Synthesis and antiviral activity of imidazo[1,2- a]pyridines

Imidazo[1,2- a]pyridines bearing a 3-(dithiolan-, dioxolan- or oxathiolan-2-yl) substituent were synthesized from the corresponding aldehydes. The dithiolanyl derivative 6a proved active against cytomegalovirus at an inhibitory concentration (IC 50) of 16 μM, whilethe oxathiolanyl compound 6c inhibi...

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Bibliographic Details
Published in:European journal of medicinal chemistry 1999-03, Vol.34 (3), p.271-274
Main Authors: Lhassani, Mohammed, Chavignon, Olivier, Chezal, Jean-Michel, Teulade, Jean-Claude, Chapat, Jean-Pierre, Snoeck, Richard, Andrei, Graciela, Balzarini, Jan, De Clercq, Erik, Gueiffier, Alain
Format: Article
Language:English
Subjects:
Antibiotics. Antiinfectious agents. Antiparasitic agents
antiviral activity
Antiviral agents
Biological and medical sciences
cytomegalovirus
imidazo[1,2- a]pyridine
Medical sciences
Pharmacology. Drug treatments
respiratory syncytial virus
thioacetal
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Summary:Imidazo[1,2- a]pyridines bearing a 3-(dithiolan-, dioxolan- or oxathiolan-2-yl) substituent were synthesized from the corresponding aldehydes. The dithiolanyl derivative 6a proved active against cytomegalovirus at an inhibitory concentration (IC 50) of 16 μM, whilethe oxathiolanyl compound 6c inhibited respiratory syncytial virus (IC 50: 58 μM). The thioacetal 7 was active against cytomegalovirus at an IC 50 of 3.1 μM. None of the compounds had anti-HIV activity and were not inhibitory against other RNA and DNA viruses evaluated. Compounds 6a,c and 7 had in vitro selectivity indexes (ratio cytostatic concentration/antivirally active concentration) ranging between 8 and 10.
ISSN:0223-5234
1768-3254
DOI:10.1016/S0223-5234(99)80061-0