133262-79-0Relevant academic research and scientific papers
Synthesis of a series of potent and orally bioavailable thrombin inhibitors that utilize 3,3-disubstituted propionic acid derivatives in the P3 position
Tucker, Thomas J.,Lumma, William C.,Dale Lewis,Gardell, Stephen J.,Lucas, Bobby J.,Sisko, Jack T.,Lynch, Joseph J.,Lyle, Elizabeth A.,Baskin, Elizabeth P.,Woltmann, Richard F.,Appleby, Sandra D.,Chen, I.-Wu,Dancheck, Kimberley B.,Naylor-Olsen, Adel M.,Krueger, Julie A.,Cooper, Carolyn M.,Vacca, Joseph P.
, p. 3687 - 3693 (1997)
As part of an effort to prepare efficacious and orally bioavailable analogs of the previously reported thrombin inhibitors 1a,b, we have synthesized a series of compounds that utilize 3,3-disubstituted propionic acid derivatives as P3 ligands.
N-ACRYLOYLPIPERAZINE DERIVATIVES, THEIR PREPARATION AND THEIR USE AS PAF ANTAGONISTS
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, (2008/06/13)
Compounds of formula (I): STR1 wherein R 1 and R 2 is each--R 5,--CH=CH--R 5 or--C C--R 5, wherein R. sup.5 is optionally substituted aryl or aromatic heterocyclic; R 3 is hydrogen, alkyl, cyano or--R 5 ; X is oxygen or sulfur; A is 1,4-piperazin-1, 4-diyl or a 1,4-homopiperazin-1,4-diyl; B' is alkylene, carbonyl, thiocarbonyl, sulfinyl or sulfonyl; and R 4 is optionally substituted phenyl and pharmaceutically acceptable salts thereof have valuable PAF antagonist activity, and may be prepared by reacting a compound containing the piperazine or homopiperazine part of the molecular with a compound containing the other part of the molecule.
