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Gastrosparing novel prodrugs (MAM and MAT) synthesized consisted of mefenamic acid (MA) with menthol (M) and thymol (T). Structural characterizations of synthesized esters were done by Infra red spectroscopy (IR), proton nuclear magnetic resonance (1HNMR), mass spectroscopy. After evaluation of pharmacological i.e. anti-inflammatory, analgesic and ulcerogenic activities, the preformulation studies were undertaken. Based on these a few formulation (suspensions) were designed and prepared. The formulated suspensions were evaluated for content uniformity, sedimentation volume, recovery studies, redispersibility, viscosity, pH, particle size, zeta potential, effect of temperature and in-vitro dissolution rate. All the above parameters were found to be within the limit these indicated that the synthesized esters are good candidate for liquid dosage form. Thus it can be concluded synthesized prodrugs can be formulated in suspension form. [ABSTRACT FROM AUTHOR]

In this manuscript we have designed and synthesized 1,4-Naphthoquinone analogs substituted with 1,3,4 Oxadiazolenucleus. The synthesized compound (M1-M14) were characterized using the different analytical technique¹H NMR, 13C NMR, FTIR, Mass spectroscopy, melting point, elemental analysis and further subjected for the evaluation of their anticancer activity using MCF-7, Hela and HepG2 cancer cell lines. The compound M-5 was found to exhibit most potent cytotoxicity against cancer cell lines i.e. HeLa (IC50 =10.76 ± 0.11 µM), MCF-7 (IC50 = 9.30 ± 0.14 µM) and HepG2 (IC50 = 11.93 ± 0.38µM). Compound M-5 has also shown potent tyrosine kinase inhibitory activity with IC50 = 1.53 ± 0.05 µM. Moreover, molecular docking has exposed that compound M-5 has strong binding affinity to the active site of tyrosine kinase. These results give promising beginning stages to assist in the improvement of novel and powerful anticancer agents. [ABSTRACT FROM AUTHOR]

A novel mutual prodrug (MA-P) consisting of mefenamic acid (MA) and paracetamol (P) has been synthesized as a gastrosparing NSAID, devoid of ulcerogenic side effects. The structure of synthesized drug was confirmed by elemental analysis, infrared spectroscopy, 1H NMR spectroscopy and mass spectrometry.The kinetics of ester hydrolysis was studied by HPLC at pH 2, pH 7.4 as well as in human plasma. The pharmacological activities (anti-inflammatory, analgesic and ulcerogenic) were evaluated for the synthesized drug. The ulcerogenic reduction in terms of gastric wall mucosa, hexosamine and total proteins were also measured in glandular stomach of rats. The results indicated that MA-P ester has better ulcer index than the parent drug.