Quantitative structure-activity analysis in dihydropteroate synthase inhibition of sulfones. Comparison with sulfanilamides

PG De Benedetti, D Iarossi, C Menziani…

Index: Benedetti, Pier G. De; Iarossi, Dario; Menziani, Cristina; Caiolfa, Valeria; Frassineti, Chiara; Cennamo, Carlo Journal of Medicinal Chemistry, 1987 , vol. 30, # 3 p. 459 - 464

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Citation Number: 32

Abstract

A set of 25 4'-, eight 2', 4'-, and five 2', 4', 6'-substituted 4-aminodiphenyl sulfones were tested for their inhibitory activity on dihydropteroate synthase of Escherichia coli. Linear regression analysis shows that enzymic inhibition indices correlate well with both quantum chemical and spectroscopic descriptors of the electronic structure of the common moiety 4- NH2-C6H4-SO2 of the sulfones (the above descriptors being expressed in relation to the ...