324572-77-2Relevant articles and documents
1,7- and 2,7-naphthyridine derivatives as potent and highly specific PDE5 inhibitors
Ukita, Tatsuzo,Nakamura, Yoshinori,Kubo, Akira,Yamamoto, Yasuo,Moritani, Yasunori,Saruta, Kunio,Higashijima, Takanori,Kotera, Jun,Fujishige, Kotomi,Takagi, Michino,Kikkawa, Kohei,Omori, Kenji
, p. 2341 - 2345 (2007/10/03)
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.