CHROMATOGRAPHICALLY DERIVED HYDROPHOBICITY PARAMETERS IN QSAR ANALYSIS OF DIARYLSULPHONE ANALOGS

Citation
Rd. Puri et al., CHROMATOGRAPHICALLY DERIVED HYDROPHOBICITY PARAMETERS IN QSAR ANALYSIS OF DIARYLSULPHONE ANALOGS, Indian journal of chemistry. Sect. B: organic chemistry, including medical chemistry, 35(12), 1996, pp. 1271-1274
Citations number
12
Categorie Soggetti
Chemistry Inorganic & Nuclear
ISSN journal
03764699
Volume
35
Issue
12
Year of publication
1996
Pages
1271 - 1274
Database
ISI
SICI code
0376-4699(1996)35:12<1271:CDHPIQ>2.0.ZU;2-3
Abstract
4-Amino-4'-substituted-diphenylsulphones have been synthesised and tes ted for antileprotic activity. The values of the parameters R(m) and l og k' have been estimated using reverse phase thin layer chromatograph y (RPTLC) and reverse phase high performance liquid chromatography (RP HPLC) respectively and correlated individually with calculated pi and molecular connectivity (chi) values in a typical Hansch analysis. Resu lts indicate that log k' is a better descriptor of lipophilicity than R(m) in the present homologous series of compounds. Molecular connecti vity index appears to be a poor descriptor of the lipophilic character istic of these compounds. Quantitative relationships between the vario us physicochemical parameters and biological activity have been analys ed using linear regression analysis. It has been found that electronic effect of a substituent is more contributive for inhibitory potency t han lipophilicity.