Category: 144060-99-1

Darekar, N. R. published the artcileMicrowave Assisted Synthesis and Antibacterial Activity of New 1,3,4-Thiadiazoles and 1,2,4-Triazoles Derived from 2-{2-[2-(4-Fluorophenyl)-4-methylthiazol-5-yl]-1H-benzo[d]imidazol-1-yl}acetohydrazide, Recommanded Product: 2-(4-Fluorophenyl)-4-methylthiazole-5-carboxylic acid, the main research area is phenyl fluorophenyl methylthiazolyl benzoimidazolyl acetyl thiosemicarbazide preparation antibacterial; methyl phenyl fluorophenyl methylthiazolyl benzoimidazolyl triazole thiol preparation antibacterial; fluorophenyl methylthiazolyl benzoimidazolyl methyl phenyl thiadiazol amine preparation antibacterial; microwave irradiation.

A series of novel derivatives of 1-(2-{2-[2-(4-fluorophenyl)-4-methylthiazol-5-yl]-1H-benzo[d]imidazol-1-yl}acetyl)-4-phenylthiosemicarbazide, 5-({2-[2-(4-fluorophenyl)-4-methylthiazol-5-yl]-1H-benzo[d]imidazol-1-yl}methyl)-4-phenyl-4H-1,2,4-triazole-3-thiol and 5-({2-[2-(4-fluorophenyl)-4-methylthiazol-5-yl]-1H-benzo[d]imidazol-1-yl}methyl)-N-phenyl-1,3,4-thiadiazol-2-amine was synthesized by the conventional method as well as using MW irradiation All newly synthesized compounds were tested for antibacterial activity. Several products were demonstrated moderate activity against gram pos. and gram neg. bacterial strains.

Russian Journal of General Chemistry published new progress about Antibacterial agents. 144060-99-1 belongs to class thiazole, name is 2-(4-Fluorophenyl)-4-methylthiazole-5-carboxylic acid, and the molecular formula is C11H8FNO2S, Recommanded Product: 2-(4-Fluorophenyl)-4-methylthiazole-5-carboxylic acid.

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica

Zhang, Qian published the artcileDiscovery of Triazolo-pyridazine/-pyrimidine Derivatives Bearing Aromatic (Heterocycle)-Coupled Azole Units as Class II c-Met Inhibitors, Application In Synthesis of 144060-99-1, the main research area is triazolopyridazine triazolopyrimidine preparation cMet kinase inhibition SAR anticancer human.

Two series of novel triazolo-pyridazine/-pyrimidine derivatives were designed, synthesized, and evaluated for their inhibitory activity against c-Met kinase, as well as three c-Met overexpressed cancer cell lines (A549, MCF-7, and HeLa) and one normal human hepatocytes cell line LO2 in vitro. The most promising compound I exhibited significant cytotoxicity against A549, MCF-7, and HeLa cell lines with IC50 values of 1.06 +/- 0.16, 1.23 +/- 0.18, and 2.73 +/- 0.33μM, resp. Moreover, the inhibitory activity of compound I against c-Met kinase (IC50 = 0.090μM) was equal to that of Foretinib (IC50 = 0.019μM). The result of the acridine orange single staining test demonstrated that compound I could remarkably induce apoptosis of A549 cells. The results of apoptosis and cycle distribution of cells showed that compound I could induce late apoptosis of A549 cells and stimulate A549 cells arresting in the G0/G1 phase. Structure-activity relationships (SARs), pharmacol. results, and docking studies indicated that the introduction of 5-methylthiazole fragment to the five-atom moiety was beneficial for the activity. So far, the existing data indicated that I may become a potential class II c-Met inhibitor.

ACS Omega published new progress about Antitumor agents. 144060-99-1 belongs to class thiazole, name is 2-(4-Fluorophenyl)-4-methylthiazole-5-carboxylic acid, and the molecular formula is C11H8FNO2S, Application In Synthesis of 144060-99-1.

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica

Nomura, Masahiro published the artcileDiscovery of cyclic amine-substituted benzoic acids as PPARα agonists, Product Details of C11H8FNO2S, the main research area is benzoic acid cyclic amine substituted preparation SAR PPAR agonist.

A series of novel cyclic amine-substituted benzoic acid derivatives was synthesized and evaluated for PPARα agonist activity. Structure-activity relationship studies led to the identification of (S)-3-[3-[2-(4-chlorophenyl)-4-methylthiazole-5-carboxamido]piperidin-1-yl]benzoic acid (I) (KRP-105) as a potent and high subtype-selective human PPARα agonist. I showed excellent PK profile, and oral administration of I to high-fat diet dogs effectively lowered triglycerides.

