Pyrazole and isoxazole derivatives as new, potent, and selective 20-hydroxy-5, 8, 11, 14-eicosatetraenoic acid synthase inhibitors

…, N Miyata, K Taniguchi, K Bando, A Koda…

Index: Nakamura, Toshio; Sato, Masakazu; Kakinuma, Hiroyuki; Miyata, Noriyuki; Taniguchi, Kazuo; Bando, Kagumi; Koda, Ayumi; Kameo, Kazuya Journal of Medicinal Chemistry, 2003 , vol. 46, # 25 p. 5416 - 5427

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Citation Number: 67

Abstract

In a previous paper, we reported the N-hydroxyformamidine derivative HET0016 as a potent and selective 20-HETE synthase inhibitor. Despite its attraction as a potential therapeutic agent for cerebral diseases, the preparation of an injectable formulation of HET0016 was limited by its poor solubility under neutral conditions and instability under acidic conditions. The instability of HET0016 in acidic conditions is due to the N-hydroxyformamidine moiety, ...