Synthesis and biological evaluation of nonpeptide integrin antagonists containing spirocyclic scaffolds |
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| Authors: | Smallheer Joanne M Weigelt Carolyn A Woerner Francis J Wells Jennifer S Daneker Wayne F Mousa Shaker A Wexler Ruth R Jadhav Prabhakar K |
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| Affiliation: | Bristol-Myers Squibb Company, Pharmaceutical Research Institute, PO Box 5400, Princeton, NJ 08543-5400, USA. |
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| Abstract: | ![]()
Analogues of isoxazoline alpha(v)beta(3) antagonist 1 designed to further restrict the four carbon alkyl tether were prepared by incorporating two spirocyclic scaffolds, 1-oxa-2-azaspiro[4,5]dec-2-ene and 1-oxa-2,7-diazaspiro[4,4]non-2-ene. Additional optimization provided potent antagonists of both alpha(v)beta(3) and alpha(5)beta(1) which are selective over GPIIb/IIIa. |
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