86922-38-5

Upstream product

• 122-39-4 diphenylamine 
• 42393-65-7 N-(2-chloroethyl)-N-phenylaniline 
• 1074-82-4 potassium phtalimide 

Downstream Products

• 1140-29-0 N-(2-aminoethyl)-N-phenylaniline 
• 86922-19-2 2-Isopropyl-11-oxo-11H-pyrido[2,1-b]quinazoline-8-carboxylic acid (2-diphenylamino-ethyl)-amide 
• 138354-51-5 1-(4-Chloro-phenyl)-3-(2-diphenylamino-ethyl)-urea 

Relevant academic research and scientific papers

DUAL INHIBITORS OF SOLUBLE EPOXIDE HYDROLASE AND 5-LIPOXYGENASE

The invention pertains to a novel structure (I) that provides an activity as a dual inhibitor of the enzymes soluble epoxide hydrolase (sEH) and 5-lipoxygenase (5-LOX). The invention pertains to multiple derivatives of the new class of dual inhibitors, their application in medicine, pharmaceutical compositions comprising them as well as to methods for synthesizing the new compounds.

Design, Synthesis, and Structure-Activity Relationship Studies of Dual Inhibitors of Soluble Epoxide Hydrolase and 5-Lipoxygenase

Inhibition of multiple enzymes of the arachidonic acid cascade leads to synergistic anti-inflammatory effects. Merging of 5-lipoxygenase (5-LOX) and soluble epoxide hydrolase (sEH) pharmacophores led to the discovery of a dual 5-LOX/sEH inhibitor, which was subsequently optimized in terms of potency toward both targets and metabolic stability. The optimized lead structure displayed cellular activity in human polymorphonuclear leukocytes, oral bioavailability, and target engagement in vivo and demonstrated profound anti-inflammatory and anti-fibrotic efficiency in a kidney injury model caused by unilateral ureteral obstruction in mice. These results pave the way for investigating the therapeutic potential of dual 5-LOX/sEH inhibitors in other inflammation- and fibrosis-related disease models.

Reversal agent and linker variants of reversed chloroquines: Activities against Plasmodium falciparum

We have shown that "reversed chloroquine molecules" constructed from chloroquine-like and resistance "reversal-agent"-like cores can be powerful drugs against malaria (J. Med. Chem. 2006, 49, 5623-5625). Several reversed chloroquines are now presented that probe parameters governing the activities against chloroquine-resistant and chloroquine-sensitive malaria strains. The design is tolerant to linker and reversal agent changes, but a piperazinyl group adjacent to the quinoline, at least for the group of compounds studied here, may be detrimental. 2009 American Chemical Society.

Hybrid Cholecystokinin-A Antagonists Based on Molecular Modelling of Lorglumide and L-364,718

A series of novel nonpeptide cholecystokinin-A (CCK-A) antagonists have been synthesized.Designed on the basis of the structural homology between lorgumide and L-364,718, as investigated with molecular modeling, these compounds constitute a link between the N-acylglutamic acid and 3-amino-5-phenyl-1,4-benzodiazepin-2-one derived antagonists.The prepared compounds were tested in vitro as antagonists of the binding of -(+/-)-L-364,718 and -CCK-8(S) to rat pancreas and guinea pig brain membranes, respectively.All compounds proved to be selective for the(peripheral) CCK-A receptor, the most potent analogue, 6, having a Ki value of 90 nM.The structure-activity profile of the series of hybrid compounds relates closest to that of the N-acylglutamic acid derived antagonists.

Antagonists of slow-reacting substance of anaphylaxis. 1. Pyrido[2,1-b]quinazolinecarboxylic acid derivatives

Members of a series of basic amide and ester derivatives of 2-substituted pyrido[2,1-b]quinazoline-8-carboxylic acids were prepared and evaluated for their ability to prevent slow-reacting substance of anaphylaxis (SRS-A) induced contractions of guinea pi