197435-52-2

Upstream product

• 1692-15-5 4-pyridylboronic acid 
• 131818-17-2 tert-butyl (4-bromophenyl)carbamate 
• 19524-06-2 4-bromopyridine hydrochloride 
• 330793-01-6 (4-tert-butoxycarbonylaminophenyl)boronic acid pinacol ester 
• 106-40-1 4-bromo-aniline 
• 24424-99-5 di-tert-butyl dicarbonate 

Downstream Products

• 928320-12-1 (R)-1-(2-hydroxy-1-phenylethyl)-3-(4-(pyridin-4-yl)phenyl)urea 
• 928320-12-1 AS1892802 
• 1357473-73-4 1-phenethyl-3-(4-(pyridin-4-yl)phenyl)urea 
• 1357473-74-5 (S)-1-(1-hydroxy-3-phenylpropan-2-yl)-3-(4-(pyridin-4-yl)phenyl)urea 
• 1357473-72-3 phenyl 4-(pyridin-4-yl)phenylcarbamate 
• 13296-04-3 4-(pyridin-4-yl)aniline 

Relevant academic research and scientific papers

The synthesis of a rigid conjugated viologen and its cucurbituril pseudorotaxanes

A linear viologen (bis[4-(4-pyridinyl)phenyl] viologen, BPPV) characterized by a fully-conjugated structure was synthesized through Zinke reaction. BPPV consists of a unique linear sexiaryl structure and is apt to be encapsulated by cucurbit[n]uril (CB[n]

INHIBITORS OF RHO ASSOCIATED PROTEIN KINASES (ROCK) AND METHODS OF USE

Compounds and compositions having activity as inhibitors of Rho-associated proteinkinases (ROCKs), and methods of making and using the subject compounds are disclosed.

Fragment-based and structure-guided discovery and optimization of Rho kinase inhibitors

Using high concentration biochemical assays and fragment-based screening assisted by structure-guided design, we discovered a novel class of Rho-kinase inhibitors. Compound 18 was equipotent for ROCK1 (IC50 = 650 nM) and ROCK2 (IC50 = 670 nM), whereas compound 24 was more selective for ROCK2 (IC50 = 100 nM) over ROCK1 (IC50 = 1690 nM). The crystal structure of the compound 18-ROCK1 complex revealed that 18 is a type 1 inhibitor that binds the hinge region in the ATP binding site. Compounds 18 and 24 inhibited potently the phosphorylation of the ROCK substrate MLC2 in intact human breast cancer cells.

Differentiation between partial agonists and neutral 5-HT(1B) antagonists by chemical modulation of 3-[3-(N,N-dimethylamino)propyl]-4- hydroxy-N-[4-(pyridin-4-yl)phenyl]benzamide (GR-55562)

The synthesis and binding affinity at cloned h5-HT(1B), h5-HT(1D), and h5-HT(1A) receptors of 3-[3-(N,N-dimethylamino)propyl]-4-hydroxy-N-[4- (pyridin-4-yl)phenyl]benzamide (2, GR-55562) and four O-methylated analogs are described. The functional activity of these compounds was determined at the h5-HT(1B) receptor using a [35S]GTPγS binding assay. The four analogs have been prepared in order to evaluate the influence of the alkylamino side chain conformation on binding and intrinsic activity. Whereas 2 and its derivatives display a similar binding affinity profile, major differences arise from analysis of the intrinsic activity data at h5-HT(1B) receptors. The O-methylated analog of 2, 3-[3-(N,N-dimethylamino)propyl]-4-methoxy-N- [4-(pyridin-4-yl)phenyl]benzamide (3a), and the (1Z)-3-(N,N- dimethylamino)prop-1-enyl derivative (3c) act as neutral and potent antagonists (in a similar way to 2), while the 3-(N,N-dimethylamino)-prop-1- ynyl (3b) and (1E)-3-(N,N-dimethylamino)prop-1-enyl (3d) analogs display nonnegligible agonist activity. Molecular modeling studies show that, when the common triaryl portions of the molecules are overlapped, the partial agonists and the neutral antagonists differ by a near-orthogonal orientation of the NH+ projection to the hydrogen-bond receptor site.