30235-28-0

Usage

Uses

Used in Pharmaceutical Industry:
4-PYRIDIN-4-YL-THIAZOL-2-YLAMINE is used as a synthetic intermediate for the development of pharmaceutical products. Its unique structure and properties make it a valuable component in the synthesis of various drugs, particularly those targeting specific biological pathways or receptors.
As a synthetic intermediate, 4-PYRIDIN-4-YL-THIAZOL-2-YLAMINE can be incorporated into the molecular structure of new drugs, enhancing their efficacy, selectivity, and pharmacokinetic properties. This allows researchers and pharmaceutical companies to develop innovative treatments for a wide range of diseases and conditions.
In addition to its role in drug synthesis, 4-PYRIDIN-4-YL-THIAZOL-2-YLAMINE may also have potential applications in other areas of the pharmaceutical industry, such as drug delivery systems or as a component in the development of prodrugs. Its versatility and unique chemical properties make it a promising candidate for further research and development in the field of pharmaceuticals.

InChI:InChI=1/C8H7N3S/c9-8-11-5-7(12-8)6-1-3-10-4-2-6/h1-5H,(H2,9,11)

Upstream product

• 1122-54-9 methyl (4-pyridyl) ketone 
• 17356-08-0 thiourea 
• 6221-13-2 4-(bromoacetyl)pyridine 
• 5349-17-7 4-bromoacetylpyridine hydrobromide 
• 1701-69-5 1-(4-pyridyl)-1-propanone 
• 53289-47-7 2-chloro-1-pyridin-4-yl-ethanone 

Downstream Products

• 692870-64-7 2-(2-fluorophenyl)-N-(4-pyridin-4-yl-thiazol-2-yl)acetamide 
• 1187669-22-2 N-(3-methylbenzyl)-4-(4-pyridinyl)-1,3-thiazol-2-amine 
• 393839-09-3 4-methoxy-N-[4-(4-pyridinyl)-1,3-thiazol-2-yl]benzamide 
• 476625-88-4 N-[4-(4-pyridinyl)-1,3-thiazol-2-yl]benzamide 
• 476631-30-8 3-methyl-N-[4-(4-pyridinyl)-1,3-thiazol-2-yl]benzamide 
• 476631-28-4 4-methyl-N-[4-(4-pyridinyl)-1,3-thiazol-2-yl]benzamide 
• 1328052-08-9 1-phenyl-3-(4-(pyridin-4-yl)thiazol-2-yl)urea 
• 1342277-11-5 1-(4-fluorophenyl)-3-(4-(pyridin-4-yl)thiazol-2-yl)urea 
• 1342276-58-7 1-benzyl-3-(4-(pyridin-4-yl)thiazol-2-yl)urea 
• 1342276-63-4 1-(4-chlorobenzyl)-3-(4-(pyridin-4-yl)thiazol-2-yl)urea 
• 1342276-92-9 1-(3-fluorobenzyl)-3-(4-(pyridin-4-yl)thiazol-2-yl)urea 
• 1342276-85-0 (R)-1-(1-phenylethyl)-3-(4-(pyridin-4-yl)thiazol-2-yl)urea 
• 1342276-89-4 (S)-1-(1-phenylethyl)-3-(4-(pyridin-4-yl)thiazol-2-yl)urea 
• 1342277-18-2 phenyl 4-(pyridin-4-yl)thiazol-2-ylcarbamate 

Relevant academic research and scientific papers

4-(Pyridin-4-yl)thiazol-2-amine as an efficient non-toxic inhibitor for mild steel in hydrochloric acid solutions

A novel eco-friendly corrosion inhibitor, namely, 4-(pyridin-4-yl)thiazol-2-amine (PTA), was synthesized and evaluated as a corrosion inhibitor for mild steel in 1 M HCl solution. Its inhibition effect against mild steel corrosion was investigated via weight loss methods, electrochemical measurements, and surface analyses. The experimental results showed that PTA is an effective corrosion inhibitor for mild steel in an acid medium, and the maximum inhibition efficiency reached 96.06% at 0.2 mM concentration. Polarization studies showed that PTA acted as a mixed inhibitor. The sorption behavior on the steel surface complies with the Langmuir adsorption isotherm, exhibiting both physisorption and chemisorption. The constitution and characteristic of the protective layer on the steel surface were verified using scanning electron microscopy (SEM)/energy-dispersive X-ray spectroscopy (EDX) and UV-Vis spectroscopy. Quantum chemistry calculations were used to study the relationship between the inhibition efficiency and molecular structure of the inhibitor.

Design and development of novel fasudil derivatives as potent antibreast cancer agent that improves intestinal flora and intestinal barrier function in rats

This study was conducted to develop novel fasudil derivatives after incorporation of substituted thiazoles as potent anti-breast cancer (BC) agents. The compounds were developed using a facile synthetic route in excellent yields. The entire set of developed compounds was tested for inhibitory activity against rho-associated coiled-coil kinase (ROCK; ROCK1 and ROCK2) kinase, where they exhibit potent and selective inhibition of ROCK1 as compared to ROCK2. The most potent ROCK2 inhibitor, compound 6h significantly inhibited the viability of BC cells (MCF-7). It also causes inhibition of migration and invasion of MCF-7 cells. Moreover, the anti-BC activity of compound 6h was studied in 7,12 dimethyl Benz(a)anthracene (DMBA)-induced BC in female Sprague Dawley rats. Results suggest that it causes significant improvement in the bodyweight of the animals with a reduction in oxidative stress in the liver and mammary tissues of rats. It showed improvement in the intestinal barrier function of rats by restoring the level of Diamine oxidase, d-lactate, and endotoxin. In western blot analysis, it showed improvement in (ZO-1), occludin, and claudin-1 in the colon tissue of the rat as compared to the DMBA group. Our study demonstrated the development of the novel class of fasudil derivatives potent anti-BC agent that improves intestinal flora and intestinal barrier function in rats.

