We report a library consisting of some novel Hantzsch dihydropyridines and Biginelli dihydropyrimidines of biological interest as well as their synthesis and analysis. The important steps in the synthetic part were found to be Hantzsch and Biginelli multicomponent reactions. The synthesized compounds were screened for their in vitro antibacterial activity against two gram-positive bacteria: Staphylococcus aureus and Bacillus subtilis. The title compounds did not exhibit potential antibacterial activity. Furthermore, compounds were subjected to in vitro cytotoxicity against Vero cells. Compounds exhibited weak, moderate, or high cytotoxicity. Compounds 4a, 4b, 4c, 4f, 4g, 4h, 4i, 7i, 7l, 7m, and 7r exhibited potential cytotoxicity. CoMFA study has resulted in the identification of structural features contributing toward their cytotoxicity.
Introduction: Pellionia heyneana Wedd. Leaves have long been employed as a traditional remedy by the Cholanaikan tribe of South India to treat various ailments. Methods: Pharmacological and physicochemical evaluation of P. heyneana leaf has been carried out to determine its macro and microscopic characters, and also some of its quantitative characters as per standard procedures. Results: The pharmacognostical evaluation of P. heyneana leavesrevealed the presence of characteristic microscopic features of the crude drug like cystoliths in upper epidermis, helicocytic stomata in lower epidermis, large number of peculiar shaped, huge (200-400 µm) foliar sclereids, absence of palisade tissue in the lamina etc. Powder microscopy showed the presence of calcium oxalate crystals, stone cells, multicellular trichomes, resinous blocks, spiral vessels, xylem fibre, starch grains, simple fibre etc. Conclusions: All the parameters evaluated in the study will aid to identify the authenticity of P. heyneana leaf even from the crushed or powdered form.
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