Authors: Mesaik, M. A.; Khan, K. M.; Rahat, S.; Zia-Ullah, Zia-Ullah; Choudhary, M. I.; Murad, S.; Abdullah, N. R.; Atta-ur-Rahman, Atta-ur-Rahman; Ahmad, A.; Siddiqui, R. A.

Source: Letters in Drug Design & Discovery, Volume 2, Number 6, September 2005 , pp. 490-496(7)

Publisher: Bentham Science Publishers

Abstract:

Thirteen imidazolone derivatives were synthesized and characterized by 1H NMR, EI, IR and UV spectroscopic and CHN analysis. Among the compounds tested, two compounds, 3-hydroxy-2-phenyl-5-[Ephenylmethylidene]- 3,5-dihydro-4H-imidazol-4-one (12) and 4-[E-(5-methyl-2-furyl) methylidene]-1,2- diphenyl-1H-imidazol-5-one (13) shown to have suppressing activities on the oxidative burst of neutrophils. These two compounds were then further investigated for their effects on different cellular immune responses including neutrophils, phagocytosis and chemotaxis activities of T-cell proliferation, and cytokine production from mononuclear cells. The results demonstrate that compounds 12 and 13 inhibit reactive oxygen species (ROS) generation and phytohemagglutinin (PHA)-induced T-cell proliferation in a dose dependent manner.

Keywords: imidazolone derivative; immunomodulation; cell proliferation; oxidative burst; chemotaxis

Document Type: Review article

DOI: http://dx.doi.org/10.2174/1570180054771554

Affiliations: 1: HEJ Research Institute of Chemistry International Centre for Chemical Sciences, University of Karachi, Karachi-75270, Pakistan.

Publication date: 2005-09-01

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• Letters in Drug Design & Discovery publishes original letters on all areas of rational drug design and discovery including medicinal chemistry, in-silico drug design, combinatorial chemistry, high-throughput screening, drug targets, and structure-activity relationships. The emphasis will be on publishing quality papers very rapidly. Letters will be processed rapidly by taking full advantage of Internet technology for both the submission and review of manuscripts. The journal is essential reading to all pharmaceutical scientists involved in research in drug design and discovery.

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