21278-86-4

Basic information

• Product Name: 2-(4-PYRIDYL)THIAZOLE-4-CARBOXYLIC ACID
• Synonyms: AKOS BBS-00003760;2-(4-PYRIDYL)THIAZOLE-4-CARBOXYLIC ACID;2-(4-PYRIDYL)-1,3-THIAZOLE-4-CARBOXYLIC ACID;2-(4-PYRIDINYL)-1,3-THIAZOLE-4-CARBOXYLIC ACID;2-PYRIDIN-4-YL-THIAZOLE-4-CARBOXYLIC ACID;BUTTPARK 99\12-12;2-(Pyridin-4-yl)-1,3-thiazole-4-carboxylic acid;4-Carboxy-2-(pyridin-4-yl)-1,3-thiazole, 4-(4-Carboxy-1,3-thiazol-2-yl)pyridine
• CAS NO: 21278-86-4
• Molecular Formula: C₉H₆N₂O₂S
• Molecular Weight: 206.22
• Product Categories: Carboxylic Acids;Thiazoles, Isothiazoles &Benzothiazoles;Heterocyclic Compounds;Carboxylic Acids;Thiazoles, Isothiazoles & Benzothiazoles;Building Blocks;Heterocyclic Building Blocks;Thiazoles;Building Blocks;C8 to C9;Chemical Synthesis;Heterocyclic Building Blocks
• Mol File: 21278-86-4.mol
• Article Data: 5

Chemical Properties

• Melting Point: >300 °C(lit.)
• Boiling Point: 469.3 °C at 760 mmHg
• Flash Point: 237.6 °C
• Appearance: /
• Density: 1.44 g/cm³
• Vapor Pressure: 1.31E-09mmHg at 25°C
• PKA: 3.25±0.10(Predicted)
• Water Solubility: Insoluble in water.
• CAS DataBase Reference: 2-(4-PYRIDYL)THIAZOLE-4-CARBOXYLIC ACID(CAS DataBase Reference)
• NIST Chemistry Reference: 2-(4-PYRIDYL)THIAZOLE-4-CARBOXYLIC ACID(21278-86-4)
• EPA Substance Registry System: 2-(4-PYRIDYL)THIAZOLE-4-CARBOXYLIC ACID(21278-86-4)

Safety Data

• Hazard Codes: Xn
• Statements: 22-36/37/38
• Safety Statements: 26-36
• WGK Germany: 3
• HazardClass: IRRITANT
• Hazardous Substances Data: 21278-86-4(Hazardous Substances Data)

Usage

Uses

2-(4-Pyridyl)thiazole-4-carboxylic acid, is used as pharmaceutical intermediate and also used in the field of organic synthesis.

InChI:InChI=1/C9H6N2O2S/c12-9(13)7-5-14-8(11-7)6-1-3-10-4-2-6/h1-5H,(H,12,13)/p-1

Upstream product

• 1113-59-3 bromopyruvic acid 
• 2196-13-6 pyridine-4-carbothioamide 
• 21278-85-3 ethyl 2-(4-pyridyl)-1,3-thiazole-4-carboxylate 

Downstream Products

• 1620222-82-3 N-(4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl)-2-(pyridin-4-yl)thiazole-4-carboxamide 
• 1093255-39-0 N-({4-chloro-3-[(3-chloro-5-cyanophenyl)oxy]-2-fluorophenyl}methyl)-2-(4-pyridinyl)-1,3-thiazol-4-carboxamide trifluoroacetate 
• 854399-38-5 (S)-2-{(S)-3-(tert-Butyl-diphenyl-silanyloxy)-2-[(2-pyridin-4-yl-thiazole-4-carbonyl)-amino]-propionylamino}-3-hydroxy-propionic acid methyl ester 
• 854399-27-2 3-(tert-butyl-diphenyl-silanyloxy)-2-[(2-pyridin-4-yl-thiazole-4-carbonyl)-amino]-propionic acid 

Relevant articles and documents

Discovery of Novel Aryl Carboxamide Derivatives as Hypoxia-Inducible Factor 1α Signaling Inhibitors with Potent Activities of Anticancer Metastasis

In order to discover novel hypoxia-inducible factor 1 (HIF-1) inhibitors for the cancer metastasis treatment, 68 new aryl carboxamide compounds were synthesized and evaluated for their inhibitory effect by dual luciferase-reporter assay. Based on five rounds of investigation on structure-activity relationships step by step, compound 30m was discovered as the most active inhibitor (IC50 = 0.32 μM) with no obvious cytotoxicity (CC50 > 50 μM). It effectively attenuated hypoxia-induced HIF-1α protein accumulation and reduced transcription of vascular epidermal growth factor in a dose-dependent manner, which was further demonstrated by its inhibitory potency on capillary-like tube formation, angiogenesis of zebrafish as well as cellular migration and invasion. Importantly, compound 30m exhibited antimetastatic potency in breast cancer lung metastasis in the mice model, indicating its promising therapeutic potential for prevention and treatment of tumor metastasis. These results definitely merit attention for further rational design of more efficient HIF-1 inhibitors in the future.

COMPOSITIONS USEFUL AS INHIBITORS OF ROCK AND OTHER PROTEIN KINASES

The present invention relates to substitute thiazole and thiophene derivatives useful as inhibitors of rock and other protein kinaeses. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders, including proliferative, cardiac and neurodegenerative diseases.

Sulfonamide derivatives, their production and use

The present invention provides compounds which specifically inhibit FXa, which are effective when orally administered and which are useful as a safe medicine for the prevention or treatment of diseases caused by thrombus or infarction. Compounds of this invention are piperazinones of the formula: wherein R1is an optionally substituted hydrocarbon group or an optionally substituted heterocyclic group; the ring A is an optionally substituted divalent nitrogen-containing heterocyclic group, in addition to being substituted by the group of the formula: and the group of the formula: Y is an optionally substituted divalent hydrocarbon group or an optionally substituted divalent heterocyclic group; X is a direct bond or an optionally substituted alkylene chain; Z is (1) an amino group substituted with an optionally substituted hydrocarbon group, (2) an optionally substituted imino group or (3) an optionally substituted nitrogen-containing heterocyclic group; provided that when X is a direct bond and Z is an optionally substituted 6-membered nitrogen-containing aromatic heterocyclic group, Y is an optionally substituted divalent hydrocarbon group or an optionally substituted divalent unsaturated heterocyclic group; or a salt thereof.