Furo(3,2-b)indole derivatives. II. Synthesis and analgesic and anti-inflammatory activities of 4-alkoxycarbonyl-2-morpholinocarbonylfuro(3,2-b)indole derivatives.

hp, the Component of Log P Controlling Structure-activity Relationships Amongst Non-steroidal Anti-inflammatory Drugs

“…The partition coefficient P and its allies continue to provide a major means of studying drug activities (Leahy et al 1992). Typical applications to the non-steroidal anti-inflammatory drugs (NSAIDs) have been made by Gund & Jensen (1983), Nakashima et al (1985), Kuchar et al (1989) and Dearden et a1 (1989) amongst others. In order to achieve useful quantitative structure-activity relationships (QSAR) log P is commonly supplemented by other physical and chemical quantities including pK,, (log P)2, Hammett sigma values, refractivities, and steric parameters, while yet further constants and coefficients emerge from the application of regression analysis as in studies undertaken by Habicht & Brune (1 983) on salicylic acids, Dewhirst (1 980) on phenols, Kuchar et al (1989) Thus in individual series a high degree of correlation can be achieved by a suitable selection of parameters, corrections, and coefficients, but as each series requires its own selection of modifications, no general correlation has yet been recognized and attempts to establish correlations independent of structural type have been uncommon.…”