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Synthesis and phosphodiesterase 5 inhibitory activity of new sildenafil analogues containing a phosphonate group in the 5′-sulfonamide moiety of phenyl ring

Title
Synthesis and phosphodiesterase 5 inhibitory activity of new sildenafil analogues containing a phosphonate group in the 5′-sulfonamide moiety of phenyl ring
Authors
Kim D.-K.Lee J.Y.Park H.-J.Thai K.M.
Ewha Authors
김대기
SCOPUS Author ID
김대기scopus
Issue Date
2004
Journal Title
Bioorganic and Medicinal Chemistry Letters
ISSN
0960-894XJCR Link
Citation
Bioorganic and Medicinal Chemistry Letters vol. 14, no. 9, pp. 2099 - 2103
Indexed
SCI; SCIE; SCOPUS WOS scopus
Document Type
Article
Abstract
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. Enzyme assays revealed that maximum 10-fold increase in PDE5 inhibitory activity, compared with sildenafil, was achieved by introducing a phosphonate group in the 5′-sulfonamide moiety. 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. © 2004 Elsevier Ltd. All rights reserved.
DOI
10.1016/j.bmcl.2004.02.040
Appears in Collections:
약학대학 > 약학과 > Journal papers
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