Discovery of a benzimidazole series of ADAMTS-5 (aggrecanase-2) inhibitors by scaffold hopping

S Sogame, Y Suenaga, M Atobe, M Kawanishi…

Index: Sogame, Shinya; Suenaga, Yoshihito; Atobe, Masakazu; Kawanishi, Masashi; Tanaka, Eiichi; Miyoshi, Shiro European Journal of Medicinal Chemistry, 2014 , vol. 71, p. 1 - 9

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Citation Number: 5

Abstract

Abstract We describe a medicinal chemistry approach to generate a series of benzimidazoles bearing thiazolidin-4-one using scaffold hopping from thiazole 1, our previously described thiazole. Our goal was to discover a potent and permeable small- molecule ADAMTS-5 inhibitor. The results suggest that small compound 22 shows promise as a potent small-molecule ADAMTS-5 inhibitor with good permeability.