Azetidin-2-one analogues are reported to exhibit various pharmacological activities like cholesterol absorption inhibitory activity, human tryptase, thrombin and chymase inhibitory activity, vasopressin V1a antagonist activity, antidiabetic, anti-inflammatory, antiparkinsonian and anti-HIV activity in addition to antimicrobial. 1-6 In the present study, Isoniazid (INH), the established antitubercular drug was selected as the lead for the design and development of antitubercular agents with minimal toxic effects. A novel series of amino azetidinones were designed from corresponding azetidin-2-ones using various in silico methods. Docking studies were performed at Mtb enoyl acp reductase (4DRE) and the derivatives exhibited best docking scores were prepared from corresponding azetidin-2-ones by treating with various molecules containing amino groups in the presence of TEA. Azetidin-2-ones in turn were obtained from a series of INH Schiff bases by reaction with chloro acetyl chloride. Structures of the newly synthesized compounds were assigned on the basis of elemental analysis, IR, 1 H NMR, 13 CNMR and mass spectral studies. The newly synthesized compounds were screened for their in vitro antitubercular activity using Alamar blue assay method and the hepatotoxicity was determined by MTT assay method using chang liver cells. AAZ1V, the amino azetidinone obtained from N-[3-chloro-2-(4-chlorophenyl)-4-oxoazetidin-1-yl] pyridine-4-carboxamide (AZ1V) by combining with 4-amino 1, 2, 4-triazole produced significant antitubercular activity. The percentage viability produced by AAZ1V against Chang liver cells for hepatotoxicity was better than the percentage viability produced by INH.

Refractive indices and ET values were measured for the ternary mixture methanol–acetonitrile–1‐propanol at 25.0 °C for 13 mole fractions, and also for the corresponding binary mixtures, methanol–1‐propanol, methanol–acetonitrile and 1‐propanol–acetonitrile, at 25.0 and 50.0 °C, at 10 different compositions. Solvent exchange equilibrium models were applied to the transition energy of the Dimroth–Reichardt ET(30) solvatochromic indicator in the binary systems and the Redlich–Kister polynomial was used to correlate excess ETN and nD values for the binary solvent mixtures data. The results allowed the analysis of synergetic behaviours, polarizability effects and preferential solvation trends both in the binary and in the ternary mixtures. Our results point towards the prevalence of specific solute–solvent–solvent interactions mainly due to hydrogen bonding by the hydroxylic components of the ternary mixture. Copyright © 2002 John Wiley & Sons, Ltd.

The rate of solvolysis of tert-butyl halides is increased by both nucleophilic and electrophilic solvents.

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