1612893-69-2

Upstream product

• 1612893-55-6 5-(4-guanidinophenyl)isoxazole-3-carboxylic acid hydrochloride 
• 591-19-5 m-Bromoaniline 
• 54808-56-9 4-(4-nitrophenyl)-2,4-dione-butyric acid ethyl ester 
• 159670-70-9 ethyl 5-(4-nitrophenyl)isoxazole-3-carboxylate 
• 908802-68-6 ethyl 5-(4-amino-phenyl)isoxazole-3-carboxylate 
• 100-19-6 (4-nitrophenyl)ethanone 
• 1612893-54-5 5-(4-guanidinophenyl)isoxazole-3-carboxylic acid methyl ester hydrochloride 

Relevant academic research and scientific papers

Isoxazole type of model acrosomal enzyme inhibitor and method for preparing same (by machine translation)

The invention relates to a novel acrosin inhibitor, a preparation method and application in preparation of male antifertility drugs thereof. Specifically, the invention relates to a novel acrosin inhibitor shown as formula I, wherein all substituents are defined as the specification. The invention also relates to the preparation method of the acrosin inhibitor and application of the inhibitor in preparation of male antifertility drugs. (formula I).

Design and synthesis of phenylisoxazole derivatives as novel human acrosin inhibitors

Human acrosin is an attractive target for the discovery of novel male contraceptives. Isoxazole derivative ISO-1, a small-molecule weak human acrosin inhibitor, was used as the starting point for lead optimization. After two rounds of structure-based inhibitor design, a highly potent inhibitor B6 (IC50 = 1.44 μM) was successfully identified, which showed good selectivity over trypsin and represents one of the most active human acrosin inhibitors up to date.