4-Benzylamino-1-chloro-6-substituted phthalazines: synthesis and inhibitory activity toward phosphodiesterase 5

N Watanabe, Y Kabasawa, Y Takase…

Index: Watanabe, Nobuhisa; Kabasawa, Yasuhiro; Takase, Yasutaka; Matsukura, Masayuki; Miyazaki, Kazuki; Ishihara, Hiroki; Kodama, Kohtarou; Adachi, Hideyuki Journal of Medicinal Chemistry, 1998 , vol. 41, # 18 p. 3367 - 3372

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Citation Number: 152

Abstract

We synthesized various 4-benzylamino-1-chloro-6-substituted phthalazines (15) and 4- benzylamino-1-chloro-7-substituted phthalazines (16) and evaluated their inhibitory activity toward phosphodiesterase 5 (PDE5) purified from porcine platelets. The PDE5-inhibitory activities of 15 were greater than those of the isomers (16). The preferred substituent at the 4- position of phthalazine was a (3-chloro-4-methoxybenzyl) amino group, and those at the 6 ...