297756-32-2

Usage

Class

Carboxylic acid esters

Derivative

Benzimidazole

Usage

Organic synthesis and pharmaceutical research

Pharmacological properties

Antiparasitic, anti-cancer, and anti-inflammatory activities

Potential

Drug candidate for the treatment of various diseases

Ester group

1,1-dimethylethyl ester (provides stability and enhances biological activity)

Upstream product

• 94-52-0 5-nitrobenzimidazole 
• 24424-99-5 di-tert-butyl dicarbonate 
• 934-22-5 5-aminobenzimidazole 
• 94-52-0 6-nitro-1H-benzo[d]imidazole 
• 1425932-17-7 tert-butyl 5-nitro-1H-benzo[d]imidazole-1-carboxylate 
• 1442459-46-2 tert-butyl 6-nitro-1H-benzo[d]imidazole-1-carboxylate 

Downstream Products

• 1098591-99-1 C₂₉H₃₇N₃O₅ 

Relevant academic research and scientific papers

CONJUGATED PROTEINS AND USES THEREOF

Disclosed herein, in certain embodiments, are protein-probe adducts and synthetic ligands that inhibit protein-probe adduct formation, in which the proteins are regulated by NRF2. In some instances, also described herein are protein-binding domains that interact with a probe and/or a ligand described herein, in which the proteins are regulated by NRF2.

Structure-activity relationship of human glutaminyl cyclase inhibitors having an N-(5-methyl-1H-imidazol-1-yl)propyl thiourea template

In an effort to design inhibitors of human glutaminyl cyclase (QC), we have synthesized a library of N-aryl N-(5-methyl-1H-imidazol-1-yl)propyl thioureas and investigated the contribution of the aryl region of these compounds to their structure-activity relationships as cyclase inhibitors. Our design was guided by the proposed binding mode of the preferred substrate for the cyclase. In this series, compound 52 was identified as the most potent QC inhibitor with an IC50 value of 58 nM, which was two-fold more potent than the previously reported lead 2. Compound 52 is a most promising candidate for future evaluation to monitor its ability to reduce the formation of pGlu-Aβ and Aβ plaques in cells and transgenic animals.

1, 3, 4-BENZOTRIAZEPIN-2-ONE SALTS AND THEIR USE AS CCK RECEPTOR LIGANDS

This invention relates to pharmaceutically acceptable salts of compounds of formula (I) wherein: W is N or N+-O-; R2 is an optionally substituted C1 to C18 hydrocarbyl group wherein up to three C atoms may optionally be replaced by N, O and/or S atoms. R3 is -(CR11R12)m-X-(CR13R14)p-R9; m is 0, 1, 2, 3 or 4; p is 0, 1 or 2; X is a bond, -CR15=CR16-, -C≡C-, C(O)NH, NHC(O), C(O)NMe, NMeC(O), C(O)O, NHC(O)NH, NHC(O)O, OC(O)NH, NH, O, CO, SO2, SO2NH, C(O)NHNH, R9 is H ; C1 to C6 alkyl ; or phenyl, naphthyl, pyridyl, benzimidazolyl, indazolyl, quinolinyl, isoquinolinyl, tetrahydroisoquinolinyl, indolinyl, isoindolinyl, indolyl, isoindolyl or 2-pyridonyl substituted with -L-Q. R4 is an optionally substituted C1 to C18 hydrocarbyl group wherein up to three C atoms may optionally be replaced by N, O and/or S atoms ; and Such salts are useful, for example, for the treatment of gastrin related disorders.

Neutrophil inhibitors to reduce inflammatory response

The invention provides novel compounds selected from the group consisting of: The compounds of the present invention are useful for the treatment and prevention of a variety of diseases and conditions associated with undesirable or abnormal inflammatory responses, such as ischemia-reperfusion injury. Accordingly, the invention further provides pharmaceutical compositions comprising these compounds. The invention still further provides methods of treatment or prevention for the above disorders using theses compounds or the compositions containing them.

3-(anilinomethylene) oxindoles

The present invention relates generally to novel amine substituted oxindole compounds and compositions. Such compounds and compositions have utility as pharmacological agents in treating diseases or conditions alleviated by the inhibition or antagonism of