SYNTHESIS, CHARACTERIZATION AND IN VITRO ANTIMICROBIAL EVALUATION OF SOME NEW AMIDES OF THIOMORPHOLINE CARBOXYLATE

Objective: Synthesis and antimicrobial evaluation of some new amides of Thiomorpholine caboxylate.Methods: A series of new amides of Thiomorpholine caboxylate were synthesized by reacting 4-tert-butyl 2-methyl thiomorpholine-2,4-dicarboxylate 1,1-dioxide with primary amines in presence of Trimethyl aluminum in toluene at ambient temperature in good yields. 4-tert-butyl 2-methyl thiomorpholine-2,4-dicarboxylate 1,1-dioxide was synthesized by reacting tert-butyl thiomorpholine-4-carboxylate 1,1-dioxide with methyl chloroformate in presence of LiHMDS (1M in THF) at -78oC for the first time. The newly synthesized compounds were characterized by IR, 1HNMR, 13C NMR, Mass spectral studies and elemental analysis.Results: A series of new amides of Thiomorpholine carboxylate were synthesized in good yields and all the compounds were screened for their In-vitro antimicrobial activities. Conclusion: Preliminary results revealed that the synthesized compounds were showed moderate to good antibacterial and antifungal activity

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-

One-pot synthesis of novel 1,2,3-triazole-pyrimido[4,5-c]isoquinoline hybrids and evaluation of their antioxidant activity

<p>A series of novel pyrimido[4,5-<i>c</i>]isoquinolines (<b>3a–3h</b>) and 1,2,3-triazole-coupled pyrimido[4,5-<i>c</i>]isoquinolines (<b>4a–4h</b>) were synthesized in good to excellent yields in the one-pot method. The reaction of 6-amino-1,3-dimethyluracil with different 2-iodo benzoyl chlorides using Pd catalyst in dimethylformamide afforded corresponding pyrimido[4,5-<i>c</i>]isoquinolines (<b>3a–3h</b>). One-pot reaction of pyrimido[4,5-<i>c</i>]isoquinolines with propargyl bromide and benzyl azide in THF at room temperature furnished 1,2,3-triazole-coupled pyrimido[4,5-<i>c</i>]isoquinoline (<b>4a–4h</b>). In vitro antioxidant activity examination revealed that compounds <b>4d</b> and <b>4c</b> found to exhibit potent antioxidant activity as compared to the standard drug Trolox with IC₅₀ values 6.02 ± 0.6 and 12.18 ± 0.9 µM, respectively.</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