Design, synthesis and structure–activity relationship of new HSL inhibitors guided by pharmacophore models

JD Al-Shawabkeh, AH Al-Nadaf, LA Dahabiyeh…

Index: Al-Shawabkeh, Jumana D.; Al-Nadaf, Afaf H.; Dahabiyeh, Lina A.; Taha, Mutasem O. Medicinal Chemistry Research, 2014 , vol. 23, # 1 p. 127 - 145

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Abstract

Abstract Hormone-sensitive lipase (HSL) is a critical enzyme involved in the hormonally regulated release of fatty acids and glycerol from adipocyte lipid stores. Its inhibition may improve insulin sensitivity and blood glucose handling in type 2 diabetes. Accordingly, many small-molecule HSL inhibitors have recently been identified. In continuation of our efforts for discovery of new HSL inhibitors, we prepared a variety of esters, amides, sulfonamides ...