Synthesis of 1H-1,2,3-triazole linked β–lactam-Isatin Bifunctional Hybrids and preliminary analysis of in vitro activity against the protozoal parasite Trichomonas vaginalis
ORCID
Kirkwood M. Land: 0000-0001-5951-9630
Document Type
Article
Publication Title
European Journal of Medicinal Chemistry
Department
Biological Sciences
ISSN
0223-5234
Volume
63
DOI
10.1016/j.ejmech.2013.03.019
First Page
897
Last Page
906
Publication Date
5-1-2013
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.
Recommended Citation
Raj, R.,
Singh, P.,
Haberkern, N. T.,
Faucher, R. M.,
Patel, N.,
Land, K. M.,
&
Kumar, V.
(2013).
Synthesis of 1H-1,2,3-triazole linked β–lactam-Isatin Bifunctional Hybrids and preliminary analysis of in vitro activity against the protozoal parasite Trichomonas vaginalis.
European Journal of Medicinal Chemistry, 63, 897–906.
DOI: 10.1016/j.ejmech.2013.03.019
https://scholarlycommons.pacific.edu/cop-facarticles/770
