91759-68-1Relevant articles and documents
Synthesis, Spectral Evaluation and in Silico Studies of S-Aralkylated 5-(4-methoxyphenyl)-4-phenyl-4H-1,2,4-triazole-3-thiols: As suitable Alzheimer's disease drug candidates
Abbasi, Muhammad Athar,Arfan, Muhammad,Ashraf, Muhammad,Aziz-Ur-Rehman,Khan, Khalid Mohammed,Saleem, Rahman Shah Zaib,Shah, Syed Adnan Ali,Siddiqui, Sabahat Zahra,Zaib, Amna Shah
, p. 694 - 705 (2021/12/31)
Our efforts lay emphasis on synthesis of S-aralkylated 5-(4-OMeC6H5)-4-phenyl-4H-1,2,4-triazol-3-thiols like pharmacologically active candidates to counter neurodegenerative disorder; Alzheimer's disease. A synthetic strategy was instigated by esterifying
Synthesis, molecular docking and evaluation of library of 3-mercapto-1,2,4-triazole derivatives as antimicrobial agents
Gaonkar, Santosh L.,Hakkimane, Sushruta S.,Nayak, Swarnagowri,Shetty, Nitinkumar S.,Swapna, B.
, p. 3039 - 3046 (2021/12/14)
Due to the increasing microbial resistance to antibacterial and antifungal drugs, the development of new antimicrobial agents is an urgent priority. In search of newer antimicrobial agents, a series of 4,5-disubstituted-3-mercapto-1,2,4-triazole derivatives were synthesized from aromatic acids and substituted isothiocyanates. The in silico study was performed to study the binding interactions of the synthesized compounds with the active pocket of CYP51. Among the synthesized 3-mercapto-triazole derivatives, compounds 6r, 6s and 6u exhibited promising antimicrobial activity comparable to standard drugs. The results suggested that the structural modification to 3-mercapto-1,2,4-triazole derivatives could lead to promising antimicrobial scaffolds.
New 1,2,4-triazole-Chalcone hybrids induce Caspase-3 dependent apoptosis in A549 human lung adenocarcinoma cells
Ahmed, Fatma F.,Abd El-Hafeez, Amer Ali,Abbas, Samar H.,Abdelhamid, Dalia,Abdel-Aziz, Mohamed
, p. 705 - 722 (2018/04/17)
A series of novel 1, 2, 4-triazole/chalcone hybrids was prepared and identified with different spectroscopic techniques. The prepared compounds showed remarkable cytotoxic activity against different cancer cell lines. Compounds 24, 25, 27, 41 and 47 had shown the highest cytotoxicity among the tested compounds against human lung adenocarcinoma A549 cells with IC50 ranging from 4.4 to 16.04 μM compared to cisplatin with IC50 of 15.3 μM. Flow cytometric analysis of the tested compounds showed an increase in the number of apoptotic cells in a dose-dependent manner. The further mechanistic study demonstrated that 1, 2, 4-triazole-chalcone hybrids induced apoptosis via increased level of proapoptotic protein Bax, release of cytochrome c from mitochondria and activation of caspase-3/8/9 proteins. However, general caspase inhibition by the pan-caspase inhibitor, z-VAD-fmk, significantly decreased the apoptosis induced by the tested hybrids, suggesting dependency of apoptosis on activation of the caspase-3 pathway.