Journal
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
Volume 97, Issue -, Pages 778-785Publisher
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2014.11.064
Keywords
Drug design; Heterocycle; Benzoxazole; Oxazolopyridine; Oxazolopyrazine
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Funding
- Lundbeck foundation
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The benzoxazole heterocycle is often found in ligands targeting a plethora of receptors and enzymes. By analysis of published X-ray structures, this review aims at highlighting key interactions which the benzoxazole may engage in with its host protein. Furthermore, bioavailability, metabolism and the use of benzoxazole as a bioisostere are discussed. The review is extended to cover structure activity relationship studies of 2-substituted benzoxazoles, 2-substituted oxazolopyridines, and in perspective, application of the recently published novel heterocycle oxazolopyrazine in medicinal chemistry studies. (C) 2014 Elsevier Masson SAS. All rights reserved.
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