22067-29-4Relevant academic research and scientific papers
Design, synthesis and biological evaluation of some novel benzylidene-2-(4-phenylthiazol-2-yl) hydrazines as potential anti-inflammatory agents
Bharti, Sanjay Kumar,Singh, Sushil Kumar
, p. 1004 - 1015 (2014/03/21)
A series of substituted benzylidene-2-(4-phenylthiazol-2-yl) hydrazines (2a-q) have been synthesized, characterized and evaluated for their anti-inflammatory activity by carrageenin-induced hind paw edema (acute inflammation) and cotton pellet granuloma (chronic inflammation) methods in rats. In carrageenin-induced hind paw edema method, compounds 2a, 2b, 2c, 2d, 2h, 2k and 2p at a dose of 20 mg kg-1 body weight, p.o. showed excellent inhibitions (51.80-86.74 %) in between 1 and 4 h. Similarly, in cotton pellet granuloma method, compounds 2a, 2b, 2c, 2d, 2h, 2k and 2p at a dose of 20 mg kg-1 body weight, p.o. inhibited the granuloma formation (71.71-90.19 % inhibition) which was comparable to that of standard drug, ibuprofen (90.36 % inhibition of paw volume at 3 h and 94.02 % inhibition of granuloma formation). Structure activity relationship studies showed excellent activity of the compounds containing electron withdrawing group (fluoro, chloro, bromo or nitro) in phenyl ring at C2 and/or C4 position of thiazole ring.
Study of oxidative cyclization using PhI(OAc)2 in the formation of benzo[4,5]thiazolo[2,3- C ][1,2,4]triazoles and related heterocycles - Scope and limitations
Demmer, Charles S.,Jorgensen, Morten,Kehler, Jan,Bunch, Lennart
, p. 1279 - 1282 (2014/06/10)
A one-pot, two-step reaction for the synthesis of benzo[4,5]thiazolo[2,3-c] [1,2,4]triazoles and related heterocycles under mild conditions was herein developed. The key step of this transformation is an oxidative cyclization employing PhI(OAc)2/sub
Efficient one-pot three-component synthesis of N-(4-arylthiazol-2-yl) hydrazones in water under ultrasound irradiation
Zhang, Dong-Nuan,Li, Ji-Tai,Song, Ya-Li,Liu, Hui-Min,Li, Hong-Ya
experimental part, p. 475 - 478 (2012/04/23)
A highly efficient and facile one-pot three-component synthesis of N-(4-arylthiazol-2-yl) hydrazones was carried out in excellent yield without any catalyst in water under ultrasound irradiation.
Eco-friendly one-pot synthesis of 2,4-disubstituted thiazoles by grinding under catalyst- and solvent-free conditions
Ding, Quansehng,Zhu, Dongjian,Jin, Huile,Chen, Jiuxi,Ding, Jinchang,Wu, Huayue
experimental part, p. 220 - 224 (2011/04/26)
Chemical Equation Presented An efficient and facile synthesis of 2,4-disubstituted thiazoles is achieved by a one-pot reaction of aldehydes and α-bromoketones with thiosemicarbazide by grinding under catalyst- and solvent-free conditions. This method has notable advantages in terms of simple workup, neat conditions, high yield, reasonably rapid reaction rate, and environmental friendliness. Supplemental materials are available for this article. Go to the publisher's online edition of Phosphorus, Sulfur, and Silicon and the Related Elements to view the free supplemental file. Copyright Taylor & Francis Group, LLC.