Bioorganic & Medicinal Chemistry Letters published new progress about Cyclic amines Role: PAC (Pharmacological Activity), PKT (Pharmacokinetics), RCT (Reactant), SPN (Synthetic Preparation), THU (Therapeutic Use), BIOL (Biological Study), RACT (Reactant or Reagent), PREP (Preparation), USES (Uses). 144060-99-1 belongs to class thiazole, name is 2-(4-Fluorophenyl)-4-methylthiazole-5-carboxylic acid, and the molecular formula is C11H8FNO2S, Product Details of C11H8FNO2S.

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica

Liu, Xiaobo published the artcileDesign, synthesis, and biological evaluation of [1,2,4]triazolo[4,3-a] pyrazine derivatives as novel dual c-Met/VEGFR-2 inhibitors, Synthetic Route of 144060-99-1, the main research area is triazolopyrazine preparation antitumor activity apoptosis hemolytic toxicity mol docking; antiproliferative activity; antitumor; c-Met inhibitor; pyrazine derivatives; targeted drug.

In this study, a series of novel [1,2,4]triazolo[4,3-a]pyrazine derivatives, I (R = 4-methyl-2-phenyl-1,3-thiazol-5-yl, 4-(4-methyl-1,3-thiazol-2-yl)pyridine, 3-(thiophen-2-yl)-1H-pyrazol-5-yl, etc.; R1 = H, Me; X = H, F) evaluated for their inhibitory activities toward c-Met/VEGFR-2 kinases and antiproliferative activities against tested three cell lines in vitro was designed and synthesized. Most of the compounds I showed satisfactory activity compared with lead compound foretinib. Among them, the most promising compound I (R = 1-(4-chlorophenyl)-5-(trifluoromethyl)-1H-pyrazol-4-yl, R1 = Me; X = F) (II) exhibited excellent antiproliferative activities against A549, MCF-7, and Hela cancer cell lines with IC50 values of 0.98 ± 0.08, 1.05 ± 0.17, and 1.28 ± 0.25μM, resp., as well as excellent kinase inhibitory activities (c-Met IC50 = 26.00 nM and VEGFR-2 IC50 = 2.6μM). Moreover, compound II inhibited the growth of A549 cells in G0/G1 phase in a dose-dependent manner, and induced the late apoptosis of A549 cells. Its intervention on intracellular c-Met signaling of A549 was verified by the result of Western blot. Fluorescence quant. PCR showed that compound 17l inhibited the growth of A549 cells by inhibiting the expression of c-Met and VEGFR-2, and its hemolytic toxicity was low. Mol. docking and mol. dynamics simulation indicated that compound II could bind to c-Met and VEGFR-2 protein, which was similar to that of foretinib.

Frontiers in Chemistry (Lausanne, Switzerland) published new progress about Acids Role: RCT (Reactant), RACT (Reactant or Reagent). 144060-99-1 belongs to class thiazole, name is 2-(4-Fluorophenyl)-4-methylthiazole-5-carboxylic acid, and the molecular formula is C11H8FNO2S, Synthetic Route of 144060-99-1.

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica

Sierra, Michael L. published the artcileSubstituted 2-[(4-Aminomethyl)phenoxy]-2-methylpropionic Acid PPARα Agonists. 1. Discovery of a Novel Series of Potent HDLc Raising Agents, Application In Synthesis of 144060-99-1, the main research area is arylmethylpropionic acid derivative SAR preparation PPAR agonist HDLc raising.

The peroxisome proliferator activated receptors PPARα, PPARγ, and PPARδ are ligand-activated transcription factors that play a key role in lipid homeostasis. The fibrates raise circulating levels of high-d. lipoprotein cholesterol and lower levels of triglycerides in part through their activity as PPARα agonists; however, the low potency and restricted selectivity of the fibrates may limit their efficacy, and it would be desirable to develop more potent and selective PPARα agonists. Modification of the selective PPARδ agonist 1 (GW501516) so as to incorporate the 2-aryl-2-methylpropionic acid group of the fibrates led to a marked shift in potency and selectivity toward PPARα agonism. Optimization of the series gave 25a, which shows EC50 = 4 nM on PPARα and at least 500-fold selectivity vs. PPARδ and PPARγ. Compound 25a (GW590735) has been progressed to clin. trials for the treatment of diseases of lipid imbalance.

Journal of Medicinal Chemistry published new progress about Lipid metabolism disorders Role: BIOL (Biological Study). 144060-99-1 belongs to class thiazole, name is 2-(4-Fluorophenyl)-4-methylthiazole-5-carboxylic acid, and the molecular formula is C11H8FNO2S, Application In Synthesis of 144060-99-1.

