阿伐那非用于治疗勃起功能障碍的发现：一种新型嘧啶-5-甲酰胺衍生物作为一种强效且高度选择性的磷酸二酯酶5抑制剂。
The discovery of avanafil for the treatment of erectile dysfunction: a novel pyrimidine-5-carboxamide derivative as a potent and highly selective phosphodiesterase 5 inhibitor.
作者信息
Sakamoto Toshiaki, Koga Yuichi, Hikota Masataka, Matsuki Kenji, Murakami Michino, Kikkawa Kohei, Fujishige Kotomi, Kotera Jun, Omori Kenji, Morimoto Hiroshi, Yamada Koichiro
机构信息
Medicinal Chemistry Research Laboratories II, Mitsubishi Tanabe Pharma Corporation, 2-2-50 Kawagishi, Toda, Saitama 335-8505, Japan.
Pharmacology Research Laboratories II, Mitsubishi Tanabe Pharma Corporation, 2-2-50 Kawagishi, Toda, Saitama 335-8505, Japan.
出版信息
Bioorg Med Chem Lett. 2014 Dec 1;24(23):5460-5. doi: 10.1016/j.bmcl.2014.10.008. Epub 2014 Oct 28.
Novel pyrimidine-5-carboxamide derivatives bearing a 3-chloro-4-methoxybenzylamino group at the 4-position were identified as potent and highly selective phosphodiesterase 5 inhibitors. Among them, we successfully found 10j (avanafil) which exhibited a potent relaxant effect on isolated rabbit cavernosum (EC30=2.1 nM) and a high isozyme selectivity.
在4位带有3-氯-4-甲氧基苄基氨基的新型嘧啶-5-甲酰胺衍生物被鉴定为强效且高度选择性的磷酸二酯酶5抑制剂。其中，我们成功发现了10j（阿伐那非），它对离体兔海绵体表现出强效舒张作用（EC30 = 2.1 nM）且具有高同工酶选择性。
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