Activity of capuramycin analogues against Mycobacterium tuberculosis, Mycobacterium avium and Mycobacterium intracellularein vitro and in vivo

Abstract

These results suggest that capuramycin analogues exhibit strong antimycobacterial potential and should be considered for further evaluation in the treatment of M. tuberculosis and M. avium-M. intracellulare complex infections in humans.

Synthetic Applications of the Parkins Nitrile Hydration Catalyst [PtH{(PMe2O)2H}(PMe2OH)]: A Review

“…Concerning its mechanism of action, Ghaffar and Parkins proposed that in aqueous medium, protonation of the hydride ligand of 1 by water readily takes place, generating a vacant coordination site on the metal for substrate binding, with concomitant dihydrogen extrusion (Scheme 2) [16][17][18]. [22], and its congeners are considered to be important lead molecules for the development of new drugs for Mycobacterium tuberculosis infections [23]. Accordingly, remarkable efforts have been devoted to establish convergent synthetic routes to access 5 that allow the preparation of analogues for SAR (structure-activity relationship) studies [24].…”

Role of quinolones and quinoxaline derivatives in the advancement of treatment of tuberculosis

“…Resistance to one fluoroquinolone, particularly if of high level, generally confers cross-resistance to all other members of this class. With the increasing use of fluoroquinolones for a variety of infections, including respiratory tract infections, fluoroquinolone resistance has emerged among strains of Streptococcus pneumonia [143][144][145][146][147][148][149][150].…”

Challenges facing the drug discovery pipeline for non-tuberculous mycobacteria

“…SQ-641 is a potent anti-TB candidate identified from a library of w7000 analogues of capuramycin created by Daiichi-Sankyo (Japan), and targets translocase I (TL1) with potent bactericidal activity against mycobacteria (Hotoda et al, 2003;Koga et al, 2004). Translocase I is an essential enzyme for the biosynthesis of the bacterial cell wall.…”