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Book Review ArzneimittelЧFortschritte 1972 bis 1985. Edited by A. Kleemann E. Lindner and J

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graph. Furthermore, it can be seen just by scanning the list
of contents that the individual methods have received very
unequal treatment as regards length, without there being,
in the introduction for example, any indication of the reasons for this o r of the editors’ aims. The suspicion that is
thereby raised, that this is a rather heterogeneous collection of review articles of different sorts, is reinforced when
reading the book. The individual contributions vary greatly
in breadth of coverage and in depth and quality of treatment, and also in the extent to which they are up-to-date.
As is only to be expected from a collection of individual
articles, there can be no uniformity of style and presentation in this book, and it cannot offer the majority of readers a balanced treatment of the different methods included. It would certainly have helped if the editors had
exercised a tighter coordination of the individual contributions, although the resulting delay in publication would
have made the book less up-to-date. Its appearance should
nevertheless be welcomed, as it has at present no competitor in the analyst’s bookshelves, and the numerous references give rapid access to the original papers.
Dietmar Stiiwer [NB 935 IE]
Institut fur Spektrochemie und
angewandte Spektroskopie
Dortmund (FRG)
Arzneimittel-Fortschritte 1972 bis 1985. Edited by A .
Kleemann, E. Lindner and J. Engel. VCH Verlagsgesellschaft, Weinheim 1987. xiv, 1517 pp., bound,
D M 540.00.--ISBN 3-527-26329-2
This book is a supplementary volume which updates
and extends the five-volume work ‘‘Arzneimittel- Entwicklung, Wirkung und Darstellung”, by Ehrhart and Ruschig, which was published in its second edition in 1972.
In twenty chapters by numerous experts the book deals
with the progress made in pharmaceutical chemistry in the
thirteen years from 1972 to 1985.
The volume begins with a short survey of drug design by
J . K . Seydel, which in 51 pages summarizes the theory of
structure-activity relationships, continuing up to molecular
modelling and computer graphics.
In the second chapter (59 pp.) o n enzyme inhibitors H .
Tschesche reports on reversible proteinase inhibitors, including the renin- and angiotensin-converting enzyme inhibitors and the microbial a-glucosidase inhibitors, but
makes no reference whatever to irreversible enzyme inhibitors such as a-difluoromethylornithine (see, for example,
C. Walsh, Tetrahedron 38 (1982) 871-909). However, some
of these enzyme inhibitors are discussed later, along with
mechanisms, when antihormones are treated in Chapter
In the third, quite short, chapter (36 pp.) 7’.Y. Shen and
P. Dauies summarize the latest developments in the area of
anti-inflammatory agents and the most important methods
for synthesizing them.
In Chapter 4, which is also short (28 pp.), J. A . Vida
reports on progress in psychotropic drugs, from the neuroleptics to the anxiolytic drugs.
Next, in Chapter 5 (281 pp.), several groups of authors
in turn deal with new cardiovascular drugs. A short section
o n sympathomimetics and positive inotropic substances is
followed by a very detailed discussion of the cardiac glycosides. Next antihypertensives are discussed; in addition to
the pure a,-adrenoreceptor antagonists such as Prazosin,
Ketanserin is also included. After covering the centralIy
acting a*-adrenoreceptor agonists of the clonidine type,
the new dopamine agonists such as Fenoldopam are
briefly discussed, followed by drugs with direct myogenic
vasodilatory activity such as Hydralazine and Minoxidil.
Also included under this class of substances is the new,
very interesting potassium dilator BRL-34915, although
the mechanism of its activity was not clarified until after
the chapter was written.
The tables that follow listing substances with activity on
the renin-angiotensin system illustrate the large number of
similar and highly active ACE inhibitors that are currently
being developed, and they also give evidence of the beginning of the very active phase of development in the area of
renin inhibitors and angiotensin-I1 antagonists. Next
comes a brief description of the chemical syntheses of
most of the cardiovascular drugs that are listed here. The
section which follows gives a survey of the development of
beta-receptor blockers, with tables giving in each case the
important intrinsic sympathomimetic activity (ISA). In the
discussion of anti-anginal and anti-hypertensive drugs
(23 pp.), the very important calcium antagonists and their
syntheses are unfortunately only treated very briefly. The
sections that follow summarize developments in vasoactive drugs and nootropics.
