Title:Carbapenem Antibiotics: Recent Update on Synthesis and Pharmacological
Activities
Volume: 15
Issue: 1
Author(s): Abhishek Tiwari*, Varsha Tiwari, Biswa Mohan Sahoo, Bimal Krishna Banik, Manish Kumar and Navneet Verma
Affiliation:
- Pharmacy Academy, IFTM University, Lodhipur-Rajput, Moradabad (U.P.) -244102 India
Keywords:
Carbapenem, antibiotics, structure, chemistry, resistance, mechanism of action.
Abstract: Right from the breakthrough of carbapenems since 1976, many schemes on synthesis,
structure-activity relationship (SAR), and biological activities have been carried out, and
several carbapenems have been developed, including parentally active carbapenems like
imipenem, doripenem, biapenem, meropenem, ertapenem, panipenem, razupenem, tomopenem,
and cilastatin, whereas orally active carbapenems like GV-118819, GV-104326, CS-834, L-084,
DZ-2640, CL 191, 121, L-646, 591, S-4661, ER-35768, MK-826. Prodrugs of carbapenem with
increased bioavailability include temopenem, tebipenem, sanfetrinem, LK-157, and CP 5484.
Merck, Glaxo Welcome Research Group, Johnson & Johnson, Sankyo Group and Dai-ichi
Group, and Wyeth-Ayerst Group were among the businesses that produced carbapenems. In this
review Witting reaction, Mitsunobu reaction, Dieckmann reaction, palladium-catalyzed hydrogenolysis,
E. coli-based cloned synthesis, as well as biosynthetic enzymes such as carbapenem
synthetase (carA), carboxymethylproline synthase (carB), carbapenem synthase (carC) are included.
Carbapenems are biologically mainly active in the infections like urinary tract infections,
bloodstream infections, tuberculosis, intra-abdominal infections, and pathogens like anaerobes,
gram-positive and gram-negative bacteria.