The development of new antibacterial drugs with different mechanisms of action is urgently needed to address antimicrobial resistance. MraY is an essential membrane enzyme required for bacterial cell wall synthesis. Sphaerimicins are naturally occ...
The total synthesis of capuramycin (1), which is a promising anti-tubercular antibiotics, has been accomplished using Ferrier-type I reaction as a key step. This total synthesis is an alternative approach to the synthesis of capuramycin and its an...
Malcolm S Cole   Michael D Howe   Joseph A Buonomo   Sachin Sharma   Elise A Lamont   Scott I Brody   Neeraj K Mishra   Yusuke Minato   Joshua M Thiede   Anthony D Baughn   Courtney C Aldrich   
Chemistry (Weinheim an der Bergstrasse, Germany) 2022年6月 [査読有り]
Tuberculosis (TB) is a leading source of infectious disease mortality globally. Antibiotic-resistant strains comprise an estimated 10% of new TB cases and present an urgent need for novel therapeutics. β-lactam antibiotics have traditionally been ...
It is important to understand and control the biologically active conformation in medicinal chemistry. Muraymycins and caprazamycins, which are strong inhibitors of MraY, are promising antibacterial agents with a novel mode of action. Focusing on ...
Joshua M Thiede   Nicholas A Dillon   Michael D Howe   Ranee Aflakpui   Samuel J Modlin   Sven E Hoffner   Faramarz Valafar   Yusuke Minato   Anthony D Baughn   
mBio e0043921 2022年2月 [査読有り]
Pyrazinamide (PZA) plays a crucial role in first-line tuberculosis drug therapy. Unlike other antimicrobial agents, PZA is active against Mycobacterium tuberculosis only at low pH. The basis for this conditional drug susceptibility remains undefin...