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
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.