Desmethyl Macrolides: Synthesis and Evaluation of 4,8,10-Tridesmethyl Telithromycin | Zendy

Venkata Velvadapu | Zendy; Tapas Paul | Zendy; Bharat Wagh | Zendy; Dorota Klepacki | Zendy; Olgun Guvench | Zendy; Alexander D. MacKerell | Zendy; Rodrigo Andrade | Zendy

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Desmethyl Macrolides: Synthesis and Evaluation of 4,8,10-Tridesmethyl Telithromycin

Author(s) -

Venkata Velvadapu,

Tapas Paul,

Bharat Wagh,

Dorota Klepacki,

Olgun Guvench,

Alexander D. MacKerell,

Rodrigo Andrade

Publication year - 2010

Publication title -

acs medicinal chemistry letters

Language(s) - English

Resource type - Journals

SCImago Journal Rank - 1.065

H-Index - 66

ISSN - 1948-5875

DOI - 10.1021/ml1002184

Subject(s) - telithromycin , erythromycin , desmethyl , antibiotics , ketolide , macrolide antibiotics , medicine , microbiology and biotechnology , pharmacology , biology , metabolite

There is an urgent need to discover new drugs to address the pressing problem of antibiotic-resistance. Macrolide antibiotics such as erythromycin (1) are safe, broad-spectrum antibiotics used in the clinic since 1954. Herein we report the synthesis and evaluation of 4,8,10-tridesmethyl telithromycin (3), a novel desmethyl analogue of the 3rd-generation drug telithromycin (2), which is a semisynthetic derivative of 1. Analogue 3 was found to possess antibiotic activity and was superior to telithromycin (2) when tested against resistant strains of S. aureus possessing an A→T mutation at position 2058 (E. coli numbering).

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