One pot synthesis of 1-((1-aryl-1H-1,2,3-triazol-4-yl)methyl)-1H-benzo[d] imidazoles in ionic liquids: Evaluation of antioxidant and antimicrobial activities

In view of pharmacological importance of benzimidazole and 1,2,3-triazole nuclei, we made an effort to synthesize the bi-functional mimic 1,2,3-triazolyl-benzimidazoles through the copper catalyzed azide-alkyne 1,3-dipolar cycloaddition reaction in ionic liquids. The synthesized compounds were characterized by NMR, IR and Mass spectral analysis. The synthesized compounds were screened for antimicrobial and antioxidant activities. A good number of the compounds found to possess potent antioxidant and antimicrobial activities

Synthesis and biological evaluation of (3-arylisoxazol-5-yl) methyl 6-fluoro-4-oxo-4H-chromene-2-carboxylates as antioxidant and antimicrobial agents

A series of novel (3-aryl-1,2-oxazol-5-yl) methyl 6-fluoro-4-oxo-4H- -chromene-2-carboxylate derivatives (C1-C12) were synthesized by Cu (I) catalyzed reaction of in situ generated nitrile oxides with prop-2-yn-1-yl 6-fluoro-4-oxo-4H-chromene-2-carboxylate in good yields and investigated their antioxidant and antimicrobial activities. Among all the synthesized compounds, C1 (IC50: 16.43 ± 0.57 μM) and C12 (IC50:15.98 ± 0.72 μM) have registered good antioxidant activity as compared to the standard drug Trolox. Compound-C1, C3, and C6 have registered very good inhibition against all gram-positive and gram-negative bacterial strains with MIC values ranging from 9.375 to 37.5 (μg mL-1). Compound-C7, C8, C9, C10, and C11 have registered good inhibition against B. subtilis and S. aureus with MIC values ranging from 18.75 to 37.5 (μg mL-1). Compound-C10 and C11 against P. aero-ginosa have shown prominent activity than the standard drug Penicillin (MIC: 12.5 μg mL-1) with MIC 9.375 μg mL-1 (~ 1.33 fold potent than Penicillin). Compound-C7, C8, and C9 have registered good to moderate antifungal activity against four tested fungal strains with MIC values ranging from 18.75 and 37.5 μg mL-

Synthesis and antimicrobial evaluation of some novel thiomorpholine derived 1,4-disubstituted 1,2,3-triazoles

A convenient synthesis of novel1,4-disubstituted 1,2,3-triazoles (4a-j & 5a-j) is reported via copper (I) - catalyzed one pot [3+2] cycloaddition of various alkyl halides, sodium azide with (prop-2-yn-1-yl)thiomorpholine and 4-(prop-2-yn-1-yl)thiomorpholine 1,1-dioxide. All the synthesized compounds were investigated for their antimicrobial activity. Compounds 4a, 4b, 4c, 4g, 5a and 5j against S.epidermidis, 4a, 5a and 5d against P. aeroginosa, 4a, 4b and 4g against K.pneumoniae, 4b, 5a and 5d against S.aureus and 5b, 5e and 5j against B.Subtilis have shown excellent antibacterial activity compared to the standard drugs Penicillin and Streptomycin. Compounds 4c, 4e, 4f, 4j, 5c, 5d, 5g and 5j have registered moderate antifungal activity as compared with standard drug Ampothericin-B

Design, synthesis, and biological evaluation of novel substituted imidazo[2,1-<i>a</i>]isoindole derivatives as antibacterial agents

<p>An efficient protocol has been developed for the synthesis of fused imidazo[2,1-<i>a</i>]isoindol-5-ones (<b>2a–d</b>) from 2-iodo benzoic acids and <i>N</i>,<i>N</i>-carbonyldiimidazole (CDI) using one-pot Pd-catalyzed C‒C bond coupling. The reaction of imidazo[2,1-<i>a</i>]isoindol-5-one (<b>2a–d</b>) with substituted α-bromo ketones in toluene afforded corresponding imidazo[2,1-<i>a</i>]isoindolium derivatives (<b>3a–i</b>) in good yields. The structures of the title compounds were well established on the basis of infrared (IR), ¹H NMR, carbon-13 nuclear magnetic resonance (¹³C NMR), mass spectral data, and elemental analysis (C, H, and N). <i>In vitro</i> antibacterial results revealed that, the compounds <b>3b</b> and <b>3i</b> were found to possess an excellent broad spectrum of inhibiting potency against all the tested bacterial strains with minimum inhibitory concentration values ranging from 3.125 to 25 µg mL⁻¹.</p

Synthesis, anticancer and antibacterial evaluation of novel (isopropylidene) uridine-[1,2,3]triazole hybrids

A series of novel (isopropylidene) uridine-[1,2,3]triazole hybrids (3a–3n) were efficiently synthesized via the copper-catalyzed azide–alkyne cycloaddition (CuAAC) from N-propargyl 2′,3′-O-(isopropylidene) uridine with different aryl azides. All the synthesized compounds were screened for their in vitro anticancer and antibacterial activities. The anticancer activity results revealed that compounds 3d and 3f have registered equipotent activity against MCF-7 and 3n has shown excellent activity against HeLa in comparison with the standard drug Cisplatin. Remaining compounds have shown moderate to good anticancer activity against MCF-7 and HeLa cell lines. The antibacterial activity screening results revealed that, compounds 3b and 3n have shown excellent inhibition against Escherichia coli and Bacillus subtilis, 3d against Proteus vulgaris, 3k against Staphylococcus aureus and 3l against S. aureus and B. subtilis have shown equipotent activity in comparison with the standard drug Streptomycin