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica

Protopopov, Mykola V. published the artcileIdentification of 1,3-thiazole-5-carboxylic Acid Derivatives as Inhibitors of Protein Kinase CK2, Safety of 2-(4-Fluorophenyl)-4-methylthiazole-5-carboxylic acid, the main research area is protein kinase thiazole carboxylic acid CK inhibitor.

Serine/threonine protein kinase CK2 is involved in the regulation of a number of cellular functions such as cell growth, proliferation, differentiation and apoptosis. Increased activity of CK2 is associated with the development of different types of cancer, inflammatory response, pain and virus infections. Therefore, protein kinase CK2 is an attractive mol. target for the development of small-mol. inhibitors which can be important compounds for pharmaceutical application. The main aim of this research is to identify novel chem. class of CK2 inhibitors with good lead-like properties. In order to find novel CK2 inhibitors, virtual screening experiments were performed using Autodock software. Best-scored compounds were tested in vitro using P32 radioactive kinase assay. Small-mol. inhibitors of protein kinase CK2 were identified among the derivatives of 1,3-thiazole-5-carboxylic acid. The most active compound inhibited CK2 with IC50 value of 0.4 μM. Ligand efficiency for studied derivatives of 1,3-thiazole-5-carboxylic acid was in the range from 0.45 to 0.56 kcal/mol/non-hydrogen atom. Considering the fact that the lower limit for ligand efficiency parameter is 0.3, the identified CK2 inhibitors among the derivatives of 1,3-thiazole-5-carboxylic acid are excellent candidates for further lead optimization.

Current Enzyme Inhibition published new progress about Amino acids Role: BSU (Biological Study, Unclassified), BIOL (Biological Study). 144060-99-1 belongs to class thiazole, name is 2-(4-Fluorophenyl)-4-methylthiazole-5-carboxylic acid, and the molecular formula is C11H8FNO2S, Safety of 2-(4-Fluorophenyl)-4-methylthiazole-5-carboxylic acid.

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica

144060-99-1, Name is 2-(4-Fluorophenyl)-4-methylthiazole-5-carboxylic acid, molecular formula is C11H8FNO2S, belongs to thiazole compound, is a common compound. In a patnet, once mentioned the new application about 144060-99-1, Safety of 2-(4-Fluorophenyl)-4-methylthiazole-5-carboxylic acid

The invention relates to a novel 2-phenylthiazole-5-methanamide compound shown as a general formula I, a precursor, a stereo isomer and physiologically-acceptable salt thereof, a medicinal composition containing the compound, and an application of the compound as the aspect of medicine.

Balanced chemical reaction does not necessarily reveal either the individual elementary reactions by which a reaction occurs or its rate law.Safety of 2-(4-Fluorophenyl)-4-methylthiazole-5-carboxylic acid. In my other articles, you can also check out more blogs about 144060-99-1

Reference：
Thiazole | C3H580NS – PubChem,
Thiazole | chemical compound | Britannica

144060-99-1, Name is 2-(4-Fluorophenyl)-4-methylthiazole-5-carboxylic acid, molecular formula is C11H8FNO2S, belongs to thiazole compound, is a common compound. In a patnet, once mentioned the new application about 144060-99-1, Application In Synthesis of 2-(4-Fluorophenyl)-4-methylthiazole-5-carboxylic acid

Substituted 2-[(4-aminomethyl)phenoxy]-2-methylpropionic acid PPARalpha agonists. 1. Discovery of a novel series of potent HDLc raising agents

The peroxisome proliferator activated receptors PPARalpha, PPARgamma, and PPARdelta are ligand-activated transcription factors that play a key role in lipid homeostasis. The fibrates raise circulating levels of high-density lipoprotein cholesterol and lower levels of triglycerides in part through their activity as PPARalpha agonists; however, the low potency and restricted selectivity of the fibrates may limit their efficacy, and it would be desirable to develop more potent and selective PPARalpha agonists. Modification of the selective PPARdelta agonist 1 (GW501516) so as to incorporate the 2-aryl-2-methylpropionic acid group of the fibrates led to a marked shift in potency and selectivity toward PPARalpha agonism. Optimization of the series gave 25a, which shows EC50 = 4 nM on PPARalpha and at least 500-fold selectivity versus PPARgamma and PPARgamma. Compound 25a (GW590735) has been progressed to clinical trials for the treatment of diseases of lipid imbalance.

