Eaton’s reagent catalysed alacritous synthesis of 3-benzazepinones

An expeditious method for the synthesis of 3-benzazepinones has been developed by using a mixture of phosphorus pentoxide-methane sulfonic acid (Eaton’s reagent) at room temperature under solvent and metal catalyst free condition. Wide functional group tolerance, mild reaction conditions, simple procedure, ease of work-up and high yields is the citable features of this protocol

Synthesis and evaluation of antimitotic activity of new tetralone acid analogues of podophyllotoxin

The new tetralone acids (7a-e) were synthesized as analogues of podophyllotoxin. They were prepared by replacing 3,4,5-trimethoxyphenyl ring with cyclohexyl group in podophyllotoxin and 1,3-methylene dioxy ring with methoxy, hydrogen, methyl, thiomethyl, and fluorine atoms. The analogues of podophyllotoxin were synthesized using Gensler’s method with some changes in reagents and experimental procedure. The structures of the synthesized compounds were confirmed by IR, 1H NMR, 13C NMR, mass spectra and elemental analysis data. The synthesized tetralones acids were screened for their antimitotic activity. It is noteworthy that compound 7b possessed excellent antimitotic activity, 7c and 7e showed considerable activity and remaining 7a and 7d possessed low activity

Facile synthesis of 1,4-benzodiazepine-2,5-diones and quinazolinones from amino acids as anti-tubercular agents

A family of 1,4-benzodiazepine-2,5-diones and quinazolinones with diverse substituents at the C-3 position were synthesized via a novel, simple and convenient methodology using H2PtCl6 as the catalyst. The substitution at the C-3 position was varied using pre-defined amino acids as precursors. The synthesized benzodiazepines were screened for anti-mycobacterial tuberculosis (anti-TB) activity. The results revealed that the 1,4-benzodiazepine-2,5-diones displayed promising activity in comparison with their open chain precursors, which indicates that the diazepine frame is vital for their activity. The compounds 4h and 4f were found to be the lead nominees in the series with MIC values of 1.55 and 2.87 μg mL−1, respectively. A docking study was carried out on the enoyl acyl carrier protein to provide a better understanding of the mechanism of action of these compounds. Based on this study, the 1,4-benzodiazepine-2,5-dione framework is a good starting point for the development of new lead drug candidates in the treatment of multi-drug resistant tuberculosis