38771-64-1Relevant academic research and scientific papers
Synthesis and pharmacological screening of some novel anti-hypertensive agents possessing 5-Benzylidene-2-(phenylimino)-thiazolidin-4-one ring
Bhalgat, Chetan M.,Darda, Pooja V.,Bothara, Kailash G.,Bhandari, Shashikant V.,Gandhi, Jotsna,Ramesh
, p. 580 - 588 (2014/04/03)
In the present study, fourteen derivatives comprising of 5-benzylidene-2-(phenylimino)-thiazolidin-4-one moiety were synthesized. The structures of synthesized compounds were established by elemental analysis, IR, 1H NMR, 13C NMR and mass spectral data and tested for electrocardiographic, antiarrhythmic and antihypertensive activities. Compound 11 was found to be most potent in this series. The pharmacological results suggested that, the antiarrhythmic effects of these compounds were related to their Ca++ ion channel antagonistic properties, which are believed to be due to the presence of 5-benzilidine-2-(phenylimino)-thiazolidin-4-one moiety. The antihypertensive effect of β-blocker side chain is enhanced by the presence of less bulky aliphatic and heterocyclic tertiary amines.
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.
NEW COMBINATION FOR USE IN THE TREATMENT OF CANCER
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Page/Page column 49, (2008/12/06)
There is provided combination products comprising (a) a compound of formula (I): wherein X, Y, T, W, A1, A2 R1, R5 and R6 have meanings given in the description, and (b) tamoxifen or an aromatase inhi
Traceless solid-phase synthesis of 2-amino-5-alkylidene-thiazol-4-ones
Pulici, Maurizio,Quartieri, Francesca
, p. 2387 - 2391 (2007/10/03)
2-Amino-5-alkylidene-thiazol-4-ones bearing two diversity points are prepared by a solid-phase strategy exploiting rhodanine as the starting material. Rhodanine is first loaded on bromo-Wang resin, subjected to Knovenagel condensation with aldehydes, and cleaved off the resin in a traceless manner by means of an amine.
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.
A NEW APPROACH TO 5-ARYLIDENETHIAZOLIDIN-4-ONES
Rudorf, Wolf-Dieter,Schwarz, Ralf
, p. 3459 - 3465 (2007/10/02)
Reaction of 3-phenylpropynamides with heterocumulenes in the presence of a base yields 5-arylidenethiazolidin-4-ones by intramolecular nucleophilic addition to the α-carbon of the CC triple bond.
SYNTHESIS OF 2-SUBSTITUTED 5-ARYLIDENETHIAZOLIN-4-ONES FROM α,β-UNSATURATED ACYL ISOTHIOCYANATES
Kutschy, Peter,Dzurilla, Milan,Kristian, Pavol,Kutschyova, Kvetoslava
, p. 436 - 445 (2007/10/02)
α,β-Unsaturated acyl isothiocyanates react with N-methylaniline to give thioureas which, when treated with bromine in chloroform, afford benzothiazoline derivatives.Under the same reaction conditions primary amines, diethylamine,piperidine and morpholine
