Synthesis of thiosemicarbazones derived from N-(4-hippuric acid)thiosemicarbazide and different carbonyl compounds as antimicrobial agents

El‐Sharief, Marwa A. M. Sh.; Abbas, Samir Y.; El‐Bayouki, Khairy A. M.; El-Gammal, Eman W.

doi:10.1016/j.ejmech.2013.06.031

Cited by 58 publications

(25 citation statements)

References 16 publications

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“…On the other hand, the frequency of fungal poisons has progressively increased from the last 20 years and presents a risky threat to people health, specifically in immunocompromised humans, like those experiencing organ exchanges or antitumor chemotherapy and acquired immunodeficiency syndrome patients . In current years, the investigation has been dedicated on the enlargement of innovative antimicrobial stuffs, those can act over structure design and novel targets, overcoming the difficult of antibiotic resistance …”

Section: Introductionmentioning

confidence: 99%

Design, synthesis of tri‐substituted pyrazole derivatives as promising antimicrobial agents and investigation of structure activity relationships

Reddy

Garcia

Yuvaraja

et al. 2020

Journal of Heterocyclic Chem

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The major diseases spread in the environment only because of microbes. Even, intensive care units in the hospitals are polluted by microorganisms, particularly, Gram-positive bacteria. Although many antibiotics are existed, there is a need to develop up to date microbial-resistant agents. Hence, the current study aimed to develop prominent antimicrobial drug-related compounds. Thus, a novel series of tri-substituted analogs and their intermediates were synthesized. In addition, total new compounds were screened for their antimicrobial assay and identified as the most efficient biologically active compounds. Moreover, minimal inhibitory antimicrobial activity and appropriate structure activity relationships were investigated. From the results it was observed that, viability of Gram-positive bacteria was most powerfully affected by all active compounds. Finally, this research demonstrated that, these biologically energetic amalgams can be utilized for further preclinical studies with the ambition of standing unique inventive drugs.

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Section: Introductionmentioning

confidence: 99%

Design, synthesis of tri‐substituted pyrazole derivatives as promising antimicrobial agents and investigation of structure activity relationships

Reddy

Garcia

Yuvaraja

et al. 2020

Journal of Heterocyclic Chem

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“…1,2,4-Triazole derivatives (7)(8)(9)(10)(11)(12) were prepared in twostep synthesis. In the first step of synthesis, 3-hydroxy-2-naphthoic hydrazide was subjected to condensation reaction with appropriate isothiocyanates to afford 1,4-disubstituted thiosemicarbazide derivatives (1)(2)(3)(4)(5)(6). Then new 1,2,4-triazole-3-thiones (7)(8)(9)(10)(11)(12) were synthesized by the cyclization reaction of corresponding thiosemicarbazide (1-6) derivatives in alkaline media.…”

Section: Chemistrymentioning

confidence: 99%

“…It is known that thiosemicarbazides act as antibacterial [3][4][5], antifungal [6,7], antitubercular [8], anticonvulsant [9,10] and antitumor agents [11,12]. In turn, the 1,2,4-triazoles display a broad range of biological activities, such as antibacterial [13][14][15][16][17][18][19], antifungal [20][21][22], antitubercular [23][24][25][26], antiviral [27] and antiproliferative properties [28][29][30].…”

Section: Introductionmentioning

confidence: 99%

New 3-hydroxy-2-naphthoic hydrazide derivatives: thiosemicarbazides and 1,2,4-triazole-3-thiones, their synthesis and in vitro antimicrobial evaluation

et al. 2016

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In this paper, we describe twelve 3-hydroxy-2-naphthoic hydrazide derivatives (six thiosemicarbazides and six 1,2,4-triazole-3-thiones) which we have synthesized. Thiosemicarbazide derivatives were prepared by condensation reaction of 3-hydroxy-2-naphthoic hydrazide with appropriate isothiocyanates. The 1,2,4-triazole-3-thiones were synthesized by the cyclization reaction of corresponding thiosemicarbazide derivatives in alkaline media. All obtained compounds have been analyzed by 1 H NMR and 13 C NMR spectra and evaluated for in vitro antimicrobial activity against a panel of reference strains of microorganisms, including Gram-positive bacteria, Gramnegative bacteria and fungi belonging to yeasts Candida spp. Our antimicrobial screening results indicated that some of the newly obtained compounds showed high antibacterial activity, especially against Gram-positive bacteria. Among them, the activity of compounds 1, 2 and 4 was moderate to strong against staphylococci. In addition to this, compounds 1 and 2 showed two times higher activity than cefuroxime and four times higher activity than ampicillin against Bacillus cereus ATCC 10876. Electronic supplementary material The online version of this article (

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“…Although there are different antifungal drugs used in the treatment of fungal infections, some of them have undesirable side effects because of the biochemical similarity between human cell and fungi forms. The search for new and effective antimicrobial agents, resistant to the mechanisms of defense of these bacteria, is of paramount importance [1, 2]. Imidazoles and their fused derivatives are keys in many bioactive compounds of both natural and synthetic origins [7] such as histidine, purines, biotin and hydantoin.…”

Section: Introductionmentioning

confidence: 99%

New Imidazolidineiminothione, Imidazolidin-2-one and Imidazoquinoxaline Derivatives: Synthesis and Evaluation of Antibacterial and Antifungal Activities

Ammar

El‐Sharief

Ghorab

et al. 2016

COS

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A series of new 5-imino-4-thioxo-2-imidazolidinone derivatives 3 with various halogenated and alkylated aromatic substituents at N1 and N3 was synthesized. Imidazolidineiminothione derivatives 3 were prepared from the reaction of N-arylcyanothioformamide derivatives with aryl isocyanates. These compounds were used as key synthons for the preparation of wide variety of new substituted imidazole compounds. Imine hydrolysis of 3 with ethanolic HCl produced the corresponding 4-thioxo-2,5-imidazolidindiones 4. Condensation of 3 with benzophenonhydrazone furnished the corresponding 4-azine derivatives 5. Monohydrazono and dihydrazono derivatives 6 and 8 were obtained upon treatment of imidazolidinone derivatives 3 with hydrazine hydrate. Finally, imidazolidinones 3 were reacted with o-phenylenediamines or pyrazol-5(4H)-ones and afforded the corresponding imidazoquinoxaline and imidazolidin-4-ylidenepyrazolone-5(4H)-one derivatives 11 and 12, respectively. Evaluation of the antibacterial and antifungal activities for the synthesized compounds was carried out to probe their activities. Most of the tested compounds showed significant activities. The best antimicrobial activity was observed for 1-(3-ethoxyphenyl)-6-methyl-1-phenyl-1H-imidazo[4,5-b]quinoxalin-2(3H)-ones (11c) followed by 5-imino-3-(3-methoxy- phenyl)-1-phenyl-4-thioxoimidazolidin-2-one (3f).

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Synthesis of thiosemicarbazones derived from N-(4-hippuric acid)thiosemicarbazide and different carbonyl compounds as antimicrobial agents

Cited by 58 publications

References 16 publications

Design, synthesis of tri‐substituted pyrazole derivatives as promising antimicrobial agents and investigation of structure activity relationships

Design, synthesis of tri‐substituted pyrazole derivatives as promising antimicrobial agents and investigation of structure activity relationships

New 3-hydroxy-2-naphthoic hydrazide derivatives: thiosemicarbazides and 1,2,4-triazole-3-thiones, their synthesis and in vitro antimicrobial evaluation

New Imidazolidineiminothione, Imidazolidin-2-one and Imidazoquinoxaline Derivatives: Synthesis and Evaluation of Antibacterial and Antifungal Activities

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