Employing a highly efficient total synthesis approach, we synthesized and evaluated for
antibacterial activity diverse and novel pentacycline analogs with systematic variations at C7, C8…

Simple Summary Immune therapy is designed to stimulate tumoricidal effects in a variety of
solid tumors including breast carcinomas. However, the emergence of resistant clones leads …

Objectives: BB-83698 is a peptide deformylase inhibitor currently in clinical trials in Europe.
The purpose of this study was to provide additional susceptibility data from clinical isolates, …

Clostridium difficile infection (CDI) results in clinical manifestations ranging from mild
diarrhea to life-threatening pseudomembranous colitis. Infection is most often initiated by …

Peptide deformylase (PDF) catalyzes the removal of the N-terminal formyl group from newly
synthesized polypeptides in eubacteria. Its essential role in bacterial cells but not in …

Eravacycline is a novel broad-spectrum fluorocycline antibiotic being developed for a wide
range of serious infections. Eravacycline was efficacious in mouse septicemia models, …

A novel series of fully synthetic 8-azatetracyclines was prepared and evaluated for antibacterial
activity. Compounds were identified that overcome both efflux (tet(K)) and ribosomal …

BB-83698, a potent and selective inhibitor of peptide deformylase, was the first compound
of this novel antibacterial class to progress to clinical trials. Single- and/or multiple-dose …

Potent in vivo activity against methicillin-resistant Staphylococcus aureus (MRSA) has been
difficult to achieve with previously reported DNA binding antibacterials. Herein, we describe …

The Pseudomonas aeruginosa efflux pumps MexAB-OprM, MexCD-OprJ, and MexEF-OprN
play an important role in susceptibility to fluoroquinolones in vitro. To determine if …