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Author(s): Sperry JB; Wright DL
Title: Furans, thiophenes and related heterocycles in drug discovery
Source: CURRENT OPINION IN DRUG DISCOVERY & DEVELOPMENT 8 (6): 723-740
Date: 2005 NOV
Document Type: Journal : Review
DOI:
Language: English
Comment:
Address: Dartmouth Coll, Dept Chem, Hanover, NH 03755 USA.
Reprint: Wright, DL, Dartmouth Coll, Dept Chem, Hanover, NH 03755 USA.
E-mail: Dennis.L.Wright@Dartmouth.EDU
Author Keywords: azoles; cle-aromatization; drugs; furans; heterocycles; thiophenes
KeyWords Plus: STRUCTURE-BASED DESIGN; BIOLOGICAL EVALUATION; SELECTIVE INHIBITORS;
ANTAGONIST ACTIVITY; RECEPTOR AGONIST; ANTITUMOR AGENTS; ALPHA
AGONISTS; GABA UPTAKE; POTENT; ANALOGS
Abstract: Five-membered aromatic heterocycles containing oxygen and sulfur are key building blocks used in medicinal chemistry applications. Furans, thiophenes and related azole analogs constitute an important class of compounds that are readily available, stable and easily functionalized. In this review, the authors survey the recent literature and highlight the application of such compounds in the development of therapeutic agents. This review focuses on two major strategies involving these compounds. The first is the use of these rings as intact scaffolds within the final target compound, and the second is the use of these compounds as convenient and flexible synthons for non-aromatic structural moieties.
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