry: Advances and Perspectives. Volume 1.

Edited by Henry Eyring, University of Utah, and Douglas Henderson, IBM Research Laboratory, San Jose, Ca. Academic Press, New York, 1975. ix 224 pp. Figs. and tables. 15.5 X 23.5 em. $19.50.

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Annual reviews serve as a valuable source of information t o the specialist in almost all fields of science. There he is not only able t o find articles closely related to his own area, but also to obtain an overview of less familiar fields. To fulfill their function, annual reviews should not be so technical as ta be out of reach of a general scientific audience. They must, however, contain extensive references to where the details can be found. Eyring and Henderson have recognized that there previously has existed no annual review which dealt exclusively with theoretical ehemistrv. Thev also realize that theoretical chetniqtn is often enonwusly rquated with quantum chemistry. With thic in mind, they haw created this series in a n ntrempt 10 cover all aspects of theoretical chemistry. This includes for example, statistical mechanics, chemical reactions and collision (Continued on page A50Z)