Balanced chemical reaction does not necessarily reveal either the individual elementary reactions by which a reaction occurs or its rate law.Application In Synthesis of 2-(4-Fluorophenyl)-4-methylthiazole-5-carboxylic acid. In my other articles, you can also check out more blogs about 144060-99-1

Reference：
Thiazole | C3H579NS – PubChem,
Thiazole | chemical compound | Britannica

144060-99-1, Name is 2-(4-Fluorophenyl)-4-methylthiazole-5-carboxylic acid, molecular formula is C11H8FNO2S, belongs to thiazole compound, is a common compound. In a patnet, once mentioned the new application about 144060-99-1, Application In Synthesis of 2-(4-Fluorophenyl)-4-methylthiazole-5-carboxylic acid

Substituted 2-[(4-aminomethyl)phenoxy]-2-methylpropionic acid PPARalpha agonists. 1. Discovery of a novel series of potent HDLc raising agents

The peroxisome proliferator activated receptors PPARalpha, PPARgamma, and PPARdelta are ligand-activated transcription factors that play a key role in lipid homeostasis. The fibrates raise circulating levels of high-density lipoprotein cholesterol and lower levels of triglycerides in part through their activity as PPARalpha agonists; however, the low potency and restricted selectivity of the fibrates may limit their efficacy, and it would be desirable to develop more potent and selective PPARalpha agonists. Modification of the selective PPARdelta agonist 1 (GW501516) so as to incorporate the 2-aryl-2-methylpropionic acid group of the fibrates led to a marked shift in potency and selectivity toward PPARalpha agonism. Optimization of the series gave 25a, which shows EC50 = 4 nM on PPARalpha and at least 500-fold selectivity versus PPARgamma and PPARgamma. Compound 25a (GW590735) has been progressed to clinical trials for the treatment of diseases of lipid imbalance.

Balanced chemical reaction does not necessarily reveal either the individual elementary reactions by which a reaction occurs or its rate law.Application In Synthesis of 2-(4-Fluorophenyl)-4-methylthiazole-5-carboxylic acid. In my other articles, you can also check out more blogs about 144060-99-1

Reference：
Thiazole | C3H579NS – PubChem,
Thiazole | chemical compound | Britannica

The reaction rate of a catalyzed reaction is faster than the reaction rate of the uncatalyzed reaction at the same temperature.144060-99-1, Name is 2-(4-Fluorophenyl)-4-methylthiazole-5-carboxylic acid, molecular formula is C11H8FNO2S. In a Patent£¬once mentioned of 144060-99-1, Product Details of 144060-99-1

A novel heterocyclic compound or a salt thereof useful for selectively inhibiting the degradation of p27Kip1 is provided. The compound or the salt thereof is represented by the following formula (1): wherein A represents an alkyl group, a cycloalkyl group, an aryl group or a heterocyclic group, the group A may have a substituent; the ring B represents a 5- to 8-membered monocyclic heterocyclic ring or a condensed ring containing the monocyclic heterocyclic ring, the ring B may have a substituent; the ring C represents an aromatic ring, the ring C may have a substituent; L represents a linker comprising a main chain having 3 to 5 atoms selected from the group consisting of a carbon atom, a nitrogen atom, an oxygen atom and a sulfur atom, wherein at least one atom in the main chain is a hetero atom selected from the group consisting of a nitrogen atom, an oxygen atom and a sulfur atom, the linker L may have a substituent; and n is 0 or 1.

A novel heterocyclic compound or a salt thereof useful for selectively inhibiting the degradation of p27Kip1 is provided. The compound or the salt thereof is represented by the following formula (1): wherein A represents an alkyl group, a cycloalkyl group, an aryl group or a heterocyclic group, the group A may have a substituent; the ring B represents a 5- to 8-membered monocyclic heterocyclic ring or a condensed ring containing the monocyclic heterocyclic ring, the ring B may have a substituent; the ring C represents an aromatic ring, the ring C may have a substituent; L represents a linker comprising a main chain having 3 to 5 atoms selected from the group consisting of a carbon atom, a nitrogen atom, an oxygen atom and a sulfur atom, wherein at least one atom in the main chain is a hetero atom selected from the group consisting of a nitrogen atom, an oxygen atom and a sulfur atom, the linker L may have a substituent; and n is 0 or 1.

The reactant in an enzyme-catalyzed reaction is called a substrate. Enzyme inhibitors cause a decrease in the reaction rate of an enzyme-catalyzed reaction.I hope my blog about 144060-99-1 is helpful to your research., Product Details of 144060-99-1

Reference£º
Thiazole | C3H584NS – PubChem,
Thiazole | chemical compound | Britannica