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Book Review Introduction to Medicinal Chemistry. How Drugs Act and Why. By A. Gringauz

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BOOKS
cytochrome does not appear in the table
as such, nor does it in the index;
page 229: in the statement “. . . the C-1
centre is designated as S”,R should appear instead.
WolflPerer Kuhl and Karl-Heinz van Pee
Institut fur Biochemie
der Technische Universitat Dresden
(Germany)
NMR of Polymers. By F: A . Bovey
and P.A . Mireau. Academic Press,
San Diego, 1996. 459 pp., hardcover
%! 85.00.--ISBN 0-12-119765-4
The declared aim of this book is to
provide an overview of the applications of
NMR spectroscopy to polymer characterization. Frank A. Bovey and Peter A.
Mireau have succeeded well in their objective. Naturally, in view of the enormous
growth in the scope of this field, such an
overview cannot cover every aspect of the
current situation, and the authors make
this clear in their preface. Rather than attempting an exhaustive treatment, they
have set out to illustrate the range of
problems in the polymer sciences that can
be solved using NMR spectroscopy. The
particular strength of the book lies in the
adoption of this approach.
Chapter 1 explains the basic principles
of nuclear magnetic resonance at a level
understandable by the nonspecialist. The
authors provide a good introduction to
the subject, with a very broad choice of
material forming a grounding in the subject that is suitable for an interdisciplinary
readership. Thus we find, for example, a
drawing of a cross-section through a superconducting magnet, a description of
the frequency spectrum responsible for
magnetic relaxation, and detailed tables
of chemical shifts. A possible criticism is
that some of the figures are very basic and
lacking in detail, and contribute little to
the reader’s understanding. This applies,
for example, to Figure 1.5 showing the
separation of the alternating magnetic
field into two counterrotating components, and Figure 1.15 illustrating the
origin of the quadrupolar interaction. A
necessarily brief introduction such as this
cannot, of course, be expected to give the
newcomer a real working knowledge. Accordingly, the later discussions of specific
technique areas such as solid-state NMR
spectroscopy or two-dimensional NMR
methods are similarly limited to describing the most important pulse sequences
and the interpretation of the resulting
spectra.
AngrM Chenr Int Ed Engl. 1997.36, No 19
Chapter 2 begins with a brief and lucid
explanation of the different types of constitutional and configurational isomerism
of polymers. The authors then deal with
the various statistical models used to
derive the sequence frequencies of the
polymer chains resulting from different
growth mechanisms.
In Chapter 3 the reader learns how one
can determine the constitution and configuration of a polymer using high-resolution liquid-state NMR spectroscopy. This
chapter achieves its purpose very well by
using a large number of examples to illustrate how NMR spectroscopy can be
used. These begin with regioisomerism in
polythiophenes, and progress to problems
such as solvent association in solutions of
polymethylmethacrylate and polyvinylchloride. The reader’s understanding is
greatly helped by the frequent explanations of how one goes about predicting the
characteristic chemical shift for a given
structural element, using aids such as incremental rules, synthesizing model compounds, or recording multidimensional
spectra. The authors offer many helpful
hints on experimental aspects; for example, they point out that the chemical
shifts of methyl groups are especially sensitive to solvent effects.
Chapters 4 and 5 contain a very wideranging description of the capabilities of
solid-state NMR spectroscopy applied to
polymers. For example, the authors explain how the chain conformations of the
most important technical polymers can be
deduced from features in their 13C NMR
spectra, how one can study long-range
structures using a great variety of NMR
techniques, how the molecular mobilities
of the individual constituents in polymer
blends can be investigated, etc., etc. The
treatment is very up-to-date, as shown,
for example, by the fact that a large proportion of the book is devoted to multidimensional methods. The work is rounded
off by a very informative chapter on applications of NMR imaging.
The authors have been astute in their
choice of topics for inclusion in these
chapters. I noticed one error that has
crept in: in Figure 5.1 showing the spectral density for relaxation processes, the
extreme cases of very slow and very fast
relaxation have been interchanged, and
are opposite to those in Figure 1.8.
Which readers are most likely to benefit
from this book? It does not give enough
background on NMR fundamentals to
enable a newcomer to the field to make
effective use of the methods described. On
the other hand, experienced NMR users
will find nothing new here about techniques, although it may be useful in filling
0 WILEY-VCH Verlag GmbH, D-69451 Weinheim,
1997
gaps in their knowledge of the literature.
