Fundamentals of MedicinalChemistryBy Gareth Thomas.

Wiley, Chichester 2003. 302 pp. , soft cover$ 30.00.–ISBN 0-470-84307-1

A number of aspects of synthetic, bioor-ganic and physical organic chemistry canbe illustrated with relevant examplesfrom the realm of medicinal chemistry.Furthermore, the pharmaceutical indus-try is a major employer of chemists andbiochemists. Consequently, a series ofmedicinal chemistry lectures often formsa component of chemistry programmes.

This book is aimed at second andthird year undergraduates taking such acourse against a background of chemis-try or biochemistry. Although this bookmay invite comparison with the author';searlier Medicinal Chemistry, it is aimed ata different market. The book assumesonly a level of chemical knowledge thatwould be obtained from the first year ofa chemistry course. It makes very few de-mands on biological knowledge and itincludes in the appendices some essen-tial details of cellular structure and func-tion.

The opening two chapters of the bookset the subject in the context of bio-organic chemistry and aim to provide anoverview of medicinal chemistry in orderto develop a framework for the succeed-ing chapters. There is a discussion of theclassification of drugs, their absorption,distribution, metabolism and excretion.The next four chapters are concernedwith the factors that are involved in thedesign of a drug, the developmentof structure±activity relationships andnewer combinatorial methods of synthe-sis. The remaining chapters exemplifydrug action at particular targets, phar-macokinetics and drug metabolism, withthe final chapters being concerned withthe synthesis and production of a drug.Each chapter is accompanied by ques-

tions covering the major points. The an-swers are given at the end of the book,where there is also guidance for furtherreading.

The book is nicely presented, and thechapters contain clear headings for thevarious sections. Keywords are set inbold. However, there are a few errors inthe formulae. It is a pity that the bookdid not discuss more of the aetiology ofa disease and then the various strategiesthat have been developed to combat it.Nevertheless, this is an interesting anduseful book that fulfils its purpose inproviding a foundation of medicinalchemistry.

Jim HansonUniversity of Sussex (UK)DOI: 10.1002/cbic.200300160

Methods and Principles inMedicinal Chemistry Vol. 21:Molecular Biology inMedicinal ChemistryEdited by Theodor Dingermann,Dieter Steinhilber and Gerd Folkers.

Wiley-VCH, Weinheim 2004. 413 pp. , hardcover E 149.00.–ISBN 3-527-30431-2

The elucidationof the humangenome and thehuge number oftargets is a truechallenge for me-dicinal chemistry.The criteria fortarget selectionand the drugabili-ty of the targets are now even more im-portant. What does the target do withincells and how do you monitor it in acomplex system? Where to start? Whatto synthesize and how? All this in a

single book titled Molecular Biology inMedicinal Chemistry?

The 14 chapters by just as many au-thors or teams are grouped into foursections: molecular targets; synthesis ;analysis; and kinetics, metabolism, andtoxicology. This order reflects the re-search process in pharmaceutical indus-try. The first chapter lists cellular assaysin drug discovery and addresses the ex-perienced reader. This is a particularlycrucial task for the authors. They rushthrough a general review and slowdown a little to focus on assay tech-nologies; such as FRET, BRET, FLIPR,AlphaScreen¦, reporter genes, andenzyme fragment complementation. Thedescriptions are very brief (1=2±1 pageper assay), and detailed information isgiven only occasionally for GPCRs, ionchannels, and reporter-gene assays fortransmembrane receptors. Some assaysare summarized in nice flow charts, butthe physicochemical background of theassays remains in a black box for now(most of them will be discussed in fol-lowing chapters). The opportunity to dis-cuss false positives and negatives wasmissed. Only reporter-gene assays aretreated at the necessary depth. Thesecond chapter : gene knockout models,deals with the manipulation of embryon-ic stems cells to generate knockoutmouse models. The descriptions and fig-ures are very instructive; the drug resist-ance/sensitivity markers Neomycine/Gan-ciclovir are well explained, so is the gen-eration of blastocysts and the breedingpattern. The ten pages for the novice arefollowed by twelve pages on conditionalknockouts using LoxP/CRE, the tetracy-cline-responsive system, transgenic mice,Drosophila and finally the morpholinooligos in Zebra fish embryos. Two con-cise chapters follow on GPCRs: reporter-gene assays and the ligand hunt fororphan GPCRs. FLIPR and Ca2+-mediatedsignaling are pulled out of the black boxnow. The rather small Part II is devoted

Fundamentally Medicinal

ChemBioChem 2004, 5, 1153 ± 1156 www.chembiochem.org ¹ 2004 Wiley-VCH Verlag GmbH&Co. KGaA, Weinheim 1153