Title : Synthesis and phosphodiesterase 5 inhibitory activity of new sildenafil analogues containing a phosphonate group in the 5(')-sulfonamide moiety of phenyl ring.

Pub. Date : 2004 May 3

PMID : 15080987






3 Functional Relationships(s)
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1 Synthesis of new sildenafil analogues containing a phosphonate group in the 5(")-sulfonamide moiety of the phenyl ring, 12a-e, 13a-d, and 14a-d, and evaluation of their in vitro PDE5 inhibitory activity are disclosed. Sildenafil Citrate phosphodiesterase 5A Homo sapiens
2 Docking model of (PDE5: 12d) complex shows that the PDE5-bound conformation of 12d matches completely with that of sildenafil, while 12d is partially overlapped with cGMP with ethyl phosphonate group of 12d superimposed onto the cyclic phosphate group of cGMP. Sildenafil Citrate phosphodiesterase 5A Homo sapiens
3 Docking model of (PDE5: 12d) complex shows that the PDE5-bound conformation of 12d matches completely with that of sildenafil, while 12d is partially overlapped with cGMP with ethyl phosphonate group of 12d superimposed onto the cyclic phosphate group of cGMP. Sildenafil Citrate phosphodiesterase 5A Homo sapiens