Synthesis and antibacterial activity of some new thiazole and thiophene derivatives

Khalil, A. M.; Berghot, M. A.; Gouda, Moustafa A.

doi:10.1016/j.ejmech.2009.06.002

Cited by 84 publications

(43 citation statements)

References 11 publications

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“…They can be used to kill anopheles mosquitoes (Venugopla et al, 2013) and their inhibitory effects on Trypanosoma brucei and Candida spp. have been proved (Chementi et al, 2011;Zelisko et al, 2013 (Khalil et al, 2009;Bondock et al, 2010).…”

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confidence: 79%

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Antimicrobial activities of thiazole, imidazolidine, tetrahydropyrimidine derivatives and silver/polyvinyl alcohol nanocomposites against selected zoonotic fish bacterial pathogens

Ghasemi¹,

Beyzaei²,

Hashemi³

et al. 2017

Indian J. Fish.

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One of the serious problems faced by health and food security is the spread of drug-resistant zoonotic aquatic bacterial pathogens. For this reason, identification and application of new antibacterial agents are required. In this study, inhibitory effects of thiazole, imidazolidine and tetrahydropyrimidine derivatives and silver/polyvinyl alcohol (Ag/PVA) nanocomposites were evaluated against three important zoonotic fish bacterial pathogens namely Streptococcus iniae, Edwardsiella tarda and Aeromonas hydrophila. Ag/PVA nanocomposite was found to inhibit growth of all tested bacteria, the highest activity was observed against S. iniae with minimum inhibitory concentration (MIC) of 256 μg ml-1 and inhibition zone diameter (IZD) of 10.2 mm. No inhibitory effects were observed with imidazolidines10a-c, tetrahydropyrimidines 10d-e and thiazoles 6a-c. Among heterocyclic compounds, only thiazole derivatives 6d and 8 had inhibitory effects onS. iniae and E. tarda with MIC values of 32-256 μg ml-1 but lacked antibacterial activity against A. hydrophila.

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confidence: 79%

“…The lucidity and turbidity in each well indicated lack or existence of bacterial growth, respectively. The lowest concentration that didn't show any turbidity, was reported as MIC (Khalil et al, 2009). …”

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confidence: 99%

Antimicrobial activities of thiazole, imidazolidine, tetrahydropyrimidine derivatives and silver/polyvinyl alcohol nanocomposites against selected zoonotic fish bacterial pathogens

Ghasemi¹,

Beyzaei²,

Hashemi³

et al. 2017

Indian J. Fish.

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“…[39][40][41][42][43][44][45] Ninhydrin is extensively used to detect compounds of pharmaceutical importance [46][47][48][49][50][51][52][53][54][55][56][57] and in kinetic studies. [58][59] Scheme 1.…”

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confidence: 99%

Ninhydrin in synthesis of heterocyclic compounds

Ziarani¹,

Lashgari²,

Azimian³

et al. 2015

Arkivoc

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Ninhydrin has been utilized in many heterocyclic preparations and considered as an important building block in organic synthesis. There is a wide range of reactions that include ninhydrin in the synthesis of heterocyclic compounds. This review highlights the advances in the use of ninhydrin as starting material in the synthesis of various organic compounds and drugs in a fully comprehensive way, from its first isolation in 1910 to the end of 2013. There is also a diversity of multi-component reactions of ninhydrin and we highlight the recent reports in this review.

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“…14,[16][17][18][19][20] Recently, several studies pointed out the importance of thiophene based derivatives as antibacterial agents. [21][22][23] Besides, Epimerox is a thiophene containing compound that prevented the growth of several Gram-positive pathogens. 24) Moreover, literature survey for functional groups which could be considered as pharmacophores for the antibacterial and antitubercular activities, revealed that the hydrazone moiety is common among many of the antibacterial drugs such as Nifuroxazide 1 25) (Fig.…”

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confidence: 99%

Synthesis, <i>in Vitro</i> and <i>in Silico</i> Studies of Some Novel 5-Nitrofuran-2-yl Hydrazones as Antimicrobial and Antitubercular Agents

Abdel‐Aziz

Eldehna

Farès

et al. 2015

Biological & Pharmaceutical Bulletin

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In this study, we synthesized two series of novel 5-nitrofuran-2-carbohydrazides 21a-h and 22a-e in addition to a third series of thiophene-2-carbohydrazides 23a-g to develop potent antimicrobial and/or antitubercular agents. The newly synthesized compounds were evaluated in vitro for their antimicrobial and antimycobacterial activities. Most of the 5-nitrofuran-2-carbohydrazides 21a-h and 22a-e displayed variable activity against Aspergillus fumigates, Staphylococcus aureus, Streptococcus pneumonia, Bacillis subtilis, Salmonella typhimurium, Klebsiella pneumonia, Escherichia coli and Mycobacterium tuberculosis. The sulfonamide derivative 21f exhibited superior potency and broad-spectrum antimicrobial activity with minimum inhibitory concentration (MIC) 0.06-0.98 µg/mL and antimycobacterial activity with MIC 3.9 µg/mL. The 5-nitrofuran-2-carbohydrazides 21a, b, g, h and 22a-c exhibited significant antibacterial activity with MIC values in the range of 0.12-7.81 µg/mL. The significances of the 5-nitrofuran moiety and sulfonamide function were explored via the structure-activity relationship (SAR) study. In addition, docking studies revealed that the p-amino benzoic acid (PABA) and binding pockets of the dihydropteroate synthase (DHPS) were successfully occupied by compound 21f. Furthermore, two quantitative structure-activity relationship (QSAR) models were built to explore the structural requirements which controlled the activity.

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Synthesis and antibacterial activity of some new thiazole and thiophene derivatives

Cited by 84 publications

References 11 publications

Antimicrobial activities of thiazole, imidazolidine, tetrahydropyrimidine derivatives and silver/polyvinyl alcohol nanocomposites against selected zoonotic fish bacterial pathogens

Antimicrobial activities of thiazole, imidazolidine, tetrahydropyrimidine derivatives and silver/polyvinyl alcohol nanocomposites against selected zoonotic fish bacterial pathogens

Ninhydrin in synthesis of heterocyclic compounds

Synthesis, <i>in Vitro</i> and <i>in Silico</i> Studies of Some Novel 5-Nitrofuran-2-yl Hydrazones as Antimicrobial and Antitubercular Agents

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