In Chapter 6 (21 pp.) D. Borrnann and R . Muschaweck
report briefly on developments in diuretics, but they fail to
mention, in addition to the usual sulfonamide diuretics,
the aldosterone antagonists of the spironolactone-spirorenone type; these are, however, discussed in Chapter 9 on
steroid hormones.
In Chapter 7 (28pp.) A . Nouakoua-Banet, H . Feier, J .
Miiller and H . Zilg discuss blood factors and clotting, and
also fibrinolytics (although the plasminogen activators were
not yet known at the time), and finally blood substitutes.
Chapter 8 (42 pp.) by E. Granzer deals with lipid regulators, briefly describing Compactin and Mevinolin, and
also their use with advantage in combination with bile acid
binding resins such as Cholestipol.
The first part of Chapter 9, by W. Kiinig, consists of
more than 200 pages on regulatory peptides, and is a small
monograph in itself. The treatment of the topic ranges
from Somatostatin via A N F (atrial natriuretic factor), the
encephalins and insulin, through to the interleukins and
tumor necrosis factors (TNF); even structure-activity relationships are discussed for the important peptides. In the
careful and accurate review of progress in steroid hormones by U.Stache in Chapter 9, Part 2 (41 pp.), the only
important development missing is that of the aromatase inhibitors for future treatment of breast and prostate carcinomas, which had already emerged at the time of the review; however, this is briefly covered in Chapter 18.
The discussion of oral hypoglycemic drugs in Chapter
10 (18 pp.) by W. Hitzel and R . Weyer includes, in addition
to stimulators of endogenic insulin synthesis, a brief account of some new substances such as Acarbose and Sorbinil which reduce the blood glucose level.
I n Chapter 11 (87 pp.) G . Beck gives an overview of developments in prostaglandins, thromboxanes and leukotrienes, and assesses their likely future applications in fertility control, and in the treatment of gastric ulcers, and
more especially of cardiovascular disease. Data on the new
thromboxane-synthetase inhibitors and thromboxane antagonists, together with the 5-lipoxygenase inhibitors and
leukotriene antagonists are summarized in short tables.
In Chapter 12 (33 pp.) U. Achterrath-Tuckermann, G .
Dressen, M . MolliPre and J. Engel report on progress in
Angew. Chem. Int. Ed. Engl. 28 (1989) No. I
respiratory drugs, In addition to the antitussives and p2stimulators there is a brief account of the anti-asthmatic/
anti-allergic drugs, but surprisingly the very important cromoglycic acid disodium salt (Intal), although mentioned
briefly in the text, does not appear in the corresponding
table. In the discussion of the latest developments the potentially very important PAF antagonists are mentioned
only in a single sentence, and the thromboxane antagonists
are not mentioned at all, despite the fact that they might
have a very important role in asthma therapy, as well as
the leukotriene antagonists which are discussed in some
In Chapter 13 (30 pp.) J . Szelenyi and H. Schickaneder
describe the most important anti-ulcer drugs, from antiacids via histamine-H, antagonists to the new K + - H + ATP-ase inhibitors.
Chapter 14 ( I 18 pp.) by W. Schrock on antibiotics is confined to a detailed discussion of antibiotics of the p-lactam,
aminoglycoside, macrolide and peptide types; all other antibiotics, e.g. tetracyclins, are either omitted or dealt with
in Chapter 15 by H . Pliimpe (65 pp.), which covers compounds with antiparasitic activity; here the latest developments in treatments against protozoa and in anthelmintics
are described, including the remarkable results obtained
using Praziquantel.
In Chapter 16 (33 pp.) M . Plempel and J. Stetter summarize progress on new antimycotics, and in Chapter 17
(27 pp.) J . Hilfenaus describes developments in antiviral
agents, continuing up to Aciclovir as an inhibitor of the
viral thymidine kinase; this chapter was written before
work related to the AIDS virus came into prominence.
In the report on anti-tumor agents (Chapter 18, 72 pp.)
W. P. Brade and U. Niemeyer discuss the cytostatic drugs,
including the new platinum complexes. They then describe
progress in hormones and antihormones, and discuss,
amongst other topics, the biosynthesis of oestrogen and the
aromatase inhibitors-including the irreversible “suicide
inhibition”, mention of which was omitted from Chapter 2
on enzyme inhibitors. The LHRH analogs such as Buserelin, which are also interesting in this context, receive only a
brief mention here, but they were discussed earlier in
Chapter 9 on regulatory peptides.
