苯环上含有胍基西地那非类似物合成及磷酸二酯酶5抑制活性英文.pdfVIP

学 报 112 Jou rnal of Ch ina Pharm aceu tical U n iversity　20 10 , 41 (2) : 112 - 117 ·论 　文 · Syn th e s is a n d p ho sp ho d ie ste ra se typ e 5 inh ib ito ry a c tiv ity o f s ilde n a fil a n a lo gu e s p o s se s s in g a gu a n id in e g ro up in th e p h e ny l rin g 1 2 3 3 2 2 1 SH I J ing , L IU Zheng ,WAN G Zhen , T IAN Guanghu i , YAN G X iaojun ,WAN G Xuelan , SUN Hongb in , 2 , 3 SHEN J ingshan 1 2 Cen ter f or D rug D iscovery, Ch ina P ha rm aceu tica l Un ivers ity, N anj ing 210009; Top ha rm an S hangha i Co, L td , S hang ha i 3 2 012 09; S hang ha i Institu te of M a teria M ed ica, Ch inese A cadem y of S ciences, S hang ha i 2 012 03, Ch ina Ab s tra c t　In th is study, a serie s of new sildenafil analogue s 1127 po sse ssing a guan id ine group were syn the sized 3 to inve stigate their PD E5 inh ib itory activity and selectivity u sing [ H ] cGM P SPA k it in vitro and efficacy in the rat model of erectionMo st of the compound s showed poten t activity again st PD E5, and more importan tly, several compound s exh ib ited h igher PD E5 selectivity over PD E6 than that of sildenafilStructu reactivity relation sh ip of the se sildenafil analogue s wa s also d iscu ssedW ith in th is serie s of compound s, compound 15 ( IC50