87815-77-8

Upstream product

• 16588-16-2 ethyl 4-chloro-3-nitrobenzoate 
• 108-91-8 cyclohexylamine 
• 367-80-6 ethyl 4-fluoro-3-nitrobenzoate 
• 96-99-1 4-chloro-3-nitrobenzoate 
• 453-71-4 3-nitro-4-fluorobenzoic acid 

Downstream Products

• 347174-05-4 3-Amino-4-cyclohexylamino benzoic acid ethyl ester 
• 347165-36-0 ethyl 1-cyclohexyl-2-(4-hydroxyphenyl)-1H-benzimidazole-5-carboxylate 
• 480460-90-0 ethyl 1-cyclohexyl-2-(2-fluoro-4-hydroxyphenyl)-1H-benzimidazole-5-carboxylate 
• 347166-09-0 2-[4-(Benzyloxy)phenyl]-1-cyclohexyl-1H-benzimidazole-5-carboxylic acid 
• 885312-82-3 2-(4-benzyloxy-phenyl)-1-cyclohexyl-1H-benzoimidazole-5-carboxylic acid ethyl ester 
• 885313-15-5 ethyl 1-cyclohexyl-2-(4-diphenylmethoxyphenyl)-1H-benzimidazole-5-carboxylate 
• 885313-14-4 ethyl 1-cyclohexyl-2-[4-(5-phenylpentyloxy)phenyl]-1H-benzimidazole-5-carboxylate 

Relevant academic research and scientific papers

Design and synthesis of amino acid derivatives of substituted benzimidazoles and pyrazoles as Sirt1 inhibitors

Owing to its presence in several biological processes, Sirt1 acts as a potential therapeutic target for many diseases. Here, we report the structure-based designing and synthesis of two distinct series of novel Sirt1 inhibitors, benzimidazole mono-peptide

COMPOUNDS, COMPOSITIONS, AND METHODS FOR MODULATING FERROPTOSIS AND TREATING EXCITOTOXIC DISORDERS

The present disclosure provides, inter alia, a compound having the structure (1). Also provided are compositions containing a pharmaceutically acceptable carrier and one or more compounds according to the present disclosure. Further provided are methods f

MODULATING FERROPTOSIS AND TREATING EXCITOTOXIC DISORDERS

The present invention provides, inter alia, a compound having the structure of Formula (I). Also provided are compositions containing a pharmaceutically acceptable carrier and a compound according to the present invention. Further provided are methods for treating or ameliorating the effects of an excitotoxic disorder in a subject, methods of modulating ferroptosis in a subject, methods of reducing reactive oxygen species (ROS) in a cell, and methods for treating or ameliorating the effects of a neurodegenerative disease.

Novel arylalkylamine compounds exhibits potent selective antiparasitic activity against Leishmania major

Leishmania major (L. major) is a protozoan parasite causal agent of Leishmaniasis. It is estimated that 12 million people are currently infected and around 2 million infections occur each year. Current treatments suffer of high toxicity for the patient, low efficacy toward the parasite, high cost, and are losing effectiveness due to parasite resistance. Discovering novel small molecule with high specificity/selectivity and drug-like properties for anti-leishmanial activity remains a significant challenge. The purpose of this study is to communicate the design and synthesis strategies of novel chemical compounds based of the arylalkylamine scaffold with selective toxicity towards L. major and less toxicity to human cells in vitro. Here, we have developed a structure activity relationship (SAR) study of arylalkylamine AA1 in order to study their anti-parasitic effect in L. major. Overall, 27 arylalkylamine compounds derived from AA1 were synthesized and purified by silica gel column chromatography. The purity of each analog was confirmed by spectroscopic methods (1H, 13C NMR and LC/MS). Among these analogs, the compound AA9 showed the best toxic activity on L. major (LD50 = 3.34 μM), which represents a 9 fold higher lethality as compared with its parental AA1 (Fer-1) compound (LD50 = 28.75 μM). In addition, AA9 showed no significant toxicity at 80 μM on U20S Human Osteoblasts, Raw 264.7 Macrophages or intraperitoneal macrophages. In summary, our combined SAR study and biological evaluation data of AA1-AA27 compounds allow the identification of novel arylalkylamine compound AA9 that exhibits potent cytotoxicity against L. major promastigote with minimum toxic effect on human cells.

Ferrostatins inhibit oxidative lipid damage and cell death in diverse disease models

Ferrostatin-1 (Fer-1) inhibits ferroptosis, a form of regulated, oxidative, nonapoptotic cell death. We found that Fer-1 inhibited cell death in cellular models of Huntington's disease (HD), periventricular leukomalacia (PVL), and kidney dysfunction; Fer-1 inhibited lipid peroxidation, but not mitochondrial reactive oxygen species formation or lysosomal membrane permeability. We developed a mechanistic model to explain the activity of Fer-1, which guided the development of ferrostatins with improved properties. These studies suggest numerous therapeutic uses for ferrostatins, and that lipid peroxidation mediates diverse disease phenotypes.

COMPOUNDS, COMPOSITIONS, AND METHODS FOR MODULATING FERROPTOSIS AND TREATING EXCITOTOXIC DISORDERS

The present invention provides, inter alia, a compound having the structure: (Formula (I). Also provided are compositions containing a pharmaceutically acceptable carrier and a compound according to the present invention. Further provided are methods for treating or ameliorating the effects of an excitotoxic disorder in a subject, methods of modulating ferroptosis in a subject, methods of reducing reactive oxygen species (ROS) in a cell, and methods for treating or ameliorating the effects of a neurodegenerative disease.

Development of safe one-pot synthesis of N-1- and C-2-substituted benzimidazole via reductive cyclization of o-nitroarylamine using Na 2S2O4

We report that the reductive cyclization of o-nitroarylamine with aldehyde using sodium dithionite (Na2S2O4) could be accelerated by addition of H2O, which made it possible to control the heat release of the reaction by semibatch-type operation. Safety evaluation was performed using DSC, ARSST, in situ IR analysis, and Multimax.

Indazole derivatives as modulators of interleukin-1 receptor-associated kinase

The present invention relates to modulators of IRAK kinases of formula (I) and provides compositions comprising such modulators, as well as methods therewith for treating IRAK-mediated or IRAK-associated conditions or diseases.

Benzimidazole inhibitors of hepatitis C virus NS5B polymerase: Identification of 2-[(4-diarylmethoxy)phenyl]-benzimidazole

A series of 1-cycloalkyl-2-phenyl-1H-benzimidazole-5-carboxylic acid derivatives was synthesized and evaluated for inhibitory activity against HCV NS5B RNA-dependent RNA polymerase (RdRp). A SAR study was performed and led to identify the 2-[(4-diarylmeth

FUSED HETEROCYCLIC COMPOUND HAVING ANTI-HCV EFFECT

Disclosed is a compound represented by the formula (I) below, a pharmaceutically acceptable salt thereof, or a solvate of them. (I) (In the formula, A represents N or CH; Het represents any one of the following groups: (a), (b), (c), (d), (e), (f), (g), (h), (i), (j), (k) wherein R0 and R respectively represent a hydrogen, an optionally substituted alkyl, an optionally substituted cycloalkyl, an optionally substituted aryl or the like; R1 and R2 respectively represent a hydrogen, an optionally substituted alkyl, an optionally substituted alkenyl, an optionally substituted cycloalkyl, an optionally substituted aryl, an optionally substituted heteroaryl or the like; p is an integer of 0-3; and R3 represents an optionally substituted alkyl or the like.)