Synthesis and phosphodiesterase 5 inhibitory activity of novel pyrido[1,2-e]purin-4(3H)-one derivatives
摘要:
Synthesis and primary SAR of a novel series of 2-phenylpyrido[1,2-e]purin-4(3H)-one derivatives with piperazinyl sulfonamide substituents were described herein. As potential PDE5 inhibitors for erectile dysfunction (ED) treatment, representative compounds exhibit improved selectivity versus PDE1 and PDE6. Meanwhile, compound 3e demonstrated functional efficacy on rabbit corpus cavernosum strip in vitro. (c) 2005 Elsevier Ltd. All rights reserved.
通过咪唑并[1,2 - a ]吡啶-2-羧酰胺与2,2,2-三氟乙酰胺的原始反应,可以方便地制备新型4-氯-2-(三氟甲基)吡啶并[1,2- e ]嘌呤。报告。然后,这些衍生物通过Suzuki-Miyaura和Sonogashira催化有效地交叉偶联,从而以高收率获得具有生物学价值的相关C-4取代吡啶并[1,2- e ]嘌呤。