1620517-08-9

Upstream product

• 775302-21-1 3-(5-p-tolyl-1,3,4-oxadiazol-2-yl)aniline 
• 5807-09-0 4-(morpholin-4-yl)butanoic acid 
• 110-91-8 morpholine 
• 1620517-33-0 C₁₉H₁₈IN₃O₂ 
• 311313-24-3 N'-(4-methylbenzoyl)-3-nitrobenzohydrazide 
• 618-94-0 3-nitrobenzoic acid hydrazide 
• 618-95-1 methyl 3-nitrobenzoate 

Relevant academic research and scientific papers

Amide phenyl -1, 3, 4-oxdiazole compound and its preparation method and application

The invention discloses an amidophenyl-1,3,4-oxadiazole compound shown in the formula (I). The invention also discloses a preparation method of the amidophenyl-1,3,4-oxadiazole compound. The preparation method comprises that an amino-compound II and a substituted aliphatic acid III are condensed to form the amidophenyl-1,3,4-oxadiazole compound. The invention also discloses a use of the amidophenyl-1,3,4-oxadiazole compound I in preparation of a drug for treating type II diabetes. The amidophenyl-1,3,4-oxadiazole compound has a non-AMP structure type, can reduce side-effect risk, can obviously inhibit FBPase in a molecule level, can substantially inhibit glucose generation in a cell level, and has good cell viability and good druggability.

Synthesis and structure-activity relationship of non-phosphorus-based fructose-1,6-bisphosphatase inhibitors: 2,5-Diphenyl-1,3,4-oxadiazoles

With the aim of discovering a novel class of non-phosphorus-based fructose-1,6-bisphosphatase (FBPase) inhibitors, a series of 2,5-diphenyl-1,3,4-oxadiazoles were synthesized based on the hit compound (1) resulting from a high-throughput screening (HTS). Structure-activity relationship (SAR) studies led to the identification of several compounds with comparable inhibitory activities to AMP, the natural allosteric inhibitor of FBPase. Notably, compound 22 and 27b, bearing a terminal carboxyl or 1H-tetrazole, demonstrated remarkable inhibition to gluconeogenesis (GNG). In addition, both inhibition and binding mode to the enzyme were investigated by enzymatic kinetics and in silico experiments for representative compounds 16 and 22.