QSAR Analysis of 5-Substituted-2-Benzoyl-aminobenzoic acids as PPAR Modulator

A quantitative structure activity relationship (QSAR) study on a series of analogs of 5-aryl thiazolidine-2, 4-diones with activity on PPAR-α and PPAR-γ was made using combination of various thermodynamic, electronic and spatial descriptors. Several statistical regression expressions were obtained u...

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Main Authors: R. Hemalatha, L. K. Soni, A. K. Gupta, S. G. Kaskhedikar
Format: Article
Language:English
Published: Wiley 2004-01-01
Series:E-Journal of Chemistry
Online Access:http://dx.doi.org/10.1155/2004/306873
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author R. Hemalatha
L. K. Soni
A. K. Gupta
S. G. Kaskhedikar
author_facet R. Hemalatha
L. K. Soni
A. K. Gupta
S. G. Kaskhedikar
author_sort R. Hemalatha
collection DOAJ
description A quantitative structure activity relationship (QSAR) study on a series of analogs of 5-aryl thiazolidine-2, 4-diones with activity on PPAR-α and PPAR-γ was made using combination of various thermodynamic, electronic and spatial descriptors. Several statistical regression expressions were obtained using multiple linear regression analysis. The best QSAR model was further validated by leave one out cross validation method. The studied revealed that for dual PPAR-α/γ activity dipole-dipole energy and PMI-Z play significant role and contributed positively for PPAR-γ and PPAR-α activity respectively. Thus, QSAR brings important structural insight to aid the design of dual PPAR-α /γ receptor agonist.
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spelling doaj-art-efe1fb4ef94e45208df776638416cb642025-08-20T03:21:22ZengWileyE-Journal of Chemistry0973-49452090-98102004-01-011524325010.1155/2004/306873QSAR Analysis of 5-Substituted-2-Benzoyl-aminobenzoic acids as PPAR ModulatorR. Hemalatha0L. K. Soni1A. K. Gupta2S. G. Kaskhedikar3Molecular Modelling Study Group, CADD Laboratory, Dept. of Pharmacy, S.G.S.I.T.S., Indore-452003, IndiaMolecular Modelling Study Group, CADD Laboratory, Dept. of Pharmacy, S.G.S.I.T.S., Indore-452003, IndiaMolecular Modelling Study Group, CADD Laboratory, Dept. of Pharmacy, S.G.S.I.T.S., Indore-452003, IndiaMolecular Modelling Study Group, CADD Laboratory, Dept. of Pharmacy, S.G.S.I.T.S., Indore-452003, IndiaA quantitative structure activity relationship (QSAR) study on a series of analogs of 5-aryl thiazolidine-2, 4-diones with activity on PPAR-α and PPAR-γ was made using combination of various thermodynamic, electronic and spatial descriptors. Several statistical regression expressions were obtained using multiple linear regression analysis. The best QSAR model was further validated by leave one out cross validation method. The studied revealed that for dual PPAR-α/γ activity dipole-dipole energy and PMI-Z play significant role and contributed positively for PPAR-γ and PPAR-α activity respectively. Thus, QSAR brings important structural insight to aid the design of dual PPAR-α /γ receptor agonist.http://dx.doi.org/10.1155/2004/306873
spellingShingle R. Hemalatha
L. K. Soni
A. K. Gupta
S. G. Kaskhedikar
QSAR Analysis of 5-Substituted-2-Benzoyl-aminobenzoic acids as PPAR Modulator
E-Journal of Chemistry
title QSAR Analysis of 5-Substituted-2-Benzoyl-aminobenzoic acids as PPAR Modulator
title_full QSAR Analysis of 5-Substituted-2-Benzoyl-aminobenzoic acids as PPAR Modulator
title_fullStr QSAR Analysis of 5-Substituted-2-Benzoyl-aminobenzoic acids as PPAR Modulator
title_full_unstemmed QSAR Analysis of 5-Substituted-2-Benzoyl-aminobenzoic acids as PPAR Modulator
title_short QSAR Analysis of 5-Substituted-2-Benzoyl-aminobenzoic acids as PPAR Modulator
title_sort qsar analysis of 5 substituted 2 benzoyl aminobenzoic acids as ppar modulator
url http://dx.doi.org/10.1155/2004/306873
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