150302-19-5

Usage

Derivative of

Thiophene

Functional Groups

Amino group ( -\textNH2 )
Phenyl group ( -\textC6\textH5 )

Potential Applications

Medicinal chemistry
Pharmaceuticals

Biological Targets

Enzymes, receptors

Biological Activities

Antimicrobial
Antifungal
Anticancer

Research Focus

Drug development
Scientific applications

Upstream product

• 122-78-1 phenylacetaldehyde 
• 107-91-5 cyanoacetic acid amide 
• 98-86-2 acetophenone 

Relevant academic research and scientific papers

MgO-CeO2 nanocomposite: efficient catalyst for the preparation of 2-aminothiophenes and thieno[2,3-d]pyrimidin-4(3H)-one derivatives

MgO-CeO2 nanocomposite was prepared by a co-precipitation method and characterized by X-ray diffraction (XRD), FE-SEM, and particle size distribution analysis. The XRD pattern shows the cubic phase of cerium oxide as the dominate phase. FE-SEM images show the homogeneity distribution of magnesium and cerium oxides in the sample. The mean particle size of nanocomposite determined by the dynamic light scattering technique is 66 nm. The catalytic activity of MgO-CeO2 nanocomposite was examined on the synthesis of 2-aminothiophenes and thieno[2,3-d]pyrimidin-4(3H)-one derivatives. In all cases, products were obtained in good to excellent yields.

Structure–activity relationships for inhibitors of Pseudomonas aeruginosa exoenzyme S ADP-ribosyltransferase activity

During infection, the Gram-negative opportunistic pathogen Pseudomonas aeruginosa employs its type III secretion system to translocate the toxin exoenzyme S (ExoS) into the eukaryotic host cell cytoplasm. ExoS is an essential in vivo virulence factor that enables P. aeruginosa to avoid phagocytosis and eventually kill the host cell. ExoS elicits its pathogenicity mainly via ADP-ribosyltransferase (ADPRT) activity. We recently identified a new class of ExoS ADPRT inhibitors with in vitro IC50 of around 20 μM in an enzymatic assay using a recombinant ExoS ADPRT domain. Herein, we report structure–activity relationships of this compound class by comparing a total of 51 compounds based on a thieno [2,3-d]pyrimidin-4(3H)-one and 4-oxo-3,4-dihydroquinazoline scaffolds. Improved inhibitors with in vitro IC50 values of 6 μM were identified. Importantly, we demonstrated that the most potent inhibitors block ADPRT activity of native full-length ExoS secreted by viable P. aeruginosa with an IC50 value of 1.3 μM in an enzymatic assay. This compound class holds promise as starting point for development of novel antibacterial agents.