Journal of Medicinal Chemistry · 2001 · 118 citations · 6 references
PharmacyMedicinal ChemistryPharmacologyDrug DesignDrug DiscoverySynthetic Medicinal ChemistryAntiplatelet TherapyLead Compound DesignPlatelet ActivationPlatelet AggregationPlatelet FunctionPlatelet PhysiologyAntiplatelet DrugsIndazole SynthesisLead Compound OptimizationLead Compound ScreeningPlatelet Aggregation InhibitionPlatelet InhibitionPlatelet Receptor Signaling
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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A mutation in succinate dehydrogenase cytochrome b causes oxidative stress and ageing in nematodes
Naoaki Ishii, Michihiko Fujii, Philip S. Hartman et al. · Nature · 1998 · 688 citations
Life Sciences, Biology, Genetics +14