2-Aminothiazole

2-Aminothiazole Structure
2-Aminothiazole structure
Common Name 2-Aminothiazole
CAS Number 96-50-4 Molecular Weight 100.142
Density 1.3±0.1 g/cm3 Boiling Point 216.4±9.0 °C at 760 mmHg
Molecular Formula C3H4N2S Melting Point 91-93 °C(lit.)
MSDS Chinese USA Flash Point 84.7±18.7 °C
Symbol GHS07
GHS07
Signal Word Warning

Quantitative structure-activity relationship and complex network approach to monoamine oxidase A and B inhibitors.

J. Med. Chem. 51 , 6740-51, (2008)

The work provides a new model for the prediction of the MAO-A and -B inhibitor activity by the use of combined complex networks and QSAR methodologies. On the basis of the obtained model, we prepared and assayed 33 coumarin derivatives, and the theoretical pr...

Design, synthesis, and evaluation of potential inhibitors of nitric oxide synthase.

Bioorg. Med. Chem. 16 , 6193-206, (2008)

Selective inhibitors of neuronal nitric oxide synthase (nNOS) were shown to protect brain and may be useful in the treatment of neurodegenerative diseases. In this context, our purpose has been to design and synthesize a new family of derivatives of thiadiazo...

Effects of L-arginine, mirabegron, and oxybutynin on the primary bladder afferent nerve activities synchronized with reflexic, rhythmic bladder contractions in the rat.

Neurourol. Urodyn. 34(4) , 368-74, (2015)

We measured single-unit mechanosensitive afferent activities (SAAs) during reflexic, rhythmic bladder contractions (RBCs), and examined whether L-arginine, an NO substrate, and mirabegron, a β3-adrenoceptor agonist, and oxybutynin, an antimuscarinic agent, ca...

Multicomponent assembly of proposed DNA precursors in water.

J. Am. Chem. Soc. 134(33) , 13889-95, (2012)

We propose a novel pathway for the prebiotic synthesis of 2'-deoxynucleotides. Consideration of the constitutional chemical relationships between glycolaldehyde and β-mercapto-acetaldehyde, and the corresponding proteinogenic amino acids, serine and cysteine,...

A combination strategy to inhibit Pim-1: synergism between noncompetitive and ATP-competitive inhibitors.

ChemMedChem 8(3) , 484-96, (2013)

Pim-1 is a serine/threonine kinase critically involved in the initiation and progression of various types of cancer, especially leukemia, lymphomas and solid tumors such as prostate, pancreas and colon, and is considered a potential drug target against these ...

Antioxidant activity of an aminothiazole compound: possible mechanisms.

Chem. Biol. Interact. 173(3) , 215-23, (2008)

Oceans are among the richest natural sources of many bioactive compounds. Several of these compounds have shown pharmacological activities for many diseases. Dendrodoine (5-[(3-N-dimethylamino)-1,2,4-thiadiazolyl]-3-indanyl methanone) is an alkaloid extracted...

Drug resistance confounding prion therapeutics.

Proc. Natl. Acad. Sci. U. S. A. 110(44) , E4160-9, (2013)

There is not a single pharmaceutical that halts or even slows any neurodegenerative disease. Mounting evidence shows that prions cause many neurodegenerative diseases, and arguably, scrapie and Creutzfeldt-Jakob disease prions represent the best therapeutic t...

Cytochrome P450-mediated epoxidation of 2-aminothiazole-based AKT inhibitors: identification of novel GSH adducts and reduction of metabolic activation through structural changes guided by in silico and in vitro screening.

Chem. Res. Toxicol. 23(3) , 653-63, (2010)

A 2-aminothiazole derivative 1 was developed as a potential inhibitor of the oncology target AKT, a serine/threonine kinase. When incubated in rat and human liver microsomes in the presence of NADPH, 1 underwent significant metabolic activation on its 2-amino...

Allosteric enhancers of A1 adenosine receptors: state of the art and new horizons for drug development.

Curr. Med. Chem. 17(30) , 3488-502, (2010)

Adenosine is an important autocoid, exerting its physiological effects on the human body by activation of four different G-protein-coupled-receptors (GPCRs) classified as A(1), A(2A), A(2B), and A(3). These receptors are coupled to secondary messenger systems...

Development of isoform selective PI3-kinase inhibitors as pharmacological tools for elucidating the PI3K pathway.

Bioorg. Med. Chem. Lett. 22(17) , 5445-50, (2012)

Using a parallel synthesis approach to target a non-conserved region of the PI3K catalytic domain a pan-PI3K inhibitor 1 was elaborated to provide alpha, delta and gamma isoform selective Class I PI3K inhibitors 21, 24, 26 and 27. The compounds had good cellu...