55327-23-6Relevant academic research and scientific papers
Synthesis and antimycobacterial evaluation of new 5-(1-benzyl-1H-1,2,3-triazol-4-yl)-4-methyl-2-arylthiazole derivatives
Shinde, Vikas,Mahulikar, Pramod,Mhaske, Pravin C.,Chakraborty, Shakti,Choudhari, Amit,Phalle, Siddharth,Choudhari, Prafulla,Sarkar, Dhiman
, p. 805 - 819 (2019/04/26)
A new series of 5-(1-benzyl-1H-1,2,3-triazol-4-yl)-4-methyl-2-arylthiazole derivatives, 6a?w have been synthesized by click reaction of substituted benzylazide, 5a?d with 5-ethynyl-4-methyl-2-substituted phenylthiazole, 4a?f. The starting compounds 4-ethy
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.
Synthesis, antimycobacterial screening and molecular docking studies of 4-aryl-4′-methyl-2′-aryl-2,5′-bisthiazole derivatives
Abhale, Yogita K.,Shinde, Abhijit D.,Deshmukh, Keshav K.,Nawale, Laxman,Sarkar, Dhiman,Choudhari, Prafulla B.,Kumbhar, Santosh S.,Mhaske, Pravin C.
, p. 2889 - 2899 (2017/10/06)
A series of 4-aryl-4′-methyl-2′-aryl-2,5′-bisthiazole derivatives (5a–o) were synthesized and screened for inhibitory activity against Mycobacterium tuberculosis H37Ra (ATCC 25177) and Mycobacterium bovis BCG (ATCC 35743) strains. Five lead compounds (5e,
Synthesis and antimicrobial activities of novel series of 3-(4-(2-substituted thiazol-4-yl)phenyl)-2-(4-methyl-2-substituted thiazol-5-yl)thiazolidin-4-one derivatives
Shelke, Shivaji H.,Mhaske, Pravin C.,Narkhade, Sachin,Bobade, Vivek D.
, p. 1151 - 1156 (2014/08/05)
In the present investigation, a novel series of 3-(4-(2-substituted thiazol-4-yl)phenyl)-2-(4-methyl-2-substituted thiazol-5-yl)thiazolidin-4-one derivatives were synthesized by condensation of 2-substituted-4-methylthiazole- 5-carbaldehyde with 4-(2-subs
Synthesis and Antimicrobial Activities of Novel Series of 1-((4-Methyl-2-Substituted Thiazol-5-yl)Methyleneam INO)-2-Substituted Isothiourea Derivatives
Shelke, Shivaji H.,Mhaske, Pravin C.,Hande, Pankaj,Bobade, Vivek D.
, p. 1262 - 1270 (2013/09/23)
A novel series of 1-((4-methyl-2-substituted thiazol-5-yl)methyleneamino)- 2-substituted isothiourea derivatives was synthesized by alkylation of (Z/E)-1-((4-methyl-2-substituted thiazol-5-yl)methylene)thiosemicarbazide with alkylhalide in acetone. All th
Palladium-catalyzed direct arylation of N-heteroarenes with arylsulfonyl hydrazides
Liu, Bo,Li, Jian,Song, Feijie,You, Jingsong
supporting information; experimental part, p. 10830 - 10833 (2012/09/22)
Hydrazides applied: A palladium-catalyzed direct Ci-H arylation of heteroarenes, with arylsulfonyl hydrazides as the arylating reagents, has been developed (see scheme). The reaction is chemoselective, in that arylsulfonyl hydrazides containing halogen substituents can be employed without participation of the halogen substituent in the reaction. The method offers a straightforward approach to a variety of aryl-heteroaryl compounds. Copyright
Palladium-catalyzed desulfitative C-H arylation of heteroarenes with sodium sulfinates
Liu, Bo,Guo, Qiang,Cheng, Yangyang,Lan, Jingbo,You, Jingsong
supporting information; experimental part, p. 13415 - 13419 (2012/01/03)
Desulfitative C-H arylation: Palladium-catalyzed desulfitative C-H arylation of heteroarenes with sodium sulfinates has been disclosed to construct aryl-heteroaryl bonds without the need for any extra ligands (see scheme). Copyright
Thiazole o-quinodimethanes: The generation, electrocyclisation and Diels-Alder reactions of phenyl substituted derivatives
Potter, Andrew J.,Storr, Richard C.
, p. 5293 - 5296 (2007/10/02)
α-(2-Phenyl-4-methylthiazol-5-yl)-α-phenylmethyl acetate 2 undergoes thermal elimination of acetic acid to give the o-quinodimethane 3. In solution this can be intercepted in Diels-Alder reactions but under flash pyrolytic conditions naphthalene-2-thiol is formed by electrocyclisation and fragmentation.
Dialkyl (1,2-Epoxy-3-oxoalkyl)phosphonates as Synthons for Heterocyclic Carbonyl Compounds: Synthesis of Acyl-Substituted Thiazoles, Indolizines, Imidazopyridines and Imidazopyrimidines
Oehler, Elisabeth,El-Badawi, Mahmoud,Zbiral, Erich
, p. 4099 - 4130 (2007/10/02)
Dialkyl phosphonates (1) react with H2O2/Na2CO3 to give the corresponding trans-1,2-epoxy derivatives 2.These, on reaction with thioamides 4-7, afford (1-hydroxy-1-thiazolylalkyl)phosphonates 8-11, with ethyl α-pyridylacetate (indolizinylalkyl)phosphonates 19, with 2-aminopyridine (imidazopyridinylalkyl)phosphonates 20 (together with the α-amino compounds 22) and with 2-aminopyrimidine the (imidazopyrimidinylalkyl)phosphonates 21.On treatment with alkali or by pyrolysis the (1-hetaryl-1-hydroxyalkyl)phosphonates 9-11 and 19-21 yield the corresponding acyl-substituted heterocycles (thiazoles 13-15 and bicyclic acyl compounds 23-25). - The structure of the bicyclic derivatives 19-25 is assigned from the considerable deshielding of their 5-H NMR signals caused by the electron-rich substituents in peri-3-position.Condensation of the epoxyketones 2 with cytosine results in the isomeric (imidazopyrimidinylalkyl)phosphonates 27 and 28, which can be cleaved to the corresponding aldehydes 29 and 30, respectively.
