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Updated: Jul 6, 2026

Visualization of Bacterial Resistance using Fluorescent Antibiotic Probes
Published on: March 2, 2020
Novel antibacterial azetidine lincosamides
Hardwin O'Dowd1, Jason G Lewis, Joaquim Trias
1Pfizer Global Research & Development, Fremont, Formerly Vicuron Pharmaceuticals, Inc., CA 94555, USA. hardwin@hotmail.com
Abstract:
The synthesis and evaluation of novel azetidine lincosamides 1 are described. Eleven new (3-trans-alkyl)azetidine-2-carboxylic acids were synthesized via alkylation of N-TBS-4-oxo-azetidine-2-carboxylic acid and subsequent elaboration then coupled to 7-chloro-1-methylthio-lincosamine. The resulting lincosamides differ from the drug clindamycin in both the size of the ring and the position/structure of the alkyl side-chain. SAR within the series was explored with attention to alkyl variants in positions 1 and 3 of the azetidine ring.
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