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Study of biophysical properties, synthesis and biological evaluations of new thiazolidine-2,4-dione conjugates

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Title Study of biophysical properties, synthesis and biological evaluations of new thiazolidine-2,4-dione conjugates
 
Creator Patel, Jaydeep A
Patel, Navin B
Patel, Parth P
 
Subject 2D-QSAR
PLSR method
T_2_2_O
ADME Properties
Antimicrobial activity
Antitubercular activity
 
Description 1072-1081
Thiazolidine-2,4-dione and its derivatives are acting as antimicrobial and antitubercular agents. Computational approach
2D-QSAR is used for prediction of antitubercular activity of the synthetic derivatives. 2D-QSAR generated model using
PLSR method which predicted the statistically significant r2 = 0.3333, q2= 0.4000, pred_r2 = -1.9753 and F test = 3.0000.
2D-QSAR generated equation of pMICs is denoted the antitubercular activity correlated with thermodynamic descriptor
T_2_2_O. Pharmacokinetic properties absorption, distribution, metabolism, excretion are also predicted which are useful for
design the derivatives. A designed derivatives of (Z)-2-(5-substituted-2,4-dioxothiazolidin-3-yl)-N-(4-methoxy-6-methyl-
1,3,5-triazin-2-yl)acetamide (C1-C10) are synthesized and spectrally characterized using IR, 1H NMR, 13C NMR and mass
spectral data analysis as well as biologically evaluated against antitubercular and antimicrobial activities. From the
biologically evaluated derivatives, compounds C1 and C4 were found to be active against the different antimicrobial species.
Compounds C7 and C10 are more progressive than others against antitubercular species.
 
Date 2022-10-21T05:00:05Z
2022-10-21T05:00:05Z
2022-10
 
Type Article
 
Identifier 2583-1321 (Online); 0019-5103 (Print)
http://nopr.niscpr.res.in/handle/123456789/60722
https://doi.org/10.56042/ijc.v61i10.67207
 
Language en
 
Publisher NIScPR-CSIR,India
 
Source IJC Vol.61(10) [Oct 2022]