57320-20-4

Upstream product

• 3171-45-7 4,5-dimethyl-1,2-phenylenediamine 
• 105-34-0 methyl 2-cyanoacetate 
• 107-91-5 cyanoacetic acid amide 
• 105-56-6 ethyl 2-cyanoacetate 

Downstream Products

• 119750-30-0 3-Hydroxy-7,8-dimethyl-1-oxo-2-phenyl-1,5-dihydro-benzo[4,5]imidazo[1,2-a]pyridine-4-carbonitrile 
• 2148-86-9 ethyl 5,6-dimethyl-1H-benzimidazole-2-acetate 
• 230639-00-6 7,8-dimethyl-1-oxo-1H,5H-3-phenylpyrido<1,2-a>benzimidazole-4-carbonitrile 
• 1314881-66-7 2-(4-(1-amino-2,4-dicyano-7,8-dimethylbenzo[4,5]imidazo[1,2-a]pyridin-3-yl)phenoxy)acetamide 
• 471921-91-2 2-(4-(2-cyano-2-(5,6-dimethyl-1H-benzo[d]imidazol-2-yl)vinyl)phenoxy)acetamide 
• 1335195-72-6 6-amino-5-(5,6-dimethyl-1H-benzimidazol-2-yl)-4-(4-methoxy-phenyl)pyridine-3-carbonitrile 
• 1335195-70-4 6-amino-4-(4-chlorophenyl)-5-(5,6-dimethyl-1H-benzimidazol-2-yl)pyridine-3-carbonitrile 
• 1335195-71-5 6-amino-5-(5,6-dimethyl-1H-benzimidazol-2-yl)-4-(4-hydroxy-phenyl)pyridine-3-carbonitrile 
• 732269-37-3 C₂₂H₁₆FN₅ 
• 119750-35-5 2-Benzyl-3-hydroxy-7,8-dimethyl-1-oxo-1,5-dihydro-benzo[4,5]imidazo[1,2-a]pyridine-4-carboxylic acid ethyl ester 
• 119750-44-6 3-Ethoxy-5-ethyl-7,8-dimethyl-1-oxo-2-phenyl-1,5-dihydro-benzo[4,5]imidazo[1,2-a]pyridine-4-carbonitrile 
• 119750-57-1 1,3-Dichloro-7,8-dimethyl-2-phenyl-benzo[4,5]imidazo[1,2-a]pyridine-4-carboxylic acid ethyl ester 
• 119750-36-6 3-Hydroxy-7,8-dimethyl-1-oxo-2-phenyl-1,5-dihydro-benzo[4,5]imidazo[1,2-a]pyridine-4-carboxylic acid ethyl ester 
• 119750-43-5 3-Methoxy-5,7,8-trimethyl-1-oxo-2-phenyl-1,5-dihydro-benzo[4,5]imidazo[1,2-a]pyridine-4-carbonitrile 

Relevant academic research and scientific papers

Highly Potent and Selective Butyrylcholinesterase Inhibitors for Cognitive Improvement and Neuroprotection

Butyrylcholinesterase (BChE) has been considered as a potential therapeutic target for Alzheimer's disease (AD) because of its compensation capacity to hydrolyze acetylcholine (ACh) and its close association with Aβ deposit. Here, we identified S06-1011 (hBChE IC50 = 16 nM) and S06-1031 (hBChE IC50 = 25 nM) as highly effective and selective BChE inhibitors, which were proved to be safe and long-acting. Candidate compounds exhibited neuroprotective effects and the ability to improve cognition in scopolamine- and Aβ1-42 peptide-induced cognitive deficit models. The best candidate S06-1011 increased the level of ghrelin, a substrate of BChE, which can function as improving the mental mood appetite. The weight gain of the S06-1011-treated group remarkably increased. Hence, BChE inhibition not only plays a protective role against dementia but also exerts a great effect on treating and nursing care.

Development of benzimidazole derivatives to inhibit HIV-1 replication through protecting APOBEC3G protein

Human APOBEC3G (apolipoprotein B mRNA-editing enzyme, catalytic polypeptide-like 3G, A3G) is a potent restriction factor against human immunodeficiency virus type 1 (HIV-1) by inducing hypermutation of G to A in viral genome after its incorporation into virions. HIV-1 Vif (Virion Infectivity Factor) counteracts A3G by inducing ubiquitination and proteasomal degradation of A3G protein. Vif-A3G axis therefore is a promising therapeutic target of HIV-1. Here we report the screening, synthesis and SAR studies of benzimidazole derivatives as potent inhibitors against HIV-1 replication via protecting A3G protein. Based on the steep SAR of the benzimidazole scaffold, we identified compound 14 and 26 which provided the best potency, with IC50 values of 3.45 nM and 58.03 nM respectively in the anti-HIV-1 replication assay in H9 cells. Compound 14 and 26 also afforded protective effects on A3G protein level. Both compounds have been proved to be safe in acute toxicological studies. Taken together, we suggest that these two benzimidazole derivatives can be further developed as a new category of anti-HIV-1 leads.

Discovery of a benzimidazole series of ADAMTS-5 (aggrecanase-2) inhibitors by scaffold hopping

We describe a medicinal chemistry approach to generate a series of benzimidazoles bearing thiazolidin-4-one using scaffold hopping from thiazole 1, our previously described thiazole. Our goal was to discover a potent and permeable small-molecule ADAMTS-5 inhibitor. The results suggest that small compound 22 shows promise as a potent small-molecule ADAMTS-5 inhibitor with good permeability.

Synthesis, characterization of some benzazoles bearing pyridine moiety: Search for novel anticancer agents

Thirteen novel benzazole derivatives were synthesized as possible anticancer agents. The first intermediate 1,3-benzothiazol-2-ylacetonitrile (2) was synthesized via cyclodeamination reaction of o-aminothiophenol (1) with malononitrile. Also, the second i

Inhibition of the cellular function of perforin by 1-amino-2,4- dicyanopyrido[1,2-a]benzimidazoles

A high throughput screen showed the ability of a 1-amino-2,4- dicyanopyrido[1,2-a]benzimidazole analogue to directly inhibit the lytic activity of the pore-forming protein perforin. A series of analogues were prepared to study structure-activity relations

IMIDAZO(1,2-a)PYRIDINE DERIVATIVE

A compound reprsented by the following formula (I), its salts or nsolvates thereof capable of specifically or selectively expressig an antifungal activity in a broad spectrum based on the novel mechanism thereof of 1,6-β-glucan synthesis inhibition, and an antifungal agent containing any of them.

Benzimidazole Condensed Ring Systems. 1. Syntheses and Biological Investigations of Some Substituted Pyridobenzimidazoles

The synthesis of some substituted 3-hydroxy-1-oxo-1H,5H-pyridobenzimidazole-4-carbonitriles and 4-ethyl carboxylates 3 and their O- and N-dialkyl derivatives 5,6 is described. 3-Ethoxy-5-ethyl-2-phenyl-1H,5H-pyridobenzimidazol-1-one 7 was ob