Bioorganic and Medicinal Chemistry Letters p. 2341 - 2345 (2003)
Update date:2022-08-05
Topics:
Ukita, Tatsuzo
Nakamura, Yoshinori
Kubo, Akira
Yamamoto, Yasuo
Moritani, Yasunori
Saruta, Kunio
Higashijima, Takanori
Kotera, Jun
Fujishige, Kotomi
Takagi, Michino
Kikkawa, Kohei
Omori, Kenji
Novel 1,7- and 2,7-naphthyridine derivatives, designed by the introduction of nitrogen atom into the phenyl ring of previously reported 4-aryl-1-isoquinolinone derivatives, were disclosed as a new structural class of potent and specific PDE5 inhibitors. Among them, 2,7-naphthyridine 4c showed potent PDE5 inhibition (IC50=0.23 nM) and one of the best PDE5 specificities against PDEs1-4,6 (>100,000-fold selective versus PDE1-4, 240-fold selective vs PDE6). This compound showed more potent relaxant effects on isolated rabbit corpus cavernosum (EC30=5.0 nM) than Sildenafil (EC30=8.7 nM). The compound 4c (T-0156) was selected for further biological and pharmacological evaluation of erectile dysfunction.
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