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.

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