Probably those most likely to find the
book useful are postgraduate students
and research scientists who have a special
interest in polymer science and are already
familiar with NMR methods. It will make
them aware of the wide variety of problems that can be investigated using NMR
spectroscopy, and will bridge the gaps in
their knowledge to enable them to use the
techniques effectively. For these readers
the outlay of $85.00 should prove both
worthwhile and profitable.
Bernhard Bliimich
Lehrstuhl fur Makromolekulare Chemie
der Technischen Hochschule
Aachen (Germany)
Introduction to Medicinal Chemistry.
How Drugs Act and Why. By A .
Gringauz. WILEY-VCH, Weinheim, 1997. 721 pp., hardcover,
DM 109.00.-ISBN 0-471-18545-0
Compared to the situation in other
countries, the facilities for teaching
medicinal chemistry in German universities, as an optional extra subject for students of organic or pharmaceutical chemistry, are somewhat rudimentary, despite
the fact that many graduates hope to find
work in pharmaceutical research. It is
not surprising, therefore, that whereas the
classical disciplines of chemistry are
served by a few good quality works for
each level of study, which have become
established as standard textbooks, it is
difficult to identify corresponding books
in the area of medicinal chemistry. Alex
Gringauz, the author of the book reviewed here, explains that it is intended
for students of pharmaceutical and medicinal chemistry, and aims to provide an introductory overview of this specialized
area of biomedical research. which is of
steadily growing importance. It contains
15 self-contained chapters, the first three
of which introduce the reader to the most
important concepts of the molecular
mechanisms involved in the activity of
pharmaceutical agents. These chapters,
occupying about 90 pages, explain the
principles of the molecular interactions
between low molecular weight compounds and macromolecular target systems, and discuss the various types of
metabolic breakdown reactions undergone by medicinal compounds in the biochemical context. Unfortunately, however, the stereochemical aspects which are
of such importance for pharmaceutical
research are only touched on briefly.
0570-0833/97/3619-2131$ 17.50+ ,5010
2131
BOOKS
After these introductory chapters the
monograph becomes an encyclopedia-like
collection of data, arranged according to
the clinical conditions that the therapeutic
substances are designed to treat. However, this arrangement of the subject matter is contrary to what one might expect in
a modern textbook, as it does not correspond to current practice in pharmaceutical research. Instead we find a rather antiquated juxtaposition of often unrelated
types of compounds under the following
headings: agents for cancer therapy, analgesics, anti-inflammatory agents, antibiotics (two chapters consisting of 140
pages), cholinergic and adrenergic agents,
cardiovascular drugs (two chapters), psychotherapeutic drugs, antihistamines, and
steroids. The final chapter, entitled “New
Developments and New Problems”, occupies a mere twelve pages. Consequently it
contains only very brief treatments of
gene therapy, drug resistance, antisense
technology, cytokins, and the applications of computers in pharmaceutical research.
Unfortunately, this attempt to convey
the essence of pharmaceutical research
fails so badly that it belongs to that generation of textbooks which cannot meet the
standard of a modern works capable of
motivating students. Some important aspects of this field of research are not covered at all, such as the concept of searching for lead structures and subsequent
optimization, the study of structureactivity relationships in the context of the
targeted receptor or enzyme, the importance of combinatorial chemistry in conjunction with high-throughput screening,
and the topic of peptide mimetics, which
has undergone a renaissance in the last
few years. These are just a few of the topics that currently occupy organic chemists
engaged in pharmaceutical research, and
in relation to which this book can offer no
help at all.
On a more positive note, the book deals
with each of the above listed types of clinical conditions against the background of
the physiological processes involved, with
a wealth of detailed medical information.
