21938-35-2Relevant academic research and scientific papers
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)
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.
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.
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
experimental part, 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.
Design, synthesis and biological evaluation of novel thiazole derivatives as potent FabH inhibitors
Lv, Peng-Cheng,Wang, Kai-Rui,Yang, Ying,Mao, Wen-Jun,Chen, Jin,Xiong, Jing,Zhu, Hai-Liang
scheme or table, p. 6750 - 6754 (2010/06/12)
Fatty acid biosynthesis is essential for bacterial survival. Components of this biosynthetic pathway have been identified as attractive targets for the development of new antibacterial agents. FabH, β-ketoacyl-acyl carrier protein (ACP) synthase III, is a
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
