Azetidin-2-one derivatives as inhibitors of thrombin

Synthesis and Medicinal Evaluation of Mannich Bases Carrying Azetidinone Moiety

“…Particularly a large number of 3-chloro monocyclic ß-lactams exhibit significant antimicrobial, anti-inflammatory, anticonvulsant, antitubercular etc activities [2][3][4][5][6][7]. They also function as enzyme inhibitors and are effective on the central nervous system [8,9]. Due to the diverse nature of this scaffold, namely 2-azetidinones and in continuation of our search for novel pharmacologically active derivates [10][11][12][13], we herein report the synthesis and pharmacological evaluation of title compounds.…”

Synthesis and Antimicrobial Activity of Some New Sugar-Based Monocyclic β-Lactams

“…Gunda has reported the synthesis of monocyclic β-lactams with high diastereoselectivity [12], while Palomo and his co-workers have synthesized monocyclic β-lactams bearing carbohydrate moieties with moderate diastereoselectivity [13]. The recent discovery of new biologically active monocyclic β-lactam compounds displaying activities other than the usual antibiotic one, such as Thrombin [14], Prostate Specific Antigen [15], Human Cytomegalovirus Protease [16] and the Cholesterol Absorption inhibitors [17] is also interesting. The presence of a carbohydrate moiety side chain in a drug may also overcome the frequently observed water insolubility problem [18].…”

Monocyclic β-lactam and unexpected oxazinone formation: synthesis, crystal structure, docking studies and antibacterial evaluation

“…This results in weakly cross-linked peptidoglycan layer of cell wall leading to the high susceptibility of growing bacteria to cell lysis and death 9 . The b-lactam core structure responsible for antimicrobial activities is also associated with other interesting biological properties such as cholesterol absorption inhibitors 10 , human cytomegalovirus protease inhibitors 11 , anti-HIV 12 , thrombin inhibitors 13 , anti-tumor 14 , anti-hyperglycemic 15 , antiinflammatory, analgesic activities 16 and serine-dependent enzyme inhibitors 17 . However, bacteria have built up resistance against these antibiotics due to their wide-spread use, thus rendering them useless for the treatment of these infections 18 .…”