<p>Study of biophysical properties, synthesis and biological evaluations of newer thiazolidine-2,4-dione conjugates</p>
Online Publishing @ NISCAIR
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Authentication Code |
dc |
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Title Statement |
<p>Study of biophysical properties, synthesis and biological evaluations of newer thiazolidine-2,4-dione conjugates</p> |
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Added Entry - Uncontrolled Name |
Patel, Jaydeep A; Department of Chemistry, Vidhyadeep Institute of Science, Anita, Kim-Olpad Road, Surat-394 110, Gujarat, India
Department of Chemistry, Veer Narmad South Gujarat University, Udhana-Magdalla Road, Surat-395 007, Gujarat, India Patel, Navin B; Department of Chemistry, Veer Narmad South Gujarat University, Udhana-Magdalla Road, Surat-395 007, Gujarat, India Patel, Parth P; Department of Chemistry, Veer Narmad South Gujarat University, Udhana-Magdalla Road, Surat-395 007, Gujarat, India |
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Uncontrolled Index Term |
2D-QSAR, PLSR method, T_2_2_O, ADME Properties, Antimicrobial activity, Antitubercular activity |
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Summary, etc. |
<p style="text-align: justify;">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 r<sup>2 </sup>= 0.3333, q<sup>2</sup>= 0.4000, pred_r<sup>2</sup> = -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 (<em>Z</em>)-2-(5-substituted-2,4-dioxothiazolidin-3-yl)-<em>N</em>-(4-methoxy-6-methyl-1,3,5-triazin-2-yl)acetamide <strong>(C<sub>1</sub>-C<sub>10</sub>) </strong>are synthesized and spectrally characterized using IR, <sup>1</sup>H NMR, <sup>13</sup>C NMR and mass spectral data analysis as well as biologically evaluated against antitubercular and antimicrobial activities. From the biologically evaluated derivatives, compounds C<sub>1</sub> and C<sub>4</sub> were found to be active against the different antimicrobial species. Compounds C<sub>7 </sub>and C<sub>10</sub> are more progressive than others against antitubercular species.</p> |
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Publication, Distribution, Etc. |
Indian Journal of Chemistry (IJC) 2022-10-21 16:51:33 |
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Electronic Location and Access |
application/pdf application/pdf http://op.niscair.res.in/index.php/IJC/article/view/67207 |
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Data Source Entry |
Indian Journal of Chemistry (IJC); ##issue.vol## 61, ##issue.no## 10 (2022): Indian Journal of Chemistry-(IJC) |
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Language Note |
en |
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