… ► Sulfoximine moiety as novel S4 binding element for factor Xa has been identified. ► SAR
… 18f as potent FXa inhibitor. ► Metabolism study indicated presence of an active metabolite …

… phenylpiperazinylamides were used as S4 binding ligands to improve the … they displayed
excellent anti-FXa potency with weak CYP3A4 inhibitory … Structure-activity relationship studies …

… moieties as P2 binding element was designed, synthesized, and … Coagulation enzyme
factor Xa (FXa), a serine protease … 2) and explored the structure–activity relationships (SARs).14, …

… of factor Xa inhibitors in the antithrombotic therapy, we have taken rivaroxaban (15) and
anthranilamide based … to develop small, orally active enzyme inhibitors.Though FXa possesses …

… anthranilamide based compounds.Replacement of highly … a much less basic sulfoximine
resulted into a series of active … Synthesis and structure-activity relationship of 3-substituted 5,6…

… Our group has a persistent interest in the functionalization … a novel synthetic methodology
has been developed for C–N bond formation and for the synthesis of N-α-ketoacyl sulfoximines …

… quinazoline, a potent inhibitor of the Nuclear Factor kappa B (… , utilising existing structure-activity
relationship data from … the direct binding of the different regulatory elements on the …

… developed a novel visible-light-induced N-acylation of sulfoximines under metal-, base-, and
… It could be further utilized to synthesize α-keto N-acyl sulfoximines and modify amino acids …

… groups to develop orally active selective FXa inhibitors. 2.3.1… -based Factor Xa Inhibitors
Designing aspects, synthesis, … biological profile of anthranilamide based FXa inhibitors, we …