2195-44-0Relevant articles and documents
Synthesis, anticancer, and computational studies of 1, 3, 4-oxadiazole-purine derivatives
Faisal, Shahla,Kamal, Shagufta,Parveen, Bushra,Rasool, Nasir,Rasul, Azhar,Raza, Zohaib,Shahzadi, Irum,Zahid, Faisal M.,Zahoor, Ameer F.,Zia-ur-Rehman, Muhammad
, p. 2782 - 2794 (2020)
Theophylline-7-acetic acid (acefylline) (3) and its derivatives are pharmacologically active compounds and generally recognized as bronchodilators for the treatment of respiratory diseases like acute asthma for over 70 years. In this article, synthesis of
Synthesis and Anti-Inflammatory Properties of Substituted 5-(Tetrahydro-4-phenyl-2H-pyran-4-yl)-4H-1,2,4-triazole-3-thiols
Arustamyan, Zh. S.,Margaryan,Aghekyan,Panosyan,Muradyan,Tumajyan
, p. 195 - 202 (2021/04/02)
Abstract: 5-(Tetrahydro-4-phenyl-2H-pyran-4-yl)-4H-1,2,4-triazole-3-thiol was synthesized by the reaction of 4-phenyltetrahydropyran-4-carbonyl chloride with thiosemicarbazide and subsequent cyclization of the resulting amide in the presence of KOH. The c
Pyrazoline tethered 1,2,3-triazoles: Synthesis, antimicrobial evaluation and in silico studies
Kumar, Anil,Kumar, Ashwani,Kumar, Lokesh,Lal, Kashmiri,Paul, Avijit Kumar
, (2021/08/03)
A new series of pyrazoline-amide linked 1,2,3-triazole hybrids was wisely designed and synthesized using 1,3-dipolar cycloaddition between pyrazoline linked alkynes and 2-bromo-N-arylacetamide. All the newly synthesized compounds were evaluated in vitro against different microbial strains viz. Escherichia coli, Bacillius subtilis, Staphylococcus aureus, Aspergillus niger, and Candida albicans. Pyrazoline linked terminal alkynes (4a–c) showed MIC = 0.062–0.078 μmol/mL against different bacterial and fungal strain. However, pyrazoline-amide linked 1,2,3-triazole hybrids (6a-6t) showed MIC = 0.0229–0.050 μmol/mL. Compound 6e exhibited better efficacy against E. coli and both the fungal strains compared to standard drugs used. Docking studies of the most potent compounds were carried out against bacterial DNA Gyr A and fungal 14α-steroldemethylase were also performed. The binding potential of 4a and 6e with both the target using molecular dynamics simulations was also investigated.