Novel, non-steroidal anti-inflammatory drug (NSAID), acetaminophen conjugates 6a–l with amino acid linkers were synthesized utilizing benzotriazole chemistry. Biological data acquired for all the novel bis-conjugates showed (a) some bis-conjugates (6d, 6e, 6h, and 6k) exhibit more potent anti-inflammatory activity than their parent drugs, (b) the potent bis-conjugates show no visible stomach lesions in contrast to parent drugs which are highly ulcerogenic, and (c) that the potent bio-active compounds have no mortality rates or toxic symptoms at 5 fold the applied anti-inflammatory dosage. A statistically significant QSAR model describing the anti-inflammatory properties of 6a–l (N = 15, n = 3, R(2) = 0.891, R(2)cvOO = 0.770, R(2)cvMO = 0.796, F = 29.904, s(2) = 0.011) was obtained employing CODESSA-Pro that validated the observed bio-activity.
The phase diagrams of pseudoternary mixtures of Tween80ÀbutanolÀkeroseneÀwater system were constructed by visual titration. The major three domains, i.e., oil in water, bicontinuous, and water in oil microemulsions were demarcated through conductivity measurement. A sharp increase in specific conductance in increasing water content in the bicontinuous domain has been ascribed to the percolation of ions through water continuum. Temperature induced clouding behavior of the mixtures in the Winsor IV domains was investigated to find out the effect of composition on the clouding temperature. A generalized regression model was proposed considering the cloud point to be a function of surfactant/cosurfactant ratio and oil and emulsifier contents. The increase in all these parameters increases the cloud points of the mixture. In the turbid Winsor III domain, temperature has an emulsifying effect. With increase in temperature, the turbid phase separates to three different phases, which experience transparent, translucent, and turbid characteristics due to mass transfer from one phase to another. The mass transfer phenomenon was well visualized by using nickel as water-soluble and N-alkyl 4-(p-N,N-dimethylaminostyryl)pyridinium dyes as oil-soluble probes.
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