Benzoxazoles and oxazolopyridines in medicinal chemistry studies

Charles S Demmer; Lennart Bunch

doi:10.1016/j.ejmech.2014.11.064

Benzoxazoles and oxazolopyridines in medicinal chemistry studies

79 Citations (Scopus)

Abstract

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.

Original language	English
Journal	European Journal of Medicinal Chemistry
Volume	97
Pages (from-to)	778-785
Number of pages	8
ISSN	0223-5234
DOIs	https://doi.org/10.1016/j.ejmech.2014.11.064
Publication status	Published - 2015

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title = "Benzoxazoles and oxazolopyridines in medicinal chemistry studies",

abstract = "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.",

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AU - Demmer, Charles S

AU - Bunch, Lennart

PY - 2015

Y1 - 2015

N2 - 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.

AB - 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.

U2 - 10.1016/j.ejmech.2014.11.064

DO - 10.1016/j.ejmech.2014.11.064

M3 - Journal article

C2 - 25487760

SN - 0223-5234

VL - 97

SP - 778

EP - 785

JO - European Journal of Medicinal Chemistry

JF - European Journal of Medicinal Chemistry

ER -

Benzoxazoles and oxazolopyridines in medicinal chemistry studies

Abstract

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