No abstract

Srivastav, et al.: Synthesis and Antiretroviral Activity of 6-Acetyl-coumarin Derivatives A series of 6-acetyl-coumarin derivatives (2a-n) were synthesized and evaluated for antiretroviral activity in C8166 T-cell line infected with HxBru-Gluc strain of human immunodeficiency virus-1. Michael Addition followed by re-aromatization and subsequent acid-induced elimination of water leads to the formation of coumarin intermediate, which undergoes Claisen-Schmidt condensation with substituted bezaldehydes using silica sulphuric acid as a catalyst to form 6-acetyl-coumarin derivatives, 2a-n. In silico absorption, distribution, metabolism, excretion and toxicity parameters of compounds 2a-n were found within their reference limits. All synthesized compounds were devoid of cytotoxicity as they have shown cell viability count more than 80 % in cytotoxicity assay. Compounds 2a, 2g and 2h showed potent inhibitory activity against human immunodeficiency virus infection with IC 50 value of 4.7, 4.5 and 0.35 µM, respectively. It was found that electron-withdrawing group at phenyl ring, attached to the coumarin nucleus was crucial for activity against human immunodeficiency virus. The present study may be helpful in the development of some potent antiretroviral agents.

No abstract

Quantitative spectrophotometric analysis of poorly water-soluble drugs involves use of various organic solvents. Major drawbacks of organic solvents include high cost, volatility and toxicity. Safety of analyzer is affected by toxicity of the solvent used. In the present investigation the use of organic solvent has been avoided, making the method environmentally friendly. Urea has demonstrated enhancement in aqueous solubilities of a large number of poorly water-soluble drugs, thereby widely used as a hydrotropic agent. There was more than 10-fold enhancement in the solubility of ornidazole in 10 M urea solution as compared to its solubility in distilled water. In the present investigation, hydrotropic solution of urea (10 M) was employed as solubilizing agent to solubilize the poorly water-soluble drug, ornidazole, from fine powder of its tablet dosage form for spectrophotometric determination in ultraviolet region at 319 nm. Beer's law was obeyed in the concentration range of 5-25 μg/ml in presence of urea. Presence of urea did not interfere in the analysis. Proposed method is new, rapid, simple, accurate, and reproducible. Statistical data proved the accuracy, reproducibility and the precision of the proposed method.

No abstract