Paper
Synthesis and Anti-Herpes Activity of a Series of Indolizines
Published Oct 1, 1995 · C. Foster, M. Ritchie, D. Selwood
Antiviral Chemistry and Chemotherapy
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Abstract
A systematic screening study identified 2-phenyl-indolizine [1] as having significant human cytomegalovirus (HCMV) activity (IC50 = 7-19 μM). Preliminary mode of action studies on infected cells treated with [1] indicated supression of HCMV-related polypeptides with little effect on the host cells. A series of analogues were synthesized, some of which showed improved HCMV activity although with lower therapeutic indices than [1]. Several analogues demonstrated significant varicella zoster virus activity, with 2-(4-cyanophenyl)indolizine [5] having an IC50 of 5 μM and a therapeutic index of 20 over cell toxicity in the MRC 5 cell line.
Indolizines show potential as anti-herpes agents, with 2-(4-cyanophenyl)indolizine showing the highest anti-HCMV activity and 2-(4-cyanophenyl)indolizine showing the highest anti-varicella zoster virus activity.
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