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.
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 ?M) and C12 (IC50:15.98 ? 0.72 ?M) 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 (?g 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 (?g mL-1). Compound-C10 and C11 against P.
aero-ginosa have shown prominent activity than the standard drug Penicillin
(MIC: 12.5 ?g mL-1) with MIC 9.375 ?g 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 ?g mL-1
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