94205-70-6Relevant academic research and scientific papers
Design, synthesis and biological evaluation of 5-benzylidene-2-iminothiazolidin-4-ones as selective GSK-3β inhibitors
Arfeen, Minhajul,Bhagat, Shweta,Patel, Rahul,Prasad, Shivcharan,Roy, Ipsita,Chakraborti, Asit K.,Bharatam, Prasad V.
supporting information, p. 727 - 736 (2016/07/19)
In this work, iminothiazolidin-4-one derivatives were explored as selective GSK-3β inhibitors. Molecular docking analysis was carried to design a series of compounds, which were synthesized using substituted thiourea, 2-bromoacetophenones and benzaldehydes. Out of the twenty five compounds synthesized during this work, the in?vitro evaluation against GSK-3 led to the identification of nine compounds with activity in lower nano-molar range (2–85?nM). Further, in?vitro evaluation against CDK-2 showed five compounds to be selective towards GSK-3.
Design, Synthesis and Pharmacological Screening of Novel Antihypertensive Agents Using Hybrid Approach
Bhandari, Shashikant V.,Bothara, Kailash G.,Patil, Ajit A.,Chitre, Trupti S.,Sarkate, Aniket P.,Gore, Suraj T.,Dangre, Sudarshan C.,Khachane, Chetan V.
experimental part, p. 390 - 400 (2011/02/25)
Eight derivatives of general formula 2-(2-(4-(3-((5-substituted methylene)-4-oxo-2-(phenylimino)thiazolidin-3-yl)-2-hydroxypropylamino)b enzoyl)hydrazinyl)-2-oxoethyl nitrate were synthesized and tested for electrocardiographic, antiarrhythmic, vasorelaxing and antihypertensive activity as well as for in-vitro nitric oxide (NO) releasing ability. Compound 8b 2-(2-(4-(3-(5-benzyliden-4-oxo-2-(phenylimino)thiazolidin-3-yl)-2-hydrox ypropylamino)benzoyl)hydrazinyl)-2-oxoethyl nitrate, was the most potent in this series. The pharmacological results suggested that the antiarrhythmic effects of these compounds were related to their adrenolytic properties which are believed to be due to the presence of the 5-(substituted)methylen-2-(phenylimino)thiazolidin-4-one moiety with less bulky, electron donating substituent on the phenyl ring at 5th position of the thiazolidin-4-one. In conclusion, most of the synthesized compounds were significantly potent as antiarrhythmic and antihypertensive; this might be due to the presence of different pharmacopores which might act at different locations with different mode of action. Further insights of the same can be obtained by doing investigation at receptor level. The potency of compounds 8a-8h were promising enough to continue further experiments.
Synthesis and biological evaluation of 7-N-(n-alkoxyphthalimido)-2hydroxy- 4-aryl-6-aryliminothiazolidino [2,3-b] pyrimidines and related compounds
Singh, Bhawani Singh,Mehta, Deepika,Baregama, Lalit K.,Talesara
, p. 1306 - 1313 (2007/10/03)
Substituted aryl thioureas 1a-c react with chloroacetic acid in the presence of anhydrous sodium acetate to furnish 2-aryliminothiazolidin-4-ones 2a-c. Condensation of ω-bromoalkoxyphthalimides 3a-c with 2a-c give the corresponding alkoxyphthalimide derivatives of 2-aryliminothiazolidin-4-ones 4a-i. These on condensation with araldehydes 5a-c yield 3-N-(alkoxyphthalimido)- 5-arylidene-2-aryliminothiazolidin-4-ones 7a-a′. In an alternative route 5a-c react with 2a-c to give 6a-i, which could be cyclised with urea in the presence of sodium acetate to yield the corresponding thiazolidinopyrimidine 8a-i. 7a-a′ are also prepared from 6a-i with 3a-c, which give final compound 9a-a′ on cyclisation. Alternatively, 8a-i when condensed with 3a-c also furnish the compounds 9a-a′. Evaluation of antimalarial and antibacterial activity is also reported.
