Tailored microwave technology for synthesis of N’-[(3Z)-5-chloro-1-(morpholin-4-ylmethyl)-2-oxo-1,2- dihydro-3H-indol-3-ylidene]pyridine-4-carbohydrazide as HIV-1 inhibitors

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Rahul Hajare, Smita Kulkarni and Ramesh Paranjape

Aarti Drugs Limited, India
National AIDS Research Institute, India

: J Pharm Drug Deliv Res

Abstract

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Reaction of that with 5-Chloro Isatin (1.85 g, 0.007 mol), with morpholin (0.6 g, 0.007 mol) in the presence of catalytic amount of formaldehyde (0.3 g, 0.01 mol) and solvent ethanol (20 ml) when reflux and stirred for 4 h lead to the N-morpholinomethylindole- 2, 3-dione. Engineered microwave technology for synthesis of N’-[(3Z)-5-chloro-1-(morpholin-4-ylmethyl)-2-oxo-1,2- dihydro-3H-indol-3-ylidene]pyridine-4 carbohydrazide as HIV-1 inhibitor begins with a mix reaction to remove protecting ketone group in N-morpholinomethyl-indole-2, 3-dione 0.002M by means of 4-pyridinecarbohydrazide 0.002 M treatment with glacial acetic acid (2 ml) and solvent charge with 40 ml of ethanol and reflux with stirring for 1 hour. For ventilation, engineered microwave ovens have a built-in blower for a recirculating venting system, designed for over-the-range installation, offered two more options for venting to the outdoors. The blower can be positioned to direct exhaust air up and out through the roof via duct and harmful impurity gets effluxed through horizontally ductwork. In vitro anti-HIV-1 activity of N’-[(3Z)-5-chloro-1-(morpholin-4-ylmethyl)- 2-oxo-1,2-dihydro-3H-indol 3-ylidene]pyridine-4-carbohydrazide and further studies have suggested that this is a novel molecule and has cytotoxicity of 120.07 ug/ml for cell lines, TZM-bl. It displayed potent anti-HIV-1 activity and was found to be 25.65 μg per ml against laboratory adapted strains of National AIDS Research Institute, Pune, India.

Biography

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Email: rahulhajare@rediffmail.com