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Volume 5 of "Advances in Medicinal Chemistry" contains four
intriguing and detailed accounts of the close interface between
synthetic chemistry, structure-activity relationships,
biochemistry, and pharmacology. In Chapter 1, there is a
comprehensive survey of the immunophilin area specifically
focussing on neuroregenerative applications in the central nervous
system. In Chapter 2, there is an overview of the development of a
potent analgesic compound that works via modulation of neuronal
nicotinic acetylcholine receptors. In Chapter 3, there is a
description of dopamine D-2 autoreceptor partial agonists as
potential therapy for the treatment of schizophrenia. In Chapter 4,
there is a summary of the successful program in which potent
non-peptide inhibitors of HIV protease from the AIDS virus were
developed.
Volume 4 of "Advances in Medicinal Chemistry" is comprised of six
chapters on a wide range of topics in medicinal chemistry,
including molecular modeling, structure-based drug design, organic
synthesis, peptide conformational analysis, biological assessment,
structure-activity correlation, and lead optimization. Chapter 1
presents an account about amino acid-based peptide mimetics
corresponding to b-turn, loop, helical motifs in proteins as a
probe of ligand-receptor and ligand-enzyme molecular interactions.
Chapter 2 addresses new facets of the medicinal chemistry of the
important anticancer drug Taxol(r) (paclitaxel). Chapter 3 relates
an account of the search for new drugs for the treatment of malaria
based on the natural product artemisinin. Chapter 4 applies
computational chemistry to the evaluation of compound libraries for
biological testing. Chapter 5 describes the construction of a
3-dimensional molecular model of the human thrombin receptor, the
first protease-activated G-protein coupled receptor (PAR-1), as a
means to explore the intermolecular contacts involved in agonist
peptide recognition. Finally, Chapter 6 describes the research
conducted at Merck on inhibitors of farnesyl transferase as a
potential treatment for human cancers.
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