Synthesis, antibacterial activity and quantum-chemical studies of novel 2-arylidenehydrazinyl-4-arylthiazole analogues
Alam, Mohammad Sayed,Liu, Lijun,Lee, Yong-Eok,Lee, Dong-Ung
, p. 568 - 573 (2011/06/24)
A new series of 2-arylidenehydrazinyl-4-arylthiazole derivatives (2a-k) was designed and synthesized through a rapid, simple, and efficient methodology in excellent isolated yield. These compounds were screened for in vitro antimicrobial activities against eight bacteria, e.g. Bacillus cereus, Staphylococcus aureus, Bacillus subtilis, Bacillus megaterium, Pseudomonas aeruginosa, Shigella dysenteriae, Salmonella typhi, Escherichia coli, and three fungi e.g. Aspergillus oryzae, Candida albicans, and Saccharomyces cerevis. The results indicate that some of the compounds exhibit strong antibacterial activity, depending on the bacterial strain, but show virtually no antifungal activity. The structure-antibacterial activity relationships were studied using some physicochemical and quantum-chemical parameters with the ab initio Hartree-Fock model at the RHF/6-31G level of theory. A good qualitative correlation between predicted lipophilic parameters and antibacterial activity has been found.
Selective inhibitory activity against MAO and molecular modeling studies of 2-thiazolylhydrazone derivatives
Chimenti, Franco,Maccioni, Elias,Secci, Daniela,Bolasco, Adriana,Chimenti, Paola,Granese, Arianna,Befani, Olivia,Turini, Paola,Alcaro, Stefano,Ortuso, Francesco,Cardia, Maria C.,Distinto, Simona
, p. 707 - 712 (2007/10/03)
A series of 2-thiazolylhydrazone derivatives have been investigated for the ability to inhibit the activity of the A and B isoforms of monoamine oxidase (MAO) selectively. All of the compounds showed high activity against both the MAO-A and the MAO-B isoforms with pKi values ranging between 5.92 and 8.14 for the MAO-A and between 4.69 and 9.09 for the MAO-B isoforms. Both the MAO-A and the MAO-B isoforms, deposited in the Protein Data Bank as model 2BXR and 1GOS, respectively, were considered in a computational study performed with docking techniques on the most active and MAO-B-selective inhibitor, 18.
Synthesis of thiazolo[2,3-c]-s-triazoles using poly[(4-diacetoxyiodo) styrene]
Liu, Shi-Juan,Zhang, Ji-Zhen,Tian, Guan-Rong,Liu, Ping
, p. 1753 - 1758 (2007/10/03)
Arenecarbaldehyde-4-arylthiazol-2-ylhydrazones underwent ring closure with poly[(4-diacetoxyiodo)styrene] (PSDIB) to 3,5-diarylthiazolo[2,3-c]-s-triazoles in dichloromethane. Copyright Taylor & Francis, Inc.
An investigation of the biological effect of structural modifications of isothiosemicarbazones and their cyclic analogues
Maccioni,Cardia,Distinto,Bonsignore,De Logu
, p. 951 - 959 (2007/10/03)
Several arylideneisothiosemicarbazones and arylidenehydrazothiazoles have been synthesised to obtain new antimicrobial agents. Their activity against both bacteria and fungi has been tested and some interesting informations about their biological activity
Hypervalent iodine in the synthesis of bridgehead heterocycles: A new synthesis of 3,5-diarylthiazolo[2,3-c]-S-triazoles
Prakash,Saini,Kumar,Singh
, p. 3363 - 3371 (2007/10/03)
The synthesis of 3,5-diarylthiazolo[2,3-c]-s-triazoles (3a-f) has been accomplished by using a new method involving oxidation of arenecarbaldehyde-4-arylthiazol-2-ylhydrazones (2a-f) with iodobenzene diacetate (IBD) in dichloromethane by intramolecular cyclization in high yields.
Bromination of 4-Substituted Thiazolylhydrazones
Denisova, A. B.,Andronnikova, G. P.
, p. 863 - 867 (2007/10/03)
4-Phenyl- and 4-methylthiazolylhydrazones were brominated in chloroform and acetic acid.The use of 1.5 equivalents of bromine led to the exclusive formation of the 5-halo derivatives.Effects of substituents on the thiazole ring and of the hydrazone fragme
