Document Report Card
Basic Information
ID: ALA1134419
Journal: Bioorg Med Chem Lett
Title: Solution-Phase parallel synthesis of 5-carboxamido 1-benzyl-3-(3-dimethylaminopropyloxy)-1H-pyrazoles as activators of soluble guanylate cyclase with improved oral bioavailability.
Authors: Selwood DL, Brummell DG, Glen RC, Goggin MC, Reynolds K, Tatlock MA, Wishart G.
Abstract: A lipophilicity constrained library of 5-carboxamido 1-benzyl-3-(3-dimethylaminopropyloxy)-1H-pyrazoles was prepared by solution-phase parallel synthesis with removal of acidic by-products using the strongly basic MP-carbonate resin. Compounds show both activation of soluble guanylate cyclase and inhibition of platelet aggregation. Compound 12 also shows 22% oral bioavailability in rats.
CiteXplore: 11327597