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Wiley-VCH Verlag, ChemInform, 41(44), p. no-no, 2013

DOI: 10.1002/chin.201341150

Elsevier, European Journal of Medicinal Chemistry, (63), p. 897-906

DOI: 10.1016/j.ejmech.2013.03.019

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Synthesis of 1H-1,2,3-triazole linked β-lactam–isatin bi-functional hybrids and preliminary analysis of in vitro activity against the protozoal parasite Trichomonas vaginalis

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This paper is available in a repository.

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Abstract

Twenty-two different triazoles were prepared to examine the anti-Trichomonas vaginalis structure-activity relationships (SAR) within the β-lactam-isatin-triazole conjugate family. The compounds were synthesized by copper-catalyzed 'click chemistry.'In vitro activity against T. vaginalis was determined at 10 and 100 μM for each compound, with eighteen of the synthesized hybrids showing 100% growth inhibition at 100 μM. The compound 5i, with no cytotoxicity on cultured CHO-K1 cells, is considered a good compound for further analysis.