85106-59-8Relevant academic research and scientific papers
1,2,4-Triazole and 1,3,4-oxadiazole analogues: Synthesis, MO studies, in silico molecular docking studies, antimalarial as DHFR inhibitor and antimicrobial activities
Thakkar, Sampark S.,Thakor, Parth,Doshi, Hiren,Ray, Arabinda
, p. 4064 - 4075 (2017/07/05)
1,2,4-Triazole and 1,3,4-oxadiazole analogues are of interest due to their potential activity against microbial and malarial infections. In search of suitable antimicrobial and antimalarial compounds, we report here the synthesis, characterization and biological activities of 1,2,4-triazole and 1,3,4-oxadiazole analogues (SS 1-SS 10). The molecules were characterized by IR, mass, 1H NMR, 13C NMR and elemental analysis. The in vitro antimicrobial activity was investigated against pathogenic strains, the results were explained with the help of DFT and PM6 molecular orbital calculations. In vitro cytotoxicity and genotoxicity of the molecules were studied against S. pombe cells. In vitro antimalarial activity was studied. The active compounds were further evaluated for enzyme inhibition efficacy against the receptor Pf-DHFR computationally as well as in vitro to prove their candidature as lead dihydrofolate reductase inhibitors.
Combinatorial approach: Identification of potential antifungals from triazole minilibraries
Bhatia, Manish Sudesh,Zarekar, Bandu Eknath,Choudhari, Prafulla Balkrishna,Ingale, Kundan Bhanudas,Bhatia, Neela Manish
experimental part, p. 116 - 120 (2012/03/10)
Employing basic principles of solution phase combinatorial chemistry, a solution phase combinatorial synthesis and screening of mini libraries of 1,2,4-triazole derivatives has been carried out. 6 x 6 indexed mini libraries were synthesized comprising of 36 compounds. The libraries were analyzed by liquid chromatography - mass spectrometry - mass spectrometry (LC - MS - MS) analysis. All the synthesized mini libraries were screened for antifungal activity and by deconvolution methodology leads for every fungi used for study were identified. The leads were synthesized individually and screened for activity. The antifungal activity of individually synthesized leads was improved as anticipated, in comparison with that of any of the mini libraries. Springer Science+Business Media, LLC 2010.
Push-pull azo-chromophores containing two fused pentatomlc heterocycles and their nonlinear optical properties
Centore, Roberto,Fusco, Sandra,Peluso, Andrea,Capobianco, Amedeo,Stolte, Matthias,Archetti, Graziano,Kuball, Hans-Georg
experimental part, p. 3535 - 3543 (2009/12/01)
We have developed procedures for the synthesis of push-pull azo-chromophores containing the s-triazolo[3,4-b]thiadiazole heterocycle compatible with the presence of electron-acceptor groups (nitrophenyl group) as substituents on both the triazole and thia
In-Vitro anti-HIV and antitumor activity of new 3,6-disubstituted [1,2,4]triazolo[3,4-b][1,3,4]thiadiazoles and thiadiazine analogues
Al-Soud, Yaseen A.,Al-Masoudi, Najim A.,Loddo, Robert,La Colla, Paola
experimental part, p. 365 - 369 (2009/04/06)
A series of [1,2,4]triazolo[3,4-b][1,3,4]thiadiazoles (7-15) and the thiadiazine analogues 16-18 have been synthesized under microwave irradiation (MWI). All synthesized compounds are evaluated for their antiviral activity against the replication of HIV-1 and HIV-2 activity in MT-4. However, compounds 12 and 18 showed EC50 = 2.11 and 1.97 μg/mL. The results suggest that these compounds can be considered as a new lead in the development of antiviral agents. Compounds 4-18 were tested in vitro against a panel of tumor cell lines. All compounds are inactive against all the tumor sub-lines, except 10 which exhibited activity against CD4+ human acute T-lymphoblastic leukaemia of CC50 = 64 μM.
Synthesis of some new 2-methyl-4-(substituted benzylidene) 1-phenyl-1,2,4 triazolo [3,4,-b] 1,3,4 thiadiazole as potential AChE inhibitory agents
Sen,Shanker
, p. 465 - 467 (2007/10/03)
4-(1-aminophenyl) -1,2,4 - triazolo [3,4,-b] 1,3,4-thiadiozole (2) was prepared by treatment of 4-(1-aminophenyl)-5-mercapto-4-amino-1,2,4-S-triazole with carbondisulfide and KOH in methanol. This on further reaction with different 2-methyl-4-(substituted
