55327-29-2Relevant academic research and scientific papers
Synthesis of new 2-(thiazol-4-yl)thiazolidin-4-one derivatives as potential anti-mycobacterial agents
Abhale, Yogita K.,Shinde, Abhijit,Shelke, Monika,Nawale, Laxman,Sarkar, Dhiman,Mhaske, Pravin C.
, (2021/07/28)
To search for potent antimycobacterial lead compounds, a new series of 3-substituted phenyl-2-(2-(substituted phenyl)thiazol-4-yl) thiazolidin-4-one (5a-t) derivatives have been synthesized by the condensation of 2-substituted phenyl thiazole-4-carbaldehy
Synthesis, Characterization, and Antimicrobial Screening of 4″-methyl-2,2″-diaryl-4,2′:4′,5″-terthiazole Derivatives
Nalawade, Jitendra,Mhaske, Pravin C.,Shinde, Abhijit,Patil, Sachin V.,Choudhari, Prafulla B.,Bobade, Vivek D.
, p. 1366 - 1374 (2018/04/25)
A series of novel 4″-methyl-2,2″-diaryl-4,2′:4′,5″-terthiazole (8a-p) derivatives has been synthesized and screened for antibacterial activity against four pathogenic bacteria, Escherichia coli, Pseudomonas flurescence, Staphylococcus aureus, and Bacillus subtilis. Among them, compounds 8a and 8j exhibited excellent antibacterial activity with minimum inhibitory concentration range of 1.0 to 5.3?μg/mL and compounds 8m and 8p exhibited moderate to good antibacterial activity with minimum inhibitory concentration range of 16.9 to 29.7?μg/mL against all tested strains. All the synthesized compounds were screened for their in vitro antifungal activity against Cocinida candida. Most of the compounds reported moderate antifungal activity. This study provides valuable directions to our ongoing endeavor of rationally designing more potent antimicrobial agent.
Synthesis, antitubercular and antimicrobial potential of some new thiazole substituted thiosemicarbazide derivatives
Abhale, Yogita K.,Shinde, Abhijit,Deshmukh, Keshav K.,Nawale, Laxman,Sarkar, Dhiman,Mhaske, Pravin C.
, p. 2557 - 2567 (2017/10/06)
The increase in antibiotic resistance due to multiple factors has warranted the need for search of new compounds which are active against multidrug resistant pathogens. In this context a small focused library of thiosemicarbazide derivatives of 2-arylthiazole-4-carbaldehyde, 4-methyl-2-arylthiazole-5-carbaldehyde and 1-(4-methyl-2-arylthiazol-5-yl) ethanone, (5a–l) has been synthesized. The title compounds were screened for inhibitory activity against Mycobacterium tuberculosis H37Ra (ATCC 25177) and Mycobacterium bovis Bacille Calmette Guerin (ATCC 35743) strains. The synthesized compounds, 5a–l were further assayed for their cytotoxic activity against the two human cancer cell lines, HeLa and human colon carcinoma 116 cell lines and showed no significant cytotoxic activity against these two cell lines at the maximum concentration evaluated. Further, the synthesized compounds were found to have potential antibacterial activity against Gram-negative bacteria, Escherichia coli, Pseudomonas flurescence and Gram-positive bacteria, Staphylococcus aureus, Bacillus subtilis. Most of the synthesized compounds showed moderate activity against fungal strain Candida albicans. This study provides valuable directions to our ongoing endeavor of rationally designing more potent antimycobacterial agent.
Heterocycles 38. Biocatalytic synthesis of new heterocyclic mannich bases and derivatives
Leonte, Denisa,Bencze, László Csaba,Paizs, Csaba,Irimie, Florin Dan,Zaharia, Valentin
, p. 12300 - 12313 (2015/08/18)
This paper describes the biocatalytic synthesis of new Mannich bases containing various heterocyclic rings (thiazole, furane, thiophene, pyridine) by applying the lipase catalyzed trimolecular condensation of the corresponding heterocyclic aldehydes with acetone and primary aromatic amines, in mild and eco-friendly reaction conditions. The obtained Mannich bases were acylated to their corresponding N-acetyl derivatives. All compounds were characterized by 1H-NMR, 13C-NMR and MS spectrometry.
Heterocycles 32. Efficient kinetic resolution of 1-(2-arylthiazol-4-yl) ethanols and their acetates using lipase B from Candida antarctica
Hapau, Denisa,Brem, Juergen,Moisa, Madalina,Tosa, Monica-Ioana,Irimie, Florin Dan,Zaharia, Valentin
, p. 88 - 94 (2013/10/22)
In this paper we describe the chemoenzymatic synthesis of new enantiomerically enriched (R)- and (S)-1-(2-arylthiazol-4-yl)ethanols and their acetates by enzymatic enantioselective acetylation of the racemic alcohols rac-2a-d and by methanolysis of the corresponding racemic esters rac-3a-d mediated by lipase B from Candida antarctica (CaL-B) in non-aqueous media. In terms of stereoselectivity and activity, both procedures, acylation and alcoholysis, gave similar good results (50% conversion, E 〉 200). The absolute configuration of the kinetic resolution products was determined by a detailed 1H NMR study of the Mosher's derivatives of (S)-2b.
Synthesis, cytotoxicity assessment, and molecular docking of 4-substituted-2-p-tolylthiazole derivatives as probable c-Src and erb tyrosine kinase inhibitors
Aliabadi, Alireza,Foroumadi, Alireza,Safavi, Maliheh,Ardestani, Sussan K.
, p. 245 - 251 (2014/03/21)
In the current project we focused on the synthesis of 4-Substituted-2-p- tolylthiazole derivatives. Cytotoxicity of synthesized compounds were evaluated against T47D breast cancer cell line and also all of the final compounds 3-7 were docked into the active site of c-Src and erb tyrosine kinases. Compound 4 was the most potent derivative in cytotoxicity assay (IC50 = 2.5 μg/mL) and it was also the most potent inhibitor of erb tyrosine kinase (Binding free energy: -10.18 kcal/mol).
