tetano
Editor, Senior Moderator
Chem Biol Drug Des. 2011 Jul 13. doi: 10.1111/j.1747-0285.2011.01180.x. [Epub ahead of print]
Discovery of dihydro-alkyloxy-benzyl-oxopyrimidines as promising anti-influenza virus agents.
Yu M, Liu X, Liu A, Du G, Naesens L, Vanderlinden E, De Clercq E.
Source
Institute of Medicinal Chemistry, School of Pharmaceutical Sciences, Shandong University, No.44 Wenhuaxi Road, Jinan 250012, P. R. China Institute of Materia Medica, Chinese Academy of Medical Sciences, Peking Union Medical College, Beijing 100050, China Rega Institute for Medical Research, Katholieke Universiteit Leuven, B-3000 Leuven, Belgium.
Abstract
A series of novel dihydro-alkyloxy-benzyl-oxopyrimidine (DABO) derivatives were synthesized and evaluated for their activity against influenza virus in MDCK cells. Four DABO derivatives (4a1, 4a2, 4a3, and 4d1) showed potent activity against influenza virus. Among them, compound 4a3 was the most promising lead with broad activity against influenza A (antiviral EC(50) values of 9 and 18 μM for the A/H1N1 and A/H3N2 subtype, respectively) and influenza B virus (EC(50) : 33 μM). The antiviral mechanism of action of these DABO derivatives must be quite different from that of the currently approved anti-influenza virus drugs which target the viral M2 or neuraminidase proteins. The DABO derivatives represent a new avenue for further optimization and development of novel anti-influenza virus agents.
Copyright ? 2011 John Wiley & Sons A/S.
PMID:
21752202
[PubMed - as supplied by publisher]
http://www.ncbi.nlm.nih.gov/pubmed/21752202
Discovery of dihydro-alkyloxy-benzyl-oxopyrimidines as promising anti-influenza virus agents.
Yu M, Liu X, Liu A, Du G, Naesens L, Vanderlinden E, De Clercq E.
Source
Institute of Medicinal Chemistry, School of Pharmaceutical Sciences, Shandong University, No.44 Wenhuaxi Road, Jinan 250012, P. R. China Institute of Materia Medica, Chinese Academy of Medical Sciences, Peking Union Medical College, Beijing 100050, China Rega Institute for Medical Research, Katholieke Universiteit Leuven, B-3000 Leuven, Belgium.
Abstract
A series of novel dihydro-alkyloxy-benzyl-oxopyrimidine (DABO) derivatives were synthesized and evaluated for their activity against influenza virus in MDCK cells. Four DABO derivatives (4a1, 4a2, 4a3, and 4d1) showed potent activity against influenza virus. Among them, compound 4a3 was the most promising lead with broad activity against influenza A (antiviral EC(50) values of 9 and 18 μM for the A/H1N1 and A/H3N2 subtype, respectively) and influenza B virus (EC(50) : 33 μM). The antiviral mechanism of action of these DABO derivatives must be quite different from that of the currently approved anti-influenza virus drugs which target the viral M2 or neuraminidase proteins. The DABO derivatives represent a new avenue for further optimization and development of novel anti-influenza virus agents.
Copyright ? 2011 John Wiley & Sons A/S.
PMID:
21752202
[PubMed - as supplied by publisher]
http://www.ncbi.nlm.nih.gov/pubmed/21752202