However, the standard of production, especially with regard to graphical layout, is
much inferior to that normally found in
the chemical literature. For example, the
structural formulas are not numbered
consecutively, and are generally of such
poor quality that it is often difficult to
distinguish between single and multiple
bonds. Moreover, stereogenic centers are
simply ignored, the orientations of substituents (e.g., in perspective representations of cyclohexane rings) are shown in
ways that are very confusing and contrary
2132
to all the usual conventions, and the
mechanisms of organic reactions are misrepresented to such an extent that even the
experienced synthetic chemist will have
difficulty in deciphering the relationship
between educts and products. Here one
begins to doubt whether the manuscript
was ever subjected to copy-editing. It is
not unusual in this book to come across
hypervalent atomic centers in the structural formulas; pentavalent carbon atoms
or tetravalent (neutral) nitrogen atoms
are by no means rare. In the list of contents one occasionally finds a question
mark instead of a page number. The overall appearance of the book in its chemical
parts is more like a hastily prepared lecture manuscript than a modern textbook,
and the reader will be amazed that it has
been put onto the market at all in this
state. When compared with other textbooks on medicinal chemistry that are
currently available, such as those by R. B.
Silverman or by H.-J. Bohm, G. Klebe,
and H. Kubinyi, the book reviewed here
cannot be recommended, either to students or to working chemists. In any case,
it does not really convey the impression of
a textbook intended for students; it is at
best only suitable as a reference source for
use by the scientist who occasionally
needs information about some aspect of
medicinal chemistry. Perhaps it would
be fair to say, in conclusion, that Alex
Gringauz’s Introduction to Medicinal
Chemistry will find few friends in the
books market in view of the competition
from genuine modern textbooks.
Gerhard Miiller
Bayer AG, Leverkusen (Germany)
Spectra Interpretation of Organic
Compounds. (Series: Spectroscopic
Techniques. An Interactive Course.)
By E. Pretsch and J. 7: Clerc.
WILEY-VCH, Weinheim, 1997. xiii,
175 pp., hardcover DM 128.00.ISBN 3-527-28826-0
Spectroscopy is often seen by synthetic
chemists as having a rather low status. It
is only a slight exaggeration to say that
spectroscopy is sometimes regarded as a
necessary evit that one has to accept in
order to meet the minimum requirements
for characterizing a reaction product.
Therefore it is hardly surprising that in
many university chemistry departments
the teaching of spectroscopy is undertaken by a lecturer for whom it is only a
peripheral subject, and the students undergo an obligatory course of a minimal
standard, from which they gain only a
0 WILEY-VCH Verlag GmbH, D-69451 Weinheim,
1997
rudimentary knowledge. As a result of the
low priority afforded to it, spectroscopy
comes to be treated as a rather insignificant little wallflower bordering the main
garden of preparative chemistry. Consequently the chemistry graduate who then
moves into an industrial environment regards analysis as an overhead cost that
should be minimized, so that there is a
tendency, on the grounds of economy, to
turn a blind eye to poor standards of analysis. Synthetic work that is not backed up
by high quality analysis is worthless, and
this fact is likely to be understood by the
student who has learned to evaluate the
capabilities of the various analytical
methods. Any learning tool with the potential for helping to achieve that must be
welcomed. This book by Pretsch and
Clerc is the first volume in a new series
from Wiley-VCH with the general title
Spectroscopic Techniques: An Interactive
Course.
The book is intended to be used as a
self-study course. Its main part consists of
15 chapters, each of which is devoted to a
particular compound whose structure is
to be determined. These are moderately
difficult exercises, with a gentle trend towards increasing difficulty in the later
chapters.
Each chapter begins by showing a mass
spectrum (produced by electron impact
ionization), an IR spectrum (always of a
solution in chloroform), a proton NMR
spectrum (usually at 400 MHz, with expansions of the multiplets), and 13C
NMR spectra under different conditions
(a normal spectrum together with DEPT135 and DEPT-90 spectra for determining
the degree of substitution). UV/vis spectral data are also given in three of the exercises, and in three other cases NMR spectra obtained in different solvents are
shown.
In each case the above listed spectra are
followed by a section explaining how the
empirical formula can be determined
from the spectroscopic data (without access to an elemental analysis or to a highresolution mass spectrum), and how one
can identify the characteristic structural
groups of the unknown compound. Next
it is shown how the partial structures thus
obtained may be fitted together to give the
required molecular structure, and how
one can distinguish between possible isomeric structures. Here, however, the authors must be criticized for failing to mention the existence of two-dimensional and
multidimensional NMR spectra. Surely
nowadays there can hardly remain any
laboratories where the structural analysis
of organic compounds is carried out without the help of 2D NMR spectra! Would
0570-0833/97/3619-2132$ 1 7 50+ .:5010
Anaew. Chem. In!. Ed. E n d 19!37,36, No. 19
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