In Vitro Antimicrobial Activity and Structure-activity Relationship of C-2 Triazolylthio and Pyridinylmethylthio Carbapenems

Although the low molecular weight, excellent beta -lactamase stability and high affinity for bacterial PBPs of carbapenems provide exceptional antibacterial spectrum, the nature of C-2 substitution has also been recognized as major contributor to carbapenems antibacterial properties. Presence of basic or quaternary amino moieties at C-2 considerably improves the chemical stability and extends the antibacterial spectrum relative to compounds with less basic side chain at the same position. In this paper we have focused our attention to study the effect of groups such as 3-substituted-1,2,4-triazol-5-yl-thio and halosubstituted pyridin-3-yl-methylthio at position 2 of carbapenems towards antimicrobial activity especially against Gram-positive strains including highly resistant S. aureus.