Lopez Quezada, Landys; Li, Kelin; McDonald, Stacey L.; Nguyen, Quyen; Perkowski, Andrew J.; Pharr, Cameron W.; Gold, Ben; Roberts, Julia; McAulay, Kathrine; Saito, Kohta; Somersan Karakaya, Selin; Javidnia, Prisca Elis; Porras de Francisco, Esther; Amieva, Manuel Marin; Diaz, Sara Palomo; Mendoza Losana, Alfonso; Zimmerman, Matthew; Liang, Hsin-Pin Ho; Zhang, Jun; Dartois, Veronique; Sans, Stephanie; Lagrange, Sophie; Goullieux, Laurent; Roubert, Christine; Nathan, Carl; Aube, Jeffrey published the artcile< Dual-Pharmacophore Pyrithione-Containing Cephalosporins Kill Both Replicating and Nonreplicating Mycobacterium tuberculosis>, Electric Literature of 3811-73-2, the main research area is pyrithione containing cephalosporin Mycobacterium replication; antimycobacterial; cephalosporin; pyrithione; tuberculosis; β-lactamase.
The historical view of β-lactams as ineffective antimycobacterials has given way to growing interest in the activity of this class against Mycobacterium tuberculosis (Mtb) in the presence of a β-lactamase inhibitor. However, most antimycobacterial β-lactams kill Mtb only or best when the bacilli are replicating. Here, a screen of 1904 β-lactams led to the identification of cephalosporins substituted with a pyrithione moiety at C3′ that are active against Mtb under both replicating and nonreplicating conditions, neither activity requiring a β-lactamase inhibitor. Studies showed that activity against nonreplicating Mtb required the in situ release of the pyrithione, independent of the known class A β-lactamase, BlaC. In contrast, replicating Mtb could be killed both by released pyrithione and by the parent β-lactam. Thus, the antimycobacterial activity of pyrithione-containing cephalosporins arises from 2 mechanisms that kill mycobacteria in different metabolic states.
ACS Infectious Diseases published new progress about Blood plasma. 3811-73-2 belongs to class pyridine-derivatives, and the molecular formula is C5H4NNaOS, Electric Literature of 3811-73-2.