174422-23-2

Upstream product

• 104-86-9 4-chlorobenzylamine 
• 96-99-1 4-chloro-3-nitrobenzoate 
• 14719-83-6 methyl 3-nitro-4-chlorobenzoate 
• 174422-22-1 methyl 4-(4-chlorobenzylamine)-3-nitrobenzoic acid ester 

Downstream Products

• 1002322-47-5 methyl 1-(p-chlorobenzyl)-2-phenyl-1H-benzimidazole-5-acetate 
• 1393711-18-6 methyl 1-(4-chlorobenzyl)-2-(3,4-dichlorophenyl)-1H-benzimidazole-5-carboxylate 
• 1168138-16-6 1-[(4-chlorophenyl)methyl]-2-methyl-N-[(1R)-1-phenylpropyl]-1H-benzimidazole-5-carboxamide 
• 1096969-16-2 1-[(4-chlorophenyl)methyl]-2-methyl-1H-benzimidazole-5-carboxylic acid 
• 1168139-12-5 methyl 1-[(4-chlorophenyl)methyl]-2-methyl-1H-benzimidazole-5-carboxylate 
• 1168139-13-6 methyl 1-(4-chlorobenzyl)-1H-benzo[d]imidazole-5-carboxylate 
• 214903-74-9 1-(4-Chloro-benzyl)-2-(4-methyl-piperazin-1-yl)-1H-benzoimidazole-5-carboxylic acid methyl ester 
• 214903-76-1 1-(4-Chloro-benzyl)-2-(4-methyl-piperazin-1-yl)-1H-benzoimidazole-5-carboxylic acid 
• 214903-71-6 2-Chloro-1-(4-chloro-benzyl)-1H-benzoimidazole-5-carboxylic acid methyl ester 
• 848819-92-1 1-(4-chloro-benzyl)-2-ethoxycarbonylmethyl-1H-benzoimidazole-5-carboxylic acid methyl ester 
• 355022-45-6 2-(4-carboxy-phenyl)-1-(4-chloro-benzyl)-1H-benzoimidazole-5-carboxylic acid methyl ester 
• 214903-70-5 1-(4-Chloro-benzyl)-2-oxo-2,3-dihydro-1H-benzoimidazole-5-carboxylic acid methyl ester 
• 174422-24-3 3-Amino-4-(p-chlorophenylmethyl)aminobenzoic acid 

Relevant academic research and scientific papers

Heterocyclic derivative and pharmaceutical composition comprising the same

The present invention provides novel compounds having a P2X3 and/or P2X2/3 receptor antagonistic effect. A pharmaceutical composition having a P2X3 and/or P2X2/3 receptor antagonistic effect comprising a compoun

NOVEL HETEROCYCLIC DERIVATIVES AND PHARMACEUTICAL COMPOSITION CONTAINING SAME

The present invention provides novel compounds having a P2X3 and/or P2X2/3 receptor antagonistic effect. A pharmaceutical composition having a P2X3 and/or P2X2/3 receptor antagonistic effect comprising a compoun

Discovery of GSK1997132B a novel centrally penetrant benzimidazole PPARγ partial agonist

The peroxisome proliferator-activated receptor γ (PPARγ) is a ligand-activated nuclear receptor, thought to play a role in energy metabolism, glucose homeostasis and microglia-mediated neuroinflammation. A novel benzimidazole series of centrally penetrant PPARγ partial agonists has been identified. The optimization of PPARγ activity and in vivo pharmacokinetics leading to the identification of GSK1997132B a potent, metabolically stable and centrally penetrant PPARγ partial agonist, is described.

NOVEL COMPOUNDS

The invention relates to novel benzimidazole compounds of formula (I) wherein R1 to R1 are as defined in the specification, pharmaceutically acceptable salts thereof, to pharmaceutical compositions containing them and their use in medicine. In particular, the invention relates to compounds that are agonists of peroxisome proliferators-activated receptorγ (PPARγ).

Synthesis and antioxidant capacities of some new benzimidazole derivatives

In this study, we prepared some new oxadiazolyl benzimidazole derivatives and investigated their antioxidant properties by determination of microsomal NADPH-dependent inhibition of lipid peroxidation levels (LP assay) and microsomal ethoxyresorufin O-deet

Synthesis and potent antimicrobial activity of some novel methyl or ethyl 1H-benzimidazole-5-carboxylates derivatives carrying amide or amidine groups

A series of benzimidazole-5-carboxylic acid alkyl ester derivatives carrying amide or amidine substituted methyl or phenyl groups at the position C-2 were synthesised and evaluated for antibacterial and antifungal activities against S. aureus, methicillin

Synthesis of some novel tetrahydronaphthalene benzimidazole derivatives

Retinoids, synthetic and natural analogues of all-trans-retinoic acid (RA), exert their biological effects with responsive elements of DNA to promote on cell differentiation and proliferation and behave as potent adipogenic hormones. Herein, we describe the synthesis of a number of novel tetrahydrotetramethylnaphthalene benzimidazole derivatives as retinoids. Analogs were prepared as depicted in Scheme 1 and 2. As is evident from both shemes, a variety of tetrahydrotetramethylnaphthalene benzimidazole derivatives have been synthesized by using an appropiate NaHSO3 addiction product.

Synthesis of some new benzimidazolecarboxamides and evaluation of their antimicrobial activity

A series of 1,2-disubstituted benzimidazole-5(6)-carboxamides was prepared and evaluated in vitro for antimicrobial activity against Staphyloccus aureus, Escherichia coli and Candida albicans. The precursor benzimidazolecarboxylic acids 4a-c and 9a-c were

SYNTHESIS OF 1,2-DISUBSTITUTED BENZIMIDAZOLE-5(6)-CARBOXAMIDES AND EVALUATION OF THEIR ANTIMICROBIAL ACTIVITY

A series of 14,N'-(N,N-dialkylaminoethyl)-benzimidazole-5(6) or 5-carboxamides (1-14), having several substituents on the azole and benzene nuclei, were prepared and evalueted in vitro for antimicrobial activity.The precursor bezimidazolecarboxylic acids (15-27) were prepared via oxidative condensation of diaminobenzoic acids and several aldehydes with cupric ion.Compounds 11-14 were prepared by selective regioisomer synthesis.All carboxamides were prepared from the corresponding acids and N,N-dialkylethylenediamine.Antibacterial and antifungal activities were determined as MICs values.Of the synthesized compounds 1-10, 6 and 10 were found to be most favourable.In order to clarify the effect of the substituents at N1 on antimicrobial activity, 12 was prepared by p-chlorobenzyl substitution of compound 6, and increased activity was shown.Compounds 13 and 14, which were prepared by replacement with more bulky alkyl groups on the tert-N atom than 12, gave the best results.