Design, synthesis and bioactivity evaluation of tribactam beta lactamase inhibitors.
Known carbapenem compounds with inhibitory effect towards beta-lactamase enzymes are formed from bicyclical beta lactam structural scaffolds. On the basis of results from theoretical computational methods and molecular modelling we have designed and developed a synthetic route towards novel, biologically active tricyclic derivatives of carbapenems.
Copar
Anton
A
Lek d.d., Research and Development, Celovska 135, 1526, Ljubljana, Slovenia.
Prevec
Tadeja
T
Anzic
Borut
B
Mesar
Tomaz
T
Selic
Lovro
L
Vilar
Mateja
M
Solmajer
Tom
T
D001409:Bacillus cereus / Q000201:enzymology; D015780:Carbapenems / Q000138:chemical synthesis* / Q000494:pharmacology; D004305:Dose-Response Relationship, Drug; D015195:Drug Design; D006868:Hydrolysis / Q000187:drug effects; D008958:Models, Molecular; D065093:beta-Lactamase Inhibitors; D047090:beta-Lactams / Q000378:metabolism
D015780:Carbapenems; D065093:beta-Lactamase Inhibitors; D047090:beta-Lactams