Synthesis, characterization and antimicrobial studies on 3-((4-(4-nitrophenyl)-6-aryl-1,6-dihydropyrimidin-2-yl)thio)propanenitriles and their derivatives

Desai, N. C.; Pandya, Darshan; Vaja, Darshita V.

doi:10.1007/s00044-017-1812-2

Cited by 4 publications

(2 citation statements)

References 17 publications

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“…Overall, it appeared that electron‐withdrawing groups at the benzene ring showed higher antibacterial potency than other groups. Methyl group at the 2‐ and 4‐position, and the methoxy group at the 4‐position showed the highest anti‐fungal activity against A. niger , A. clavatus and C. albicans at 12.5 and 25 μg mL −1 , respectively …”

Section: Othersmentioning

confidence: 99%

“…Methyl group at the 2-and 4position, and the methoxy group at the 4-position showed the highest anti-fungal activity against A. niger, A. clavatus and C. albicans at 12.5 and 25 μg mL À 1 , respectively. [45] Desai et al [46] further designed and synthesized a series of 3-((6-(2,6-dichloroquinolin-3-yl)-4-aryl-1,6-dihydropyrimidin-2-yl) thio)propanenitriles and determined their MIC values. Among them, compound 78 ( Figure 13) exhibited the most potent activity with an MIC value of 0.2 μg mL À 1 against M. tuberculosis.…”

Section: Monocyclic Dihydropyrimidine Derivativesmentioning

confidence: 99%

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Recent Development of Pyrimidine‐Containing Antimicrobial Agents

Zhuang

2020

ChemMedChem

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Multidrug-resistant bacterial infections have become an important cause of clinical death in the twenty-first century. Much effort has been made to overcome this challenge. The discovery of novel antimicrobial compounds, as well as the rational use of antibacterial drugs with different structure types and mechanisms, is helping to deal with bacterial resistance. Currently, pyrimidine-containing agents are the major areas of new antibacterial drug discovery. Given their good activities and diverse mechanisms of action, many pyrimidine-containing heterocyclic compounds have become the focus of interest for many scientists. In addition, pyrimidine structure is an important part of many endogenous substances, which is an advantage that allows pyrimidine derivatives to interact with genetic materials, enzymes and other biopolymeric substances in the cell. Scientists have focused on the discovery and structural optimization of pyrimidine derivatives, which has resulted in the discovery of many novel pyrimidine derivatives with intriguing profiles. Herein we summarize the therapeutic potentials of pyrimidine compounds that are promising for antimicrobial applications over the last decade. In particular, the relationships between the structures of modified pyrimidines and their antimicrobial activity are systematically discussed.

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Section: Othersmentioning

confidence: 99%

Section: Monocyclic Dihydropyrimidine Derivativesmentioning

confidence: 99%

Recent Development of Pyrimidine‐Containing Antimicrobial Agents

Zhuang

2020

ChemMedChem

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Synthetic modifications in ethyl 2-amino-4-methylthiazole-5-carboxylate: 3D QSAR analysis and antimicrobial study

Desai

Bhatt

Joshi

2019

Synthetic Communications

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Synthesis, Antimicrobial Activity and Molecular Docking of Pyrazole Bearing the Benzodiazepine Moiety

Desai

Joshi

Khedkar³

2020

Analytical Chemistry Letters

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Antibacterial assayMueller Hinton Broth dilution method (Becton Dickinson, USA) was used for the antibacterial assay of synthesized compounds. The strains used for antimicrobial activity of newly synthesized compounds were procured from the IMTECH, Chandigarh. The compounds (2a-t) were screened for their antibacterial activity in triplicate sets against these bacteria at different concentrations of 1000, 500, 250, and 200 μg/mL. The drugs which were found to be active in primary analysis were further diluted and evaluated. 10 μg/mL suspensions were further inoculated on appropriate media and the growth was noted after one or two days. Minimum inhibitory concentration is the lowest concentration, which showed no growth of microbes after spot subculture for each drug. The test mixture should contain 10 8 cells/mL. In this study, Ciprofloxacin was the standard drug for evaluating the antibacterial activity. Antifungal assayMueller Hinton Broth dilution method (Becton Dickinson, USA) was used for the antifungal assay of synthesized compounds. The strains used for antimicrobial activity of newly synthesized compounds were procured from the IMTECH, Chandigarh. The newly prepared compounds (2a-t) were screened for their antifungal activity as primary screens in six sets against C. albicans, A. niger, and A. clavatus at various concentrations of 1000, 500, and 250 μg/mL. The primary active compounds were similarly diluted to obtain 200, 125, 100, 62.5, 50, 25, and 12.5 μg/mL concentrations for secondary screening to test in a second set of dilutions against all fungi. The fungal activity of each compound was compared with Nystatin as a standard drug, which showed 100, 100, and 100 μg/mL MIC against C. albicans, A. niger and A. clavatus, respectively. Molecular dockingThe crystal structures of the crucial microbial target DNA gyrase subunit b was retrieved from the Protein Data Bank (RCSB) 1 (PDB ID:1KZN) and refined using the Protein Preparation Wizard.

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Synthesis, characterization and antimicrobial studies on 3-((4-(4-nitrophenyl)-6-aryl-1,6-dihydropyrimidin-2-yl)thio)propanenitriles and their derivatives

Cited by 4 publications

References 17 publications

Recent Development of Pyrimidine‐Containing Antimicrobial Agents

Recent Development of Pyrimidine‐Containing Antimicrobial Agents

Synthetic modifications in ethyl 2-amino-4-methylthiazole-5-carboxylate: 3D QSAR analysis and antimicrobial study

Synthesis, Antimicrobial Activity and Molecular Docking of Pyrazole Bearing the Benzodiazepine Moiety

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