In Chapter 19 (66 pp.) a group of authors examine progress in immune stimulation and immune suppression.
After discussing the immune system and how it can be
stimulated by muramyl dipeptides and substances such as
Levamisol or Azimexon, special attention amongst immunosuppressives is given, as expected, to cyclosporin, which
represents a notable therapeutic breakthrough in this
In the 20th and last chapter (1 1 pp.), H . G . Schwick gives
an overview of antibody serums and vaccines, without,
however, mentioning monoclonal antibodies.
Leaving aside the many gaps and omissions in the material covered-e.g. chemotherapeutic compounds such as
the highly effective gyrase inhibitors are missing-one
finds that in many of the chapters the literature cited extends only up to 1981 or 1983, and only a few of the articles list references to work published in 1985 and 1986.
Looking at the volume as a whole, many of the chapters
give very good summaries of the topics covered, and there
are only a very few printing errors. Moreover, most of the
authors have tried to give fair evaluations of other pharmaceutical products in addition to those made by their own
firms, and to give them their rightful place.
It remains a mystery why this work, which is aimed at all
scientists working in the pharmaceutical field, has been
Angew. Chem. Int. Ed. Engl. 28 (1989) No. I
written and published in German, with the exception of
the two chapters by English-speaking authors (Chapter 3
by Chen and Dauies and Chapter 4 by Vida);this limits its
readership to those who can read German texts, and these
are relatively few in international terms. It inevitably limits
the distribution of the work, and this in turn makes the
price so high as to be prohibitive for many. For these reasons such works should in future, as a general principle, be
published only in English, and it should further be borne
in mind that all publications on progress in the pharmaceutical field must compete with, for example, the series
“Annual Reports in Medicinal Chemistry”, which is good
value for money and is nearly always very up-to-date.
Helmut Vorbriiggen [NB 926 IE]
Schering AG, Berlin
Ions in Solution: Basic Principles of Chemical Interactions.
By J . Burgess. Ellis Horwood, Chichester/Halsted Press,
New York 1988. 191 pp., bound, E 15.95.-ISBN 0-74580172-210-470-21059-1
Following the comprehensive monograph “Metal Ions
in Solution” (Ellis Horwood, Chichester 1978,480 pp.), the
same author has now written a shorter version on the same
topic, which nevertheless includes additional material and
has been updated. It is aimed mainly at chemistry students,
and is accompanied by two audio-cassettes (obtainable
from the Royal Society of Chemistry, Distribution Centre,
Letchworth SG6 IHN, Great Britain).
The contents of the book are conveniently arranged in
13 chapters. The first half deals with all the important aspects of the solvation of ions, the main emphasis being on
a detailed description of the behavior of metal cations in
aqueous solution. After an introductory chapter which is
devoted to the dissolution of salts and the hydration of metal cations and of simple and complex anions, the second
chapter introduces solvation numbers, and describes how
these can be determined by NMR spectroscopy or by
measuring ionic mobilities. Chapter 3 describes the types
of information that can be obtained from X-ray and neutron diffraction measurements on electrolyte solutions (radial distribution functions, ion-solvent distances), and
Chapter 4 gives an account of the use of spectroscopic and
thermochemical methods to determine the strength of intermolecular ion-solvent interactions.
This is followed in Chapter 5 by a description of the
Brernsted acidlbase behavior of aqua-metal ions, their hydrolysis, and their polymerization to form polynuclear
bridged aqua-complexes, and their stability constants are
discussed in Chapter 6. An appropriate amount of attention is given here to selective cation solvators such as coronands, cryptands and naturally occurring crown ethers
(valinomycin, monactin, monensin). Concluding this half
of the book, Chapter 7 deals with the redox potentials of
the aqua-metal ions and of the complexes derived from
them by ligand exchange.
The second half of the book is concerned with kinetic
and thermodynamic aspects of ion solvation. The first topics treated are solvent exchange reactions between solution and solvento-metal ions (Chapter 9), complex formation between solvento-metal ions and polydentate openchain or macro(po1y)cyclic ligands (Chapter lo), associative and dissociative substitution in complex ions (Chapter
ll), and redox reactions involving an “inner sphere” and
“outer sphere” electron transfer mechanism (Chapter 12).
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1972, kleemann, book, lindner, edited, arzneimittelчfortschritte, bis, review, 1985
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