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ID: ALA1138114

Journal: Bioorg Med Chem Lett

Title: Convergent, parallel synthesis of a series of beta-substituted 1,2,4-oxadiazole butanoic acids as potent and selective alpha(v)beta3 receptor antagonists.

Authors: Boys ML, Schretzman LA, Chandrakumar NS, Tollefson MB, Mohler SB, Downs VL, Penning TD, Russell MA, Wendt JA, Chen BB, Stenmark HG, Wu H, Spangler DP, Clare M, Desai BN, Khanna IK, Nguyen MN, Duffin T, Engleman VW, Finn MB, Freeman SK, Hanneke ML, Keene JL, Klover JA, Nickols GA, Nickols MA, Steininger CN, Westlin M, Westlin W, Yu YX, Wang Y, Dalton CR, Norring SA.

Abstract: We describe a series of 1,2,4-oxadiazoles, which are potent antagonists of the integrin alpha(v)beta3 and, in addition, show selectivity relative to the other beta3 integrin alpha(IIb)beta3. In whole cells, the majority of these analogs also demonstrated modest selectivity against other alpha(v) integrins such as alpha(v)beta1 and alpha(v)beta6.

CiteXplore: 16298127

DOI: 10.1016/j.bmcl.2005.11.008