73933-53-6

Upstream product

• 1493-27-2 ortho-nitrofluorobenzene 
• 3731-52-0 3-Aminomethylpyridine 
• 95-54-5 1,2-diamino-benzene 
• 500-22-1 3-pyridinecarboxaldehyde 
• 146651-75-4 tert–butyl (2–aminophenyl)carbamate 
• 73933-52-5 N-(pyridin-3-ylmethyl)-2-nitroaniline 

Downstream Products

• 600725-66-4 4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carboxylic acid ((R)-2-(4-amino-3,5-dibromo-phenyl)-1-{2-[(pyridin-3-ylmethyl)-amino]-phenylcarbamoyl}-ethyl)-amide 
• 600724-66-1 4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carboxylic acid [2-(3,4-dibromo-phenyl)-1-(1-pyridin-3-ylmethyl-1H-benzimidazol-2-yl)-ethyl]-amide 
• 600724-84-3 4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carboxylic acid [2-(4-amino-3-chloro-5-trifluoromethyl-phenyl)-1-(1-pyridin-3-ylmethyl-1H-benzimidazol-2-yl)-ethyl]-amide 

Relevant academic research and scientific papers

Benzimidazole Derivatives as Novel Zika Virus Inhibitors

We have synthesized 50 benzimidazole (BMZ) derivatives with 1,2-phenylenediamines and aromatic aldehydes under mild oxidation conditions by using inexpensive, nontoxic inorganic salt sodium metabisulfite in a one-pot condensation reaction and screened their ability to interfere with Zika virus (ZIKV) infection utilizing a cell-based phenotypic assay. Seven BMZs inhibited an African ZIKV strain with a selectivity index (SI=CC50/EC50) of 9–37. Structure-activity relationship analysis demonstrated that substitution at the C-2, N-1, and C-5 positions of the BMZ ring were important for anti-ZIKV activity. The hybrid structure of BMZ and naphthalene rings was a structural feature responsible for the high anti-ZIKV activity. Importantly, BMZs inhibited ZIKV in human neural stem cells, a physiologically relevant system considering the severe congenital anomalies, like microcephaly, caused by ZIKV infection. Compound 39 displayed the highest antiviral efficacy against the African ZIKV strain in Huh-7 (SI>37) and neural stem cells (SI=12). Compound 35 possessed the highest activity in Vero cells (SI=115). Together, our data indicate that BMZs derivatives have to be considered for the development of ZIKV therapeutic interventions.

Rhenium(I) polypyridine diamine complexes as intracellular phosphorogenic sensors: Synthesis, characterization, emissive behavior, biological properties, and nitric oxide sensing

We report the development of a series of rhenium(I) polypyridine complexes appended with an electron-rich diaminoaromatic moiety as phosphorogenic sensors for nitric oxide (NO). The diamine complexes [Re(N^N)(CO)3(py-DA)] [PF6] (py-DA=3-(N-(2-amino-5-methoxyphenyl)aminomethyl)pyridine; N^N=1,10-phenanthroline (phen) (1a), 3,4,7,8-tetramethyl-1,10-phenanthroline (Me4-phen) (2a), 4,7-diphenyl-1,10-phenanthroline (Ph 2-phen) (3a)) have been synthesized and characterized. In contrast to common rhenium(I) diimines, these diamine complexes were very weakly emissive due to quenching of the triplet metal-to-ligand charge-transfer ( 3MLCT) emission by the diaminoaromatic moiety through photoinduced electron transfer (PET). Upon treatment with NO, the complexes were converted into the triazole derivatives [Re(N^N)(CO)3(py-triazole)][PF 6] (py-triazole=3-((6-methoxybenzotriazol-1-yl)methyl)pyridine; N^N=phen (1b), Me4-phen (2b), Ph2-phen (3b)), resulting in significant emission enhancement (I/I0≈60). The diamine complexes exhibited high reaction selectivity to NO, and their emission intensity was found to be independent on pH. Also, these complexes were effectively internalized by HeLa cells and RAW264.7 macrophages with negligible cytotoxicity. Additionally, the use of complex 3a as an intracellular phosphorogenic sensor for NO has been demonstrated. Emission turned ON for NO: A series of rhenium(I) polypyridine complexes functionalized with an electron-rich diaminoaromatic moiety has been developed as a new class of phosphorogenic sensors for NO. Upon treatment with NO, the weakly emissive complexes were converted into the strongly emissive triazole derivatives, resulting in significant emission enhancement (I/I0≈60; see figure). Experiments showed that the diamine complexes can sense NO that is 1) generated exogenously by NOC-7 in HeLa cells and 2) produced endogenously in RAW264.7 macrophages.

Novel substituted piperidines, pharmaceutical compositions containing these compounds, their use and processes for the preparation thereof

The present invention relates to substituted piperidines of general formula wherein R, R2 to R5, A, X, Z and n are defined as in claim 1, the tautomers, diastereomers, enantiomers, mixtures and salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases which have valuable pharmacological properties, particularly CGRP-antagonistic properties, pharmaceutical compositions containing these compounds, the use thereof and processes for the preparation thereof.

1-(HETEROCYCLYLALKYL)-1,3-DIHYDRO-2-H-BENZIMIDAZOLE-2-ONES

Novel 1-(heterocyclylalkyl)-1,3-dihydro-2H-benzimidazol-2-ones, wherein said heterocyclyl group is a 3-pyrrolidinyl or 3-piperidinyl group, each substituted in the 1-position with a 3-aryloxy-2-hydroxypropyl, 3-arylthio-2-hydroxypropyl or 2-(2,3-dihydro-1