Design, Synthesis And Evaluation Of Antibacterial Activity Of Novel((7-Nitro/Bromo-4-Oxo-4h-Chromen-3-Yl)Methyl)-N-Phenylsulfonyl-D-Alanine/Leucine/Glycine Derivatives

Abstract

Introduction: The main cause of death worldwide is the spread of various infectious diseases. Despite significant advances in infectious disease research and treatment, the control and eradication of these diseases faces major challenges. So, to treat these deadly infectious diseases, a large number of drugs like antibiotics, antiviral and antifungal agents are used but drug resistance is the major problem among them.

Aims and Objectives: To avoid these kinds of problems, more attention has been taken towards designing, synthesis and pharmacological evaluation of some novel antimicrobial molecules. There are a large number of methods for the treatment of infectious diseases. But inhibition of DNA gyrase and RNA synthetase is the very effective mechanism for the treatment of microbial infections. Chromones are very effective against microbial agents as these are proven very successful for the inhibition of DNA gyrase and RNA synthetase. The chromone moiety has a wide variety of pharmacological activities such as anticancer antiviral, antioxidant, antifungal, anti HIV, anti-inflammatory. Similarly, Sulfonamides, have bacteriostatic action by inhibiting the conversion of p-aminobenzoic acid to dihydropteroate, which bacteria need for folate synthesis and ultimately purine and DNA synthesis. This knowledge inspired towards the designing, synthesis and pharmacological evaluation of chromone based novel sulfonamide derivatives. The present work includes synthesis of substituted 3-Formylchromones, synthesis of chromone based novel sulfonamide derivatives and evaluation of antimicrobial activity of the synthesized derivatives.

Materials and Methods: Initially, synthesis of 3-Formylchromones was carried out under ice chilled conditions with continuous stirring by reacting substituted acetophenones with POCl₃ and DMF by Vilsmeier Hack reaction. The compounds 3-Formylchromones have been reacted with various substituted sulphonamide derivatives to yield novel chromone-based sulphonamides. The solid and recrystallized over alcohol, filtered and dried. The reaction completion was monitored by TLC (hexane-ethyl acetate, 9:1).

Antibacterial Activity: All the synthesized compounds were evaluated for their in vitro antibacterial activity.