Synthesis and Antibacterial Screening of Some 1-Aroyl-3-aryl Thiourea Derivatives

Soni, Love Kumar; Narsinghani, Tamanna; Jain, R.

doi:10.1155/2014/393102

Cited by 10 publications

(5 citation statements)

References 15 publications

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“…is phenomenon has led to the design of novel antimicrobial as well as antibiotic divergent from the current classes of compounds [2]. Specifically, the growth of the new classes of antibacterial agents and modification to the known drugs must be conducted in such a way that would induce them to preserve their physiological action, but a reduction in their resistance towards the agents [3].…”

Section: Introductionmentioning

confidence: 99%

Evaluation of Novel N-(Dibenzylcarbamothioyl)benzamide Derivatives as Antibacterial Agents by Using DFT and Drug-Likeness Assessment

Misral

Sapari

Rahman

et al. 2018

Journal of Chemistry

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Isomers of monothioureas, 2a–2d, derived from the reaction of disubstituted benzoyl isothiocyanate and dibenzylamine were synthesised and characterised by using elementary analysis CHNS and IR, 1H NMR, and 13C NMR spectroscopies. The compounds were screened for their in vitro antibacterial activity by using selected Gram-positive bacteria, and moderate inhibition activity was displayed for compound 2b with the value of inhibition zone 11 ± 0.8 mm at a concentration of 50 mg/ml. The outcomes of Lipinski’s rule of five assessment appeared to be in agreement with all compounds as they adhered to most of the rules, in which they can be preliminarily classified as active drug-like. The frontier molecular orbitals (HOMO and LUMO) for halogen-substituted 3,4-dichloro (2a) and 3,4-difluoro (2b) were also determined by applying the computational method of density functional theory (DFT) to determine their relationship as a molecular descriptor in antibacterial activities. The value of LUMO energy for compound 2b (1.8229 eV) is lower than that of compound 2a (1.8492 eV) which indicates higher antibacterial activities.

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Section: Introductionmentioning

confidence: 99%

Evaluation of Novel N-(Dibenzylcarbamothioyl)benzamide Derivatives as Antibacterial Agents by Using DFT and Drug-Likeness Assessment

Misral

Sapari

Rahman

et al. 2018

Journal of Chemistry

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“…Sterile filter paper disc impregnated with 10 L of the compound in DMSO was placed on the surface of agar plate using a sterile pair of forceps. The plates were then incubated at 37 ∘ C for 24 h. The zones of inhibition were measured in millimetre (mm) to estimate the potency of the test compounds [29].…”

Section: Disc Diffusion Methodmentioning

confidence: 99%

“…All compounds experienced solubility limitation in the assays media which hindered the inhibition studies. Alternatively, disc diffusion method was performed on 1-12 [29]. Ampicillin (positive control) was used as standard drug, while dimethyl sulfoxide (DMSO) was used as negative control with aspirin as a reference.…”

Section: Methyl and Methoxy Anilines And Alkylated Anilines Prepared mentioning

confidence: 99%

Novel Synthetic Monothiourea Aspirin Derivatives Bearing Alkylated Amines as Potential Antimicrobial Agents

Nordin

Chai

Tan

et al. 2017

Journal of Chemistry

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A new series of aspirin bearing alkylated amines moieties 1–12 were synthesised by reacting isothiocyanate with a series of aniline derivatives in overall yield of 16–56%. The proposed structures of all the synthesised compounds were confirmed using elemental analysis, FTIR, and 1H and 13C NMR spectroscopy. All compounds were evaluated for antibacterial activities against E. coli and S. aureus via turbidimetric kinetic and Kirby Bauer disc diffusion method. Compound 5 bearing meta -CH3 substituent showed the highest relative inhibition zone diameter against tested bacteria compared to ortho and para substituent. Furthermore, aspirin derivatives bearing shorter chains exhibited better bacterial inhibition than longer alkyl chains.

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“…Functional moieties such as carbonyl, thiocarbonyl, and amines are building blocks of many drugs. These groups frequently perform a structural role, linking other functionalities and aiding in the optimal orientation for interaction with the drug’s target [ 18 , 19 ]. The chemical reactivity of carbonyl functional groups can also allow these groups to come into close contact with the target, generating hydrogen bonds and other intermolecular interactions.…”

Section: Introductionmentioning

confidence: 99%

In Vitro Anti-Microbial Activity and Anti-Cancer Potential of Novel Synthesized Carbamothioyl-Furan-2-Carboxamide Derivatives

2023

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A series of carbamothioyl-furan-2-carboxamide derivatives were synthesized using a one-pot strategy. Compounds were obtained in moderate to excellent yields (56–85%). Synthesized derivatives were evaluated for their anti-cancer (HepG2, Huh-7, and MCF-7 human cancer cell lines) and anti-microbial potential. Compound p-tolylcarbamothioyl)furan-2-carboxamide showed the highest anti-cancer activity at a concentration of 20 μg/mL against hepatocellular carcinoma, with a cell viability of 33.29%. All compounds showed significant anti-cancer activity against HepG2, Huh-7, and MCF-7, while indazole and 2,4-dinitrophenyl containing carboxamide derivatives were found to be less potent against all tested cell lines. Results were compared with the standard drug doxorubicin. Carboxamide derivatives possessing 2,4-dinitrophenyl showed significant inhibition against all bacterial and fungal strains with inhibition zones (I.Z) in the range of 9–17 and MICs were found to be 150.7–295 μg/mL. All carboxamide derivatives showed significant anti-fungal activity against all tested fungal strains. Gentamicin was used as the standard drug. The results showed that carbamothioyl-furan-2-carboxamide derivatives could be a potential source of anti-cancer and anti-microbial agents.

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Synthesis and Antibacterial Screening of Some 1-Aroyl-3-aryl Thiourea Derivatives

Cited by 10 publications

References 15 publications

Evaluation of Novel N-(Dibenzylcarbamothioyl)benzamide Derivatives as Antibacterial Agents by Using DFT and Drug-Likeness Assessment

Evaluation of Novel N-(Dibenzylcarbamothioyl)benzamide Derivatives as Antibacterial Agents by Using DFT and Drug-Likeness Assessment

Novel Synthetic Monothiourea Aspirin Derivatives Bearing Alkylated Amines as Potential Antimicrobial Agents

In Vitro Anti-Microbial Activity and Anti-Cancer Potential of Novel Synthesized Carbamothioyl-Furan-2-Carboxamide Derivatives

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