Structure-activity relationships for a series of thiobenzamide influenza fusion inhibitors derived from 1,3,3-trimethyl-5-hydroxy-cyclohexylmethylamine.

Bioorganic & medicinal chemistry letters ·Vol. 12 ·No. 23 ·2002-12-02 ·Pages 3379-82

Yu KL, Torri AF, Luo G, Cianci C, Grant-Young K, Danetz S, Tiley L, Krystal M, Meanwell NA

Abstract

The anti-influenza activity of a series of thiobenzamide fusion inhibitors derived from 1,3,3-trimethyl-5-hydroxy-cyclohexylmethylamine is profiled. Axial disposition of the thioamide moiety is essential for potent influenza inhibitory activity.

MeSH Terms

Animals Antiviral Agents/chemistry,pharmacology Cells, Cultured Dogs Drug Evaluation, Preclinical Hemolysis/drug effects Inhibitory Concentration 50 Membrane Fusion/drug effects Methylamines/chemistry,pharmacology Orthomyxoviridae/drug effects Quinolizines/chemistry,pharmacology Stereoisomerism Structure-Activity Relationship Thioamides/chemistry,pharmacology

Chemicals

Antiviral Agents BMY 27709 Methylamines Quinolizines Thioamides thiobenzamide methylamine

Authors & Affiliations

9 authors, click to expand affiliations / ORCID

Yu Kuo Long

Department of Chemistry, The Bristol-Myers Squibb Pharmaceutical Research Institute, Wallingford, CT 06492, USA.

Torri Albert F

Luo Guangxiang

Cianci Christopher

Grant-Young Katharine

Danetz Stephanie

Tiley Lawrence

Krystal Mark

Meanwell Nicholas A

Article Info

Journal

Bioorganic & medicinal chemistry letters

Abbr.

Bioorg Med Chem Lett

ISSN

0960-894X

DOI

10.1016/s0960-894x(02)00761-8

Published

2002-12-02

Pages

3379-82

Language

English

Region

England

NLM ID

9107377

Subset

External Links

PubMed source DOI: 10.1016/s0960-894x(02)00761-8 View journal details

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Structure-activity relationships for a series of thiobenzamide influenza fusion inhibitors derived from 1,3,3-trimethyl-5-hydroxy-cyclohexylmethylamine.

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