N-propargylated isatinmannich mono- and bis- adducts: Synthesis and preliminary analysis of in vitro activity against the protozoal pathogen Tritrichomonas foetus
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
74
DOI
10.1016/j.ejmech.2014.01.015
First Page
657
Last Page
663
Publication Date
3-3-2014
Abstract
Cu(I)Cl promoted synthesis of N-propargylated-isatin Mannich mono- and bis-adducts with an extension towards the synthesis of N-propargylated-isatin-7-chloroquinoline conjugates was described. The synthesized scaffolds were evaluated for their in vitro activity against the veterinary protozoal pathogen Tritrichomonas foetus and cytotoxicity against human prostate (PC-3) cancer cell line. The preliminary evaluation data revealed the enhancement in the activity profiles with the introduction of 7-chloroquinoline ring with the most active conjugates 7a, 7c and 7d exhibiting an IC₅₀ of 22.2, 11.3 and 24.5 μM respectively against T. foetus and minimal toxicity against human prostate (PC-3) cell lines.
Recommended Citation
Nisha.,
Kumar, K.,
Bhargava, G.,
Land, K. M.,
Chang, K.,
Arora, R.,
Sen, S.,
&
Kumar, V.
(2014).
N-propargylated isatinmannich mono- and bis- adducts: Synthesis and preliminary analysis of in vitro activity against the protozoal pathogen Tritrichomonas foetus.
European Journal of Medicinal Chemistry, 74, 657–663.
DOI: 10.1016/j.ejmech.2014.01.015
https://scholarlycommons.pacific.edu/cop-facarticles/772
