Naslov
Azetidinone-isothiazolidinones: Stereoselective synthesis and antibacterial evaluation of new monocyclic beta-lactams

Autori
Cerić, Helena ; Šindler-Kulyk, Marija ; Kovačević, Miće ; Perić, Mihaela ; Živković, Andreja

Izvornik
Bioorganic & medicinal chemistry (0968-0896) 18 (2010), 9; 3053-3058

Vrsta, podvrsta i kategorija rada
Radovi u časopisima, članak, znanstveni

Ključne riječi
beta-lactam ; antibacterial activity ; azetidinone-isothiazolidinone

Sažetak
Beta-lactam antibiotics are still the main drugs to treat infections caused by bacteria. These molecules disturb the final step of bacterial cell wall biosynthesis by inhibiting penicillin binding proteins (PBPs) involved in the crosslinking of peptidoglycan strands.1 The first classes of monocyclic beta-lactam antibacterial agents were isolated from natural sources in the late 1970s and early 1980s. The discovery of nocardicines and monobactams (Fig. 1) demonstrated for the first time that a conformationally constrained bicyclic structure was not necessary for antibacterial activity.2-5 Research efforts in this class led to preparation of semi-synthetic and synthetic monobactam analogues like Aztreonam and Carumonam (Fig. 1), active mostly against Gram-negative bacteria. Work in this area is still very active and new compounds are synthesized and reported as inhibitors of D, D-transpeptidaze, 6 beta-lactamase, 7 mammalian elastase8-9 and cholesterol uptake.10 Some of the compounds out of this class have also shown antifungal11 and antitubercular activity.12

Izvorni jezik
Engleski

Znanstvena područja
Kemija

POVEZANOST RADA