Synthesis and SAR of 2-arylbenzoxazoles, benzothiazoles and benzimidazoles as inhibitors of lysophosphatidic acid acyltransferase-beta.

Paper

Synthesis and SAR of 2-arylbenzoxazoles, benzothiazoles and benzimidazoles as inhibitors of lysophosphatidic acid acyltransferase-beta.

Published 2004 · Baoqing Gong, F. Hong, Cory Kohm

Bioorganic & medicinal chemistry letters

Q2 SJR score

7

Citations

0

Influential Citations

Semantic Scholar

Abstract

2-Arylbenzoxazoles, benzothiazoles and benzimidazoles were identified as new classes of potent, isoform specific inhibitors of lysophosphatidic acid acyltransferase-beta (LPAAT-beta). Effects of selected inhibitors on proliferation of tumor cells in vitro were investigated.

Study Snapshot

2-arylbenzoxazoles, benzothiazoles, and benzimidazoles show potential as potent, isoform-specific inhibitors of LPAAT-beta, potentially affecting tumor cell proliferation in vitro.

PopulationOlder adults (50-71 years)

Sample size24

MethodsObservational

OutcomesBody Mass Index projections

ResultsSocial networks mitigate obesity in older groups.

Paper

Synthesis and SAR of 2-arylbenzoxazoles, benzothiazoles and benzimidazoles as inhibitors of lysophosphatidic acid acyltransferase-beta.

References

Citations

Phospholipid Acyltransferases: Characterization and Involvement of the Enzymes in Metabolic and Cancer Diseases

Inhibiting GPAT and AGPAT enzymes may improve treatment of metabolic diseases and cancer by affecting lipid synthesis and their involvement in obesity, insulin resistance, and cancer.

Skin Damages—Structure Activity Relationship of Benzimidazole Derivatives Bearing a 5-Membered Ring System

Compound 10, bearing a pyrrole heterocycle on the benzimidazole ring, shows the best multifunctional properties and potential for developing drugs against skin damage, particularly melanoma.

Chemical modulation of glycerolipid signaling and metabolic pathways.

Glycerolipid metabolism and signaling are attractive targets for new therapies in various fields, and this review simplifies the literature for application in novel systems.

Molecular Design, Synthesis and Cell Based HCV Replicon Assay of Novel Benzoxazole Derivatives

Novel benzoxazole derivatives show significant inhibitory activity against hepatitis C virus, with N-Benzyl-2-phenylbenzo[1,3]oxazole-5-carboxamide (8b) and N-Phenethyl-2-phenylbenzo[1,3

Recent advances on structural modifications of benzothiazoles and their conjugate systems as potential chemotherapeutics

Benzothiazole derivatives show potent anticancer activity and show potential for future drug development, but full toxicity characterization is needed for their clinical usage as safe cancer treatments.