Molecules

Identification of terfenadine as an inhibitor of human CD81-receptor HCV-E2 interaction: synthesis and structure optimization

…, B Albrecht, B Kronenberger, A Kaul, R Bartenschlager…

Index: Holzer, Marcel; Ziegler, Sigrid; Albrecht, Beatrice; Kronenberger, Bernd; Kaul, Artur; Bartenschlager, Ralf; Kattner, Lars; Klein, Christian D.; Hartmann, Rolf W. Molecules, 2008 , vol. 13, # 5 p. 1081 - 1110

Full Text: HTML

Citation Number: 16

Abstract

Abstract: Terfenadine (4-[4-(hydroxydiphenylmethyl)-1-piperidyl]-1-(4-tert-butyl-phenyl)- butan-1-ol) was identified in a biological screening to be a moderate inhibitor (27% inhibition) of the CD81-LEL–HCV-E2 interaction. To increase the observed biological activity, 63 terfenadine derivates were synthesized via microwave assisted nucleophilic substitution. The prepared compounds were tested for their inhibitory potency by means of ...

Related Articles:

Biooxidation of methyl group: application to the preparation of alcohol and acid metabolites of terfenadine, ebastine and analogues

[El Ouarradi, Amane; Salard-Arnaud, Isabelle; Buisson, Didier Tetrahedron, 2008 , vol. 64, # 51 p. 11738 - 11744]

Structure-activity relationships within a series of analogues of the histamine H 1-antagonist terfenadine

[Zhang; Ter Laak; Timmerman European Journal of Medicinal Chemistry, 1993 , vol. 28, # 2 p. 165 - 173]

Mechanism of block of a human cardiac potassium channel by terfenadine racemate and enantiomers

[Yang; Prakash; Roden; Snyders British Journal of Pharmacology, 1995 , vol. 115, # 2 p. 267 - 274]

Design and synthesis of selective, high-affinity inhibitors of human cytochrome P450 2J2

[Lafite, Pierre; Dijols, Sylvie; Buisson, Didier; Macherey, Anne-Christine; Zeldin, Darryl C.; Dansette, Patrick M.; Mansuy, Daniel Bioorganic and Medicinal Chemistry Letters, 2006 , vol. 16, # 10 p. 2777 - 2780]

More Articles...