| Literature DB >> 9207948 |
C B Xue1, J Wityak, T M Sielecki, D J Pinto, D G Batt, G A Cain, M Sworin, A L Rockwell, J J Roderick, S Wang, M J Orwat, W E Frietze, L L Bostrom, J Liu, C A Higley, F W Rankin, A E Tobin, G Emmett, G K Lalka, J Y Sze, S V Di Meo, S A Mousa, M J Thoolen, A L Racanelli, R E Olson.
Abstract
Using isoxazoline XR299 (1a) as a starting point for the design of highly potent, long-duration GPIIb/IIIa antagonists, the effect of placing lipophilic substituents at positions alpha and beta to the carboxylate moiety was evaluated. Of the compounds studied, it was found that the n-butyl carbamate 24u exhibited superior potency and duration of ex vivo antiplatelet effects in dogs. Replacement of the benzamidin-4-yl moiety with alternative basic groups, elimination of the isoxazoline stereocenter, and reversal of the orientation of the isoxazoline ring resulted in lowered potency and/or duration of action.Entities:
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Year: 1997 PMID： 9207948 DOI： 10.1021/jm960799i
Source DB: PubMed Journal: J Med Chem ISSN： 0022-2623 Impact factor: 7.446