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1.
Molecules ; 26(14)2021 Jul 12.
Article in English | MEDLINE | ID: mdl-34299494

ABSTRACT

In this article, a zirconia-based nano-catalyst (Nano-ZrO2), with intermolecular C-N bond formation for the synthesis of various benzimidazole-fused heterocycles in a concise method is reported. The robustness of this reaction is demonstrated by the synthesis of a series of benzimidazole drugs in a one-pot method. All synthesized materials were characterized using 1HNMR, 13CNMR, and LC-MS spectroscopy as well as microanalysis data. Furthermore, the synthesis of nano-ZrO2 was processed using a standard hydrothermal technique in pure form. The crystal structure of nano-ZrO2 and phase purity were studied, and the crystallite size was calculated from XRD analysis using the Debye-Scherrer equation. Furthermore, the antimicrobial activity of the synthesized benzimidazole drugs was evaluated in terms of Gram-positive, Gram-negative, and antifungal activity, and the results were satisfactory.


Subject(s)
Anti-Bacterial Agents/pharmacology , Antifungal Agents/pharmacology , Benzimidazoles/pharmacology , Catalysis/drug effects , Nanoparticles/administration & dosage , Zirconium/pharmacology
2.
Curr Org Synth ; 17(5): 396-403, 2020.
Article in English | MEDLINE | ID: mdl-32294044

ABSTRACT

AIMS: A series of six 4-benzylidene-2-((1-phenyl-3,4-dihydro isoquinoline-2(1H)-yl)methyloxazol- 5(4H)-one derivatives were synthesized by condensation of substituted aryl aldehydes with 2-(2-(1-phenyl-3,4- dihydro isoquinoline-2(1H)-acetamido)acetic acid in the presence of sodium acetate, acetic anhydride and zinc oxide as catalysts. BACKGROUND: Novel Synthesis of 4-Benzylidene-2-((1-phenyl-3,4-dihy droisoquinoline-2(1H)-yl)methyl)oxazol- 5(4H)-one derivatives using 1,2,3,Tetrahydroisoquinoline and their antimicrobial activity. OBJECTIVE: The title compounds can be synthesized from 1,2,3,4-tetrahydroisoquinoline. METHODS: The target molecules, i.e., 4-benzylidene-2-((1-phenyl-3, 4-dihydro isoquinoline-2(1H)-yl) methyl) oxazol-5(4H)-one derivatives (8a-8f) have been synthesized from 1,2,3,4-tetrahydroisoquinoline which was prepared from benzoic acid in few steps. RESULTS: All the six compounds were evaluated based on advanced spectral data (1H NMR, 13C NMR & LCMS), and the chemical structures of all compounds were determined by elemental analysis. CONCLUSION: Antibacterial activity of the derivatives was examined for the synthesized compounds and results indicate that compound with bromine substitution has a good activity profile.


Subject(s)
Anti-Bacterial Agents/pharmacology , Isoquinolines/pharmacology , Oxazoles/pharmacology , Anti-Bacterial Agents/chemical synthesis , Bacteria/drug effects , Cyclization , Isoquinolines/chemical synthesis , Microbial Sensitivity Tests , Oxazoles/chemical synthesis
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