Green synthesis of novel quinoline based imidazole derivatives and evaluation of their antimicrobial activity

Desai, N. C.; Maheta, Abhay; Rajpara, K. M.; Joshi, V. V.; Vaghani, H. V.; Satodiya, H. M.

doi:10.1016/j.jscs.2011.11.021

Cited by 69 publications

(32 citation statements)

References 32 publications

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“…One way to overcome the rapid development of drug resistance to the currently used antimicrobials is to develop new agents, preferably with chemical characteristics that vastly differ from those of existing ones. (Desai et al, 2014) Phenylthiazoles were reported as a new scaffold acting as dual UppP and UppS inhibitors with wide antimicrobial activity against multidrug-resistant gram-positive strains including MRSA, VRSA and VRE(Haroon Mohammad et al, 2014a) with selective advantage over vancomycin.(H. Mohammad, Mayhoub, Cushman, & Seleem, 2015;Haroon Mohammad et al, 2014b) The SAR of this class of compounds is welldefined through more than 400 phenylthiazoles published derivatives.…”

Section: Introductionmentioning

confidence: 99%

Design and Synthesis of New Heterocyclic Compounds to Overcome Microbial Resistance

Helal

2019

Al-Azhar Journal of Pharmaceutical Sciences

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Though clinicians once possessed a robust arsenal of antibiotics, many of these valuable therapeutic agents have fallen prey to the expanded resistance of pathogenic bacteria. Phenylthiazoles were reported previously as a new scaffold that possesses antibacterial activity against an array of clinically-relevant strains of multidrug-resistant staphylococci. Close inspection of the structure-activity-relationships (SAR) of phenylthiazoles revealed important structural features necessary for their antibacterial activity: a nitrogenous head and a lipophilic tail. Incorporating the nitrogenous part within an oxadiazole ring resulted in analogues with a prolonged half-life, while the biphenyl tail revealed the most potent analogue. In the present work, advantageous moieties have been combined together to generate new hybrid scaffolds of phenylpyridine with the objective of promoting new moieties enhancing both antimicrobial resistance activity and drug-like properties. Among the tested oxadiazolylbiphenylpyridines, derivatives 14 and 23 were identified as the most potent analogues with MIC values as low as 8 g/mL on MRSA-US300 and other studied species.

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Section: Introductionmentioning

confidence: 99%

Design and Synthesis of New Heterocyclic Compounds to Overcome Microbial Resistance

Helal

2019

Al-Azhar Journal of Pharmaceutical Sciences

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“…But unfortunately, in the absence of an effective platform for antibiotic discovery and after years of misuse and overuse of antibiotics in humans and animals, bacteria are becoming antibiotic resistant. The fast resistance of bacteria against antibiotics has become a prevailing medical problem over the world (Desai et al 2014;AbdelAziz et al 2015). Treatment options for these infections are often insufficient particularly in immune compromised patients.…”

Section: Introductionmentioning

confidence: 99%

Synthesis, Characterization and Biological Evaluation of Some Imidazole Bearing Hydrazones as Possible Antimicrobial and Anthelmintic Agents

Sharma¹,

Kumar²,

S³

et al. 2016

BPR

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Hydrazones have been of considerable scientific interest due to their momentous biological activities.A number of imidazole bearing hydrazone derivatives were synthesized and characterized in the present investigation. Synthetic protocols were undertaken to react benzil with benzaldehyde and ammonium acetate in the presence of sulphanilic acid as catalyst to yield suitable imidazoles. Further, in the proceeding steps, reactions of imidazole were carried out to yield ester, then hydrazide and finally the hydrazone derivatives. Spectral methods were used to characterize the synthesized compounds appropriately. The synthesized hydrazones were screened for antibacterial, antifungal, anthelmintic activities. Most of the synthesized compounds showed moderate to good biological activities.

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“…Many drugs contain an imidazole ring such as antifungal drugs and nitroimidazole [1]. Nitrogen bridge head-fused heterocyclics which contain an imidazole ring are common structural motifs in pharmacologically important molecules, with activities spanning a diverse range of target [2]. The imidazole nucleus appears in a number of naturally occurring product like the amino acid histidine and purines which comprise many of the most important bases in nucleic acid [3].…”

Section: Introductionmentioning

confidence: 99%

Synthesis of New Some Imidazole Derivatives Containing ?-Lactam Ring

Journal¹

2016

Baghdad Sci.J

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In this work 5-methylene-yl - (2-methy –oxazole-4-one) (1H) imidazole (1) were synthesized from the reaction of L-Histidine with acetic anhydride and which converted to the of 5-methylene-yl-(2-methyl 3-amino imidazole-4-one)-1H-imidazole (2) by reaction with hydrazine hydrate. Schiff bases (3-6) were synthesized from the reaction of compound (2) with different aromatic aldehyde. Reaction of compounds (3-6) with chloroacetyl chloride gives azetidinone one derivatives (7-10). These compounds were characterized by FT-IR and some of them with 1H-NMR and 13C-NMR spectroscopy.

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Green synthesis of novel quinoline based imidazole derivatives and evaluation of their antimicrobial activity

Cited by 69 publications

References 32 publications

Design and Synthesis of New Heterocyclic Compounds to Overcome Microbial Resistance

Design and Synthesis of New Heterocyclic Compounds to Overcome Microbial Resistance

Synthesis, Characterization and Biological Evaluation of Some Imidazole Bearing Hydrazones as Possible Antimicrobial and Anthelmintic Agents

Synthesis of New Some Imidazole Derivatives Containing ?-Lactam Ring

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