Synthesis of some chloro-substituted isoxazoline derivatives as antibacterial agents

Abstract

Objectives: The chemistry of chalcones has generated intensive scientific studies throughout the world. Especially interest has been focused on the synthesis and biodynamic activities of isoxazoline derivatives. In recent year numerous isoxazoline derivatives have been synthesized for their anticancer, anti-inflammatory, cytotoxic, antiviral activities. The reaction of substituted chalcones with hydroxylamine hydrochloride in presence of acetic acid gave isoxazoline derivatives. : The five membered oxygen and Nitrogen containing compounds exhibited Material and methods antioxidant, analgesic, antibacterial, antifungal activities. Therefore the attempt have been made to synthesize chlorosubstituted isoxazolines by the reaction of different substituted chalcones with hydroxylamine hydrochloride in presence of few drops of acetic acid. All the synthesized compounds confirmed by TLC and spectral analysis and also screened for their antibacterial activity. : The novel chloro-substituted isoxazolines showed good to moderate Results antibacterial activity against Gram+ve and Gram-ve bacterial strains tested. : These compounds Conclusion containing chloro, bromo, iodo groups were found showed potent antibacterial, antifungal activities. These findings promoted us to to synthesize novel chloro-substituted isoxazolines derivatives which are found to be potential antibacterial agents.

Naphthyl‐Based Chalcone Derivatives: A Multifaceted Player in Medicinal Chemistry

“…These isoxazoline derivatives 91 a-f (Figure 15) were reported by Deshmukh et al and studied for antibacterial activities. [140] The synthesized isoxazoline derivatives, and demonstrated 91 a-d strong antibacterial activity against all the investigated species according to the screening experiments. The study found that electronrich 91 c, with one -OMe and two -Cl substituents, showed the best activity comparable to standard medication, supporting the hypothesis that isoxazolines with electrons have greater action.…”

“…These isoxazoline derivatives 91 a – f (Figure 15) were reported by Deshmukh et al . and studied for antibacterial activities [140] . The synthesized isoxazoline derivatives, and demonstrated 91 a – d strong antibacterial activity against all the investigated species according to the screening experiments.…”

2‐Isoxazolines: A Synthetic and Medicinal Overview

“…as they assayed the synthesized compounds against Gram‐positive and Gram‐negative strains. Among the synthesized analogues, compound 73 was found to be potent with MIC values of 26–28 μM relative to the standard drug ofloxacin [142] . A metal‐free method with assistance from potassium iodate (KIO 3 ) was generated by Kotian et al.…”

Design, Synthesis, and Insecticidal Activity of Mesoionic Pyrido[1,2-a]pyrimidinone Containing Isoxazole/Isoxazoline Moiety as a Potential Insecticide

“…Isoxazole/isoxazoline is a vital N- and O-containing heterocyclic molecule with a five-membered ring and is found throughout natural products . It has been employed extensively in drug discovery because of their potent antimicrobial, fungicidal, , and insecticidal properties. , Many products derived from these structures, such as fluralaner and afoxolaner, are commercially available. , In this study, isoxazole and isoxazoline were introduced into the 3-position benzene ring of pyrido­[1,2- a ]­pyrimidinone (Figure ) and a series of novel pyrido­[1,2- a ]­pyrimidinone compounds was synthesized. The insecticidal activity of the target compounds against A.…”

“…27 Isoxazole/isoxazoline is a vital N-and O-containing heterocyclic molecule with a five-membered ring and is found throughout natural products. 28 It has been employed extensively in drug discovery because of their potent antimicrobial, 29 fungicidal, 30,31 and insecticidal properties. 32,33 Many products derived from these structures, such as fluralaner and afoxolaner, are commercially available.…”