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Novel YC-1 analogue compound 58 selectively and potently inhibits PAR4-dependent platelet activation.
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1-Benzyl-3-(5'-hydroxymethyl-2'-furyl)indazole (28, YC-1) was selected as the lead compound for systemic structural modification. After screening for antiplatelet activity, SARs of YC-1 analogues were established. Among these potent active derivatives, compounds 29, 30, 31, 44, and 45 functioned as potent activators of sGC and inhibitors of PDE5 with potency comparable to that of YC-1. In addition, compound 58 was found to be a selective and potent inhibitor of protease-activated receptor type 4 (PAR4)-dependent platelet activation.
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Lee et al. (2001) studied this question. 1-Benzyl-3-(5'-hydroxymethyl-2'-furyl)indazole (YC-1) analogues vs. YC-1 was evaluated on Antiplatelet activity, sGC activation, PDE5 inhibition, and PAR4 inhibition. YC-1 analogues functioned as potent sGC activators and PDE5 inhibitors, with compound 58 identified as a selective and potent inhibitor of PAR4-dependent platelet activation.
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