Design, synthesis, and biological evaluation of urea-based ROCK2 inhibitors

A series of urea-based ROCK2 inhibitors were design and synthesized. The inhibitory activity on ROCK2 was screened by enzyme-linked immunosorbent assay (ELISA). The study results showed that the urea derivatives exhibited certain ROCK2 inhibitory activity. The most potent compound 10p showed ROCK2 inhibitory activity with the IC50?value of 0.03?μM. A preliminary structure-activity relationship was then summarized. The molecular docking studies showed that further optimization needs to conduct to obtain more potent ROCK inhibitors.

Design, synthesis and biological evaluation of 4-aryl-5-aminoalkyl-thiazole-2-amines derivatives as ROCK II inhibitors

A series of 4-aryl-5-aminoalkyl-thiazole-2-amines were designed and synthesized, and their inhibitory activity on ROCK II was screened by enzyme-linked immunosorbent assay (ELISA). The results showed that 4-aryl-5-aminomethyl-thiazole-2-amines derivatives had certain ROCK II inhibitory activities. Compound 10l showed ROCK II inhibitory activity with IC50 value of 20 nM.

SUBSTITUTED AMINOTHIAZOLES AS INHIBITORS OF NUCLEASES

The invention provides compounds represented by the structural formula (1): wherein R1, R2, R3, R4, R5, R6 are as defined in the claims. The compounds are inhibitors of nucleases, and are useful in particular in a method of treatment and/or prevention of proliferative diseases, neurodegenerative diseases, and other genomic instability associated diseases.

Novel tri-substituted thiazoles bearing piperazine ring: Synthesis and evaluation of their anticancer activity

Background: Cancer cells are described as an unregulated growth and spread of abnormal cells. Recently, cancer has become the most important major reason for deaths in the world. Methods: For anticancer activity, we have used the MTT method and determine

Design, Synthesis, and Structure-Activity Relationships of Pyridine-Based Rho Kinase (ROCK) Inhibitors

The Rho kinases (ROCK1 and ROCK2) are highly homologous serine/threonine kinases that act on substrates associated with cellular motility, morphology, and contraction and are of therapeutic interest in diseases associated with cellular migration and contraction, such as hypertension, glaucoma, and erectile dysfunction. Beginning with compound 4, an inhibitor of ROCK1 identified through high-throughput screening, systematic exploration of SAR, and application of structure-based design, led to potent and selective ROCK inhibitors. Compound 37 represents significant improvements in inhibition potency, kinase selectivity, and CYP inhibition and possesses pharmacokinetics suitable for in vivo experimentation.

BENZIMIDAZOLE DERIVATIVES AS SELECTIVE PROTEINE KINASE INHIBITORS

The present invention relates to compounds of formula (I) or pharmaceutically acceptable salts thereof. Wherein n, R1, R2, R3, R4, R5, A, Q and X are as defined in the description. These compounds selectively modulate, regulate, and/or inhibit signal transduction mediated by certain native and/or mutant proteine kinases implicated in a variety of human and animal diseases such as cell proliferative, metabolic, allergic, and degenerative disorders. More particularly, these compounds are potent and selective native and/or mutant c-kit inhibitors.

Synthesis and biological evaluation of 2-aminothiazole derivatives as antimycobacterial and antiplasmodial agents

A series of compounds derived from the 2-amino-4-(2-pyridyl) thiazole scaffold was synthesized and tested for in vitro antimycobacterial activity against the Mycobacterium tuberculosis H37Rv strain, antiplasmodial activity against the chloroquine sensitive NF54 Plasmodium falciparum strain and cytotoxicity on a mammalian cell line. Optimal antimycobacterial activity was found with compounds with a 2-pyridyl ring at position 4 of the thiazole scaffold, a substituted phenyl ring at the 2-amino position, and an amide linker between the scaffold and the substituted phenyl. The antiplasmodial activity was best with compounds that had the phenyl ring substituted with hydrophobic electron withdrawing groups.

Pyridylthiazole-based ureas as inhibitors of Rho associated protein kinases (ROCK1 and 2)

Potent ROCK inhibitors of a new class of 1-benzyl-3-(4-pyridylthiazol-2-yl) ureas have been identified. Remarkable differences in activity were observed for ureas bearing a benzylic stereogenic center. Derivatives with hydroxy, methoxy and amino groups at the meta position of the phenyl ring give rise to the most potent inhibitors (low nM). Substitutions at the para position result in substantial loss of potency. Changes at the benzylic position are tolerated resulting in significant potency in the case of methyl and methylenehydroxy groups. X-Ray crystallography was used to establish the binding mode of this class of inhibitors and provides an explanation for the observed differences of the enantiomer series. Potent inhibition of ROCK in human lung cancer cells was shown by suppression of the levels of phosphorylation of the ROCK substrate MYPT-1.