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Title: Synthesis of novel heteroarenes based [1,2,3]-triazoles <i style="">via</i> click chemistry and their evaluation for antibacterial activity
Authors: Prasad, Davinder
Aggarwal, Nisha
Kumar, Rajesh
Nath, Mahendra
Keywords: Heteroarenes
Click chemistry
Antibacterial activity
Issue Date: May-2012
Publisher: NISCAIR-CSIR, India
Abstract: A series of heteroarenes based [1,2,3]-triazole derivatives <b style="">8a-h</b> and <b style="">9a-f</b> has been synthesized <i style="">via</i> click chemistry through Huisgen [2+3] cycloaddition reaction of heteroarylazides <b style="">7a-e</b> with alkynes (<b style="">3a-c</b>, propargyl alcohol or phenyl acetylene) in the presence of CuSO<sub>4</sub>.5H<sub>2</sub>O and sodium ascorbate in <i style="">t</i>-butanol and water (1:1) mixture at 25°C in good to excellent yields (74-94%). All the newly synthesized compounds have been characterized on the basis of analytical and spectral data. The compounds <b style="">8a</b>, <b style="">8e</b>, <b style="">9a</b>, <b style="">9b</b>, <b style="">9c</b> and <b style="">9e</b> have been evaluated for their preliminary <i style="">in-vitro</i> antibacterial efficacy against a panel of two Gram-positive bacteria viz. <i style="">Staphylococcus aureus</i> and <i style="">Streptococcus mutans</i> and two Gram-negative bacteria viz. <i style="">Escherichia</i> <i style="">coli</i> and <i style="">Pseudomonas aeruginosa </i>using the Agar disc diffusion method.
Description: 731-738
ISSN: 0975-0983(Online); 0376-4699(Print)
Appears in Collections:IJC-B Vol.51B(05) [May 2012]

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