Synthesis, Characterization, and Biological Evaluation of Oxadiazole Derivatives Bearing 5-Phenyl-tetrazole as Osteoclast Differentiation Inhibitors

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Novel oxadiazoles bearing 5-phenyl-tetrazole (5a-k) were designed and efficiently synthesized by treating 2-(5-phenyl-2H-tetrazole-2-yl)acetohydrazide (4) with aromatic carboxylic acids in POCl3 , and their in vitro anti-osteoclastogenic activities were evaluated. In the cell-based osteoclast differentiation model, all compounds (5a-k) inhibited the formation of osteoclasts. In addition, the potential target molecules of compound 5 analogs were predicted with their chemical substructures via a web-based interface, and some of them were found to be related to osteoclast differentiation. Consequently, the scaffold containing oxadiazole-tetrazole in a single molecule and their analogs are of potential use in the design of novel anti-osteoclastogenic therapeutics.
Publisher
WILEY-V C H VERLAG GMBH
Issue Date
2015-09
Language
English
Article Type
Article
Keywords

RECEPTOR ANTAGONISTS; CANCER-CELLS; GM-CSF; BONE; 1,3,4-OXADIAZOLE; ANTIFUNGAL; DESIGN; FUSION; POTENT; AGENTS

Citation

BULLETIN OF THE KOREAN CHEMICAL SOCIETY, v.36, no.9, pp.2247 - 2253

ISSN
0253-2964
DOI
10.1002/bkcs.10436
URI
http://hdl.handle.net/10203/203497
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