189268-26-6

Basic information

• Product Name: 1H-Pyrrole-2-carbonitrile, 1-[2,4-dichloro-3-[[[(1,1-dimethylethyl)diphenylsilyl]oxy]methyl]phenyl]-
• CAS NO: 189268-26-6
• Molecular Formula: C28H26Cl2N2OSi
• Molecular Weight: 505.519
• Mol File: 189268-26-6.mol
• Article Data: 4

Chemical Properties

• CAS DataBase Reference: 1H-Pyrrole-2-carbonitrile, 1-[2,4-dichloro-3-[[[(1,1-dimethylethyl)diphenylsilyl]oxy]methyl]phenyl]-(CAS DataBase Reference)
• NIST Chemistry Reference: 1H-Pyrrole-2-carbonitrile, 1-[2,4-dichloro-3-[[[(1,1-dimethylethyl)diphenylsilyl]oxy]methyl]phenyl]-(189268-26-6)
• EPA Substance Registry System: 1H-Pyrrole-2-carbonitrile, 1-[2,4-dichloro-3-[[[(1,1-dimethylethyl)diphenylsilyl]oxy]methyl]phenyl]-(189268-26-6)

Safety Data

• Hazardous Substances Data: 189268-26-6(Hazardous Substances Data)

Upstream product

• 1189-71-5 isocyanate de chlorosulfonyle 
• 189268-25-5 1-[3-(tert-butyldiphenylsilyloxymethyl)-2,4-dichlorophenyl]pyrrole 
• 167837-45-8 3-amino-1-(tert-butyldiphenylsilyloxymethyl)-2,6-dichlorobenzene 

Downstream Products

• 189268-78-8 1-(3-tert-butyldiphenylsilyloxymethyl-2,4-dichlorophenyl)-2-formylpyrrole 
• 189268-93-7 1-(3-tert-Butyldiphenylsilyloxymethyl-2,4-dichlorophenyl)-2-[4-[N-(pyridin-2-ylmethyl)carbamoyl]-cinnamoylaminomethyl]pyrrole 
• 189268-90-4 4-{(1E)-3-[({1-[3-({[tert-butyl(diphenyl)silyl]oxy}methyl)-2,4-dichlorophenyl]-1H-pyrrol-2-yl}methyl)amino]-3-oxo-1-propenyl}-N,N-dimethylbenzamide 
• 189268-95-9 4-{(1E)-3-[({1-[2,4-dichloro-3-(hydroxymethyl)phenyl]-1H-pyrrol-2-yl}methyl)amino]-3-oxo-1-propenyl}-N-(2-pyridynylmethyl)benzamide 
• 189268-92-6 Methanesulfonic acid 2,6-dichloro-3-(2-{[(E)-3-(4-dimethylcarbamoyl-phenyl)-acryloylamino]-methyl}-pyrrol-1-yl)-benzyl ester 
• 189268-91-5 4-{(1E)-3-[({1-[2,4-dichloro-3-(hydroxymethyl)phenyl]-1H-pyrrol-2-yl}methyl)amino]-3-oxo-1-propenyl}-N,N-dimethylbenzamide 
• 189268-27-7 2-aminomethyl-1-[3-(tert-butyldiphenylsilyloxymethyl)-2,4-dichlorophenyl]pyrrole 

Relevant articles and documents

A New Series of Highly Potent Non-Peptide Bradykinin B2 Receptor Antagonists Incorporating the 4-Heteroarylquinoline Framework. Improvement of Aqueous Solubility and New Insights into Species Difference

Introduction of nitrogen-containing heteroaromatic groups at the 4-position of the quinoline moiety of our non-peptide B2 receptor antagonists resulted in enhancing binding affinities for the human B 2 receptor and reducing binding affinities for the guinea pig one, providing new structural insights into species difference. A CoMFA study focused on the diversity of the quinoline moiety afforded correlative and predictive QSAR models of binding for the human B2 receptor but not for the guinea pig one. A series of 4-(1-imidazolyl)quinoline derivatives could be dissolved in a 5% aqueous solution of citric acid up to a concentration of 10 mg/mL. A representative compound 48a inhibited the specific binding of [ 3H]BK to the cloned human B2 receptor expressed in Chinese hamster ovary cells with an IC50 value of 0.26 nM and significantly inhibited BK-induced bronchoconstriction in guinea pigs even at 1 μg/kg by intravenous administration.

Quinoline derivatives as bradykinin agonists

PCT No. PCT/JP97/00233 Sec. 371 Date Aug. 3, 1998 Sec. 102(e) Date Aug. 3, 1998 PCT Filed Jan. 31, 1997 PCT Pub. No. WO97/28153 PCT Pub. Date Aug. 7, 1997This invention relates to a compound of formula (1) wherein R1 is halogen, etc., R2 is halogen, etc., R3 is amino substituted with substituent(s) selected from the group consisting of lower alkyl and acyl, etc., R4 is heterocyclic (lower)alkyl, R5 is lower alkyl, and A1 is lower alkylene, and pharmaceutically acceptable salts thereof, to processes for preparation thereof, to a pharmaceutical composition comprising the same, and to methods of using the same therapeutically in the prevention and/or the treatment of hypertension or the like.