e.g. Filippa Pettersson or Cancer Res. 75(6) , 1102-12, (2015) or 10.1002/anie.201600521

2-Aminobenzophenones as a novel class of bradykinin B1 receptor antagonists

…, CM Harrell, SS O'Malley, RW Ransom…

Index: Su, Dai-Shi; Lim, John L.; Tinney, Elizabeth; Wan, Bang-Lin; Murphy, Kathy L.; Reiss, Duane R.; Harrell, C. Meacham; O'Malley, Stacy S.; Ransom, Rick W.; Chang, Raymond S. L.; Pettibone, Douglas J.; Yu, Jian; Tang, Cuyue; Prueksaritanont, Thomayant; Freidinger, Roger M.; Bock, Mark G.; Anthony, Neville J. Journal of Medicinal Chemistry, 2008 , vol. 51, # 13 p. 3946 - 3952

Full Text: HTML

Citation Number: 11

Abstract

Selective bradykinin (BK) B1 receptor antagonists could be novel therapeutic agents for the treatment of pain and inflammation. Elucidation of the structure activity relationships of the structurally novel HTS lead compound 1 provided potent hBK B1 receptor antagonists with excellent receptor occupancy in the CNS of hBK B1 transgenic rats.

2-AMINO-2'-FLUOROBENZOPHENONE Structure

2-AMINO-2'-FLUO...

4-Acetamidobenzenesulfonyl chloride Structure

4-Acetamidobenz...

~%

N-[4-[[2-(2-fluorobenzoyl)phenyl]sulfamoyl]phenyl]acetamide Structure

N-[4-[[2-(2-flu...

(2-aminophenyl)(3,4-difluorophenyl)methanone Structure

(2-aminophenyl)...

4-Acetamidobenzenesulfonyl chloride Structure

4-Acetamidobenz...

~%

N-[4-[[2-(3,4-difluorobenzoyl)phenyl]sulfamoyl]phenyl]acetamide Structure

N-[4-[[2-(3,4-d...

N-(2-benzoylphenyl)-4-nitrobenzenesulfonamide Structure

N-(2-benzoylphe...

~%

4-amino-N-(2-benzoylphenyl)benzenesulfonamide Structure

4-amino-N-(2-be...

2-BROMO-5-FLUOROPYRIDINE Structure

2-BROMO-5-FLUOR...

aminobenzonitrile Structure

aminobenzonitrile

~58%

(2-aminophenyl)-(5-fluoropyridin-2-yl)methanone Structure

(2-aminophenyl)...

2-(2-Aminobenzoyl)pyridine Structure

2-(2-Aminobenzo...

4-Acetamidobenzenesulfonyl chloride Structure

4-Acetamidobenz...

~%

N-[4-[[2-(pyridine-2-carbonyl)phenyl]sulfamoyl]phenyl]acetamide Structure

N-[4-[[2-(pyrid...

(2-aminophenyl)(pyridin-3-yl)methanone Structure

(2-aminophenyl)...

4-Acetamidobenzenesulfonyl chloride Structure

4-Acetamidobenz...

~%

N-[4-[[2-(pyridine-3-carbonyl)phenyl]sulfamoyl]phenyl]acetamide Structure

N-[4-[[2-(pyrid...

2-Amino-4'-fluorobenzophenone Structure

2-Amino-4'-fluo...

4-Acetamidobenzenesulfonyl chloride Structure

4-Acetamidobenz...

~%

N-[4-[[2-(4-fluorobenzoyl)phenyl]sulfamoyl]phenyl]acetamide Structure

N-[4-[[2-(4-flu...

(2-aminophenyl)(2,3-difluorophenyl)methanone Structure

(2-aminophenyl)...

4-Acetamidobenzenesulfonyl chloride Structure

4-Acetamidobenz...

~%

N-[4-[[2-(2,3-difluorobenzoyl)phenyl]sulfamoyl]phenyl]acetamide Structure

N-[4-[[2-(2,3-d...

2-Aminobenzophenone Structure

2-Aminobenzophenone

nosyl chloride Structure

~%

N-(2-benzoylphenyl)-4-nitrobenzenesulfonamide Structure

N-(2-benzoylphe...

(2-AMINO-PHENYL)-PYRIDIN-4-YL-METHANONE Structure

(2-AMINO-PHENYL...

4-Acetamidobenzenesulfonyl chloride Structure

4-Acetamidobenz...

~%

N-[4-[[2-(pyridine-4-carbonyl)phenyl]sulfamoyl]phenyl]acetamide Structure

N-[4-[[2-(pyrid...

(2-aminophenyl)(2,4-difluorophenyl)methanone Structure

(2-aminophenyl)...

4-Acetamidobenzenesulfonyl chloride Structure

4-Acetamidobenz...

~%

N-[4-[[2-(2,4-difluorobenzoyl)phenyl]sulfamoyl]phenyl]acetamide Structure

N-[4-[[2-(2,4-d...

4-Acetamidobenzenesulfonyl chloride Structure

4-Acetamidobenz...

(2-aminophenyl)-(3-fluorophenyl)methanone Structure

(2-aminophenyl)...

~%

N-[4-[[2-(3-fluorobenzoyl)phenyl]sulfamoyl]phenyl]acetamide Structure

N-[4-[[2-(3-flu...

2-Amino-4'-Chlorobenzophenone Structure

2-Amino-4'-Chlo...

4-Acetamidobenzenesulfonyl chloride Structure

4-Acetamidobenz...

~%

N-[4-[[2-(4-chlorobenzoyl)phenyl]sulfamoyl]phenyl]acetamide Structure

N-[4-[[2-(4-chl...

(2-aminophenyl)-(3-chlorophenyl)methanone Structure

(2-aminophenyl)...

4-Acetamidobenzenesulfonyl chloride Structure

4-Acetamidobenz...

~%

N-[4-[[2-(3-chlorobenzoyl)phenyl]sulfamoyl]phenyl]acetamide Structure

N-[4-[[2-(3-chl...