N-Thiolated β-Lactams: novel antibacterial agents for methicillin-Resistant Staphylococcus aureus

Abstract

In this report we describe a new family of N-thiolated beta-lactams that have antibacterial activity against methicillin-resistant Staphylococcus aureus (MRSA). The compounds show unprecedented structure-activity features and an unusual mode of action for a beta-lactam antibiotic.

Drug delivery approaches to overcome bacterial resistance to β-lactam antibiotics

“…In addition, ceftobiprole is relatively stable towards class C β -lactamases. The development of new β -lactam antibiotics with alternative mechanisms of action, such as N -alkylthio β -lactams ( Figure 15 ) [105][106][107] , offers an unprecedented new approach to tackle the resistance problem. This family of antibacterial compounds shows promising activity against only a few strategic pathogenic bacteria, a short list that includes MRSA and Bacillus anthracis .…”

Differentialin vitroinhibition effects of some antibiotics on tumor associated carbonic anhydrase isozymes of hCA-IX and hCA-XII

“…b-lactam compounds have been used in the treatment of bacterial infections for nearly 60 years [24]. Following the initial introduction of penicillin, a variety of other classes of b-lactam antibiotics were subsequently identified and used clinically, including cephalosporins, penems, carbapenems, nocardicins, and monobactams.…”

“…Following the initial introduction of penicillin, a variety of other classes of b-lactam antibiotics were subsequently identified and used clinically, including cephalosporins, penems, carbapenems, nocardicins, and monobactams. The bacterial targets of these antibiotics are membrane-bound transpeptidases referred to as the penicillin-binding proteins, which are responsible for creating crosslinks within the bacterial cell wall [24].…”

Isolation and Characterization of Bacillus subtilis MP56 with Antimicrobial Activity against MDR (Multi Drug Resistant) Strains

“…다약제 내성 세균에는 MRSA (methicillin resistant Staphylococcus aureus), VRSA (vancomycin resistant Staphylococcus aureus), VRE (vancomycin resistant enterococci) 등이 있다. MRSA의 경우 1961 년 영국에서 보고되었고, 국내에서는 80년대부터 보고되기 시작하 여 현재는 원내감염의 대표적 원인균으로 간주되고 있다 (Turos et al, 2002). 기존의 Staphylococcus aureus (황색포도상 구균)의 경우 penicillin, ampicillin, macrolides 등의 항생제군으로 치료 가 가능하였으나, 장기간 사용으로 인한 다제 내성으로 인해 최근 에는 vancomycin, teicoplanin, linezolid 등의 항생물질이 사용되 고 있다.…”