59940-08-8

Upstream product

• 79-04-9 chloroacetyl chloride 
• 2138-98-9 2-amino-5-(o-chlorophenyl)-1,3,4-oxadiazole 
• 5315-85-5 2-[(2-chlorophenyl)methylene]hydrazinecarboxamide 
• 89-98-5 2-chloro-benzaldehyde 

Downstream Products

• 59940-17-9 N,N-diphenyl-glycine 5-(2-chloro-phenyl)-[1,3,4]oxadiazol-2-ylamide 
• 59940-22-6 N-[5-(2-chloro-phenyl)-[1,3,4]oxadiazol-2-yl]-2-piperidin-1-yl-acetamide 

Relevant academic research and scientific papers

Design, synthesis, and pharmacological evaluation of aryl oxadiazole linked 1,2,4-triazine derivatives as anticonvulsant agents

A series of new clubbed aryl oxadiazole-1,2,4-triazine derivatives (6a-l) were designed and synthesized using appropriate chemical routes. The structures were designed to have the required structural elements for any compounds to be potential anticonvulsant. Preliminary screening of anticonvulsant activity was performed using maximal electroshock seizure (MES), subcutaneous pentylenetetrazole-induced seizure (scPTZ) and behavioral activity were assessed by motor impairment test and actophotometer test. The derivatives 6-((5-(4-methoxyphenyl)-1,3,4-oxadiazol-2-yl)amino)-1,2,4-triazine-3(2H)-thione (6f) and 6-((5-(4-hydroxyphenyl)-1,3,4-oxadiazol-2-yl)amino)-1,2,4-triazine-3(2H)-thione (6g) revealed significant activity against both MES and scPTZ indicating that the compounds are effective against both generalized tonic-clonic and absence seizure. The lead compound (6g) was further evaluated for quantitative evaluation and emerged as the most effective anticonvulsant with median effective dose of 28.5 mg/kg (MES ED50), 76.6 mg/kg (scPTZ) and toxic dose (TD50) was found to be >500 mg/kg. In the GABA estimation study results showed significantly increased GABA concentration. [Figure not available: see fulltext.]

Synthesis, telomerase inhibitory and anticancer activity of new 2-phenyl-4H-chromone derivatives containing 1,3,4-oxadiazole moiety

Based on previous studies, 66 2-phenyl-4H-chromone derivatives containing amide and 1,3,4-oxadiazole moieties were prepared as potential telomerase inhibitors. The results showed most of the title compounds exhibited significantly inhibitory activity on telomerase. Among them, some compounds demonstrated the most potent telomerase inhibitory activity (IC50 50 = 6.41 μM). In addition, clear structure–activity relationships were summarised, indicating that the substitution of the methoxy group and the position, type and number of the substituents on the phenyl ring had significant effects on telomerase activity. Among them, compound A33 showed considerable inhibition against telomerase. Flow cytometric analysis showed that compound A33 could arrest MGC-803 cell cycle at G2/M phase and induce apoptosis in a concentration-dependent way. Meanwhile, Western blotting revealed that this compound could reduce the expression of dyskerin, which is a fragment of telomerase.