908802-68-6

Upstream product

• 908581-03-3 5-(4-tert-butoxycarbonylaminophenyl)isoxazole-3-carboxylic acid ethyl ester 
• 54808-56-9 4-(4-nitrophenyl)-2,4-dione-butyric acid ethyl ester 
• 159670-70-9 ethyl 5-(4-nitrophenyl)isoxazole-3-carboxylate 
• 100-19-6 (4-nitrophenyl)ethanone 

Downstream Products

• 1171848-48-8 C₂₉H₂₉N₅O₈ 
• 1612893-63-6 ethyl 4-(5-(4-guanidinophenyl)isoxazole-3-carboxamido)benzoate hydrochloride 
• 1612893-65-8 5-(4-Guanidinophenyl)-N-p-tolylisoxazole-3-carboxamide hydrochloride 
• 1612893-66-9 N-(2,6-dimethylphenyl)-5-(4-guanidinophenyl)isoxazole-3-carboxamide hydrochloride 
• 1612893-69-2 N-(3-bromophenyl)-5-(4-guanidinophenyl)isoxazole-3-carboxamide hydrochloride 
• 1612893-70-5 5-(4-guanidinophenyl)-N-(o-tolyl)isoxazole-3-carboxamide hydrochloride 
• 1613109-50-4 5-(4-guanidinophenyl)-N-(4-(trifluoromethyl)phenyl)isoxazole-3-carboxamide 
• 1612893-73-8 N-(4-chlorophenyl)-5-(4-guanidinophenyl)isoxazole-3-carboxamide hydrochloride 
• 1612893-77-2 5-(4-guanidinophenyl)-N-(naphthalen-1-yl)isoxazole-3-carboxamide hydrochloride 
• 1612893-78-3 5-(4-guanidinophenyl)-N-(m-tolyl)isoxazole-3-carboxamide hydrochloride 
• 1612893-79-4 N-(4-cyanophenyl)-5-(4-guanidinophenyl)isoxazole-3-carboxamide hydrochloride 
• 1613109-58-2 N-(2,3-dimethylphenyl)-5-(4-guanidinophenyl)isoxazole-3-carboxamide 
• 1613109-59-3 N-(4-fluorophenyl)-5-(4-guanidinophenyl)isoxazole-3-carboxamide 
• 1369430-38-5 ethyl 5-(4-benzamidophenyl)isoxazole-3-carboxylate 

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.

Isoxazole moiety in the linker region of HDAC inhibitors adjacent to the Zn-chelating group: Effects on HDAC biology and antiproliferative activity

A series of hydroxamic acid based histone deacetylase inhibitors 6-15, containing an isoxazole moiety adjacent to the Zn-chelating hydroxamic acid, is reported herein. Some of these compounds showed nanomolar activity in the HDAC isoform inhibitory assay

Use of the Nitrile Oxide Cycloaddition (NOC) reaction for molecular probe generation: A new class of enzyme selective histone deacetylase inhibitors (HDACIs) showing picomolar activity at HDAC6

A series of hydroxamate based HDAC inhibitors containing a phenylisoxazole as the CAP group has been synthesized using nitrile oxide cycloaddition chemistry. An HDAC6 selective inhibitor having a potency of ～2 picomolar was identified. Some of the compounds were examined for their ability to block pancreatic cancer cell growth and found to be about 10-fold more potent than SAHA. This research provides valuable, new molecular probes for use in exploring HDAC biology.