Category: 1190875-39-8

Lee, Dahye published the artcileDiscovery of Novel Pyruvate Dehydrogenase Kinase 4 Inhibitors for Potential Oral Treatment of Metabolic Diseases, Name: (1-(1-(tert-Butoxycarbonyl)piperidin-4-yl)-1H-pyrazol-4-yl)boronic acid, the publication is Journal of Medicinal Chemistry (2019), 62(2), 575-588, database is CAplus and MEDLINE.

Pyruvate dehydrogenase kinase 4 (PDK4) activation is associated with metabolic diseases including hyperglycemia, insulin resistance, allergies, and cancer. Structural modifications of hit anthraquinone led to the identification of a new series of allosteric PDK4 inhibitors. Among this series, compound 8c showed promising in vitro activity with an IC₅₀ value of 84 nM. Good metabolic stability, pharmacokinetic profiles, and possible metabolites were suggested. Compound 8c improved glucose tolerance in diet-induced obese mice and ameliorated allergic reactions in a passive cutaneous anaphylaxis mouse model. Addnl., compound 8c exhibited anticancer activity by controlling cell proliferation, transformation, and apoptosis. From the mol. docking studies, compound 8c displayed optimal fitting in the lipoamide binding site (allosteric) with a full fitness, providing a new scaffold for drug development toward PDK4 inhibitors.

Journal of Medicinal Chemistry published new progress about 1190875-39-8. 1190875-39-8 belongs to pyrazoles-derivatives, auxiliary class Pyrazole,Piperidine,Boronic acid and ester,Amide,Boronic Acids,Boronic Acids,Boronic acid and ester,, name is (1-(1-(tert-Butoxycarbonyl)piperidin-4-yl)-1H-pyrazol-4-yl)boronic acid, and the molecular formula is C13H22BN3O4, Name: (1-(1-(tert-Butoxycarbonyl)piperidin-4-yl)-1H-pyrazol-4-yl)boronic acid.

Referemce:
https://en.wikipedia.org/wiki/Pyrazole,
Pyrazoles – an overview | ScienceDirect Topics

Cho, Sung Yun published the artcileDesign and synthesis of novel 3-(benzo[d]oxazol-2-yl)-5-(1-(piperidin-4-yl)-1H-pyrazol-4-yl)pyridin-2-amine derivatives as selective G-protein-coupled receptor kinase-2 and -5 inhibitors, HPLC of Formula: 1190875-39-8, the publication is Bioorganic & Medicinal Chemistry Letters (2013), 23(24), 6711-6716, database is CAplus and MEDLINE.

G-protein-coupled receptor kinase (GRK)-2 and -5 are emerging therapeutic targets for the treatment of cardiovascular disease. In the efforts to discover novel small mols. to inhibit GRK-2 and -5, a class of compound based on 3-(benzo[d]oxazol-2-yl)-5-(1-(piperidin-4-yl)-1H-pyrazol-4-yl)pyridin-2-amine was identified as a novel hit by high throughput screening campaign. Structural modification of parent benzoxazole scaffolds by introducing substituents on Ph displayed potent inhibitory activities toward GRK-2 and -5.

Bioorganic & Medicinal Chemistry Letters published new progress about 1190875-39-8. 1190875-39-8 belongs to pyrazoles-derivatives, auxiliary class Pyrazole,Piperidine,Boronic acid and ester,Amide,Boronic Acids,Boronic Acids,Boronic acid and ester,, name is (1-(1-(tert-Butoxycarbonyl)piperidin-4-yl)-1H-pyrazol-4-yl)boronic acid, and the molecular formula is C13H22BN3O4, HPLC of Formula: 1190875-39-8.

Referemce:
https://en.wikipedia.org/wiki/Pyrazole,
Pyrazoles – an overview | ScienceDirect Topics

Avinesh, P. published the artcileFacile Synthesis of Fully Decorated Imidazo[4,5-b] and Imidazo[4,5-c] Pyridines in Aqueous DMF via C-H Activation under Microwave Irradiation, HPLC of Formula: 1190875-39-8, the publication is ChemistrySelect (2016), 1(10), 2265-2270, database is CAplus.

Catalytic C-H bond activation of heteroarenes has gained tremendous potential in recent years due to their environmentally and economically benign nature. In this paper, the regioisomeric synthesis of fully decorated imidazopyridines, e.g., I employing a C-H activation protocol with a wide range of aryl/hetero aryl/alkyl boronic acids, e.g., II in aqueous DMF is reported. The use of inexpensive copper catalyst and bathophenanthroline as ligand were found to be instrumental in driving these reactions to completion. This optimized protocol was further extended to alkyl/aryl/heteroaryl potassium organo trifluoroborates such as potassium trifluoro(4-methoxyphenyl)boranuide, potassium trifluoro[4-(trifluoromethyl)phenyl]boranuide, potassium trifluoro(3,4,5-trimethylphenyl)boranuide, etc. A wide range of diversely substituted imidazo pyridine analogs which are known for their potential therapeutic applications have been synthesized using this highly efficient and atom economical protocol.

ChemistrySelect published new progress about 1190875-39-8. 1190875-39-8 belongs to pyrazoles-derivatives, auxiliary class Pyrazole,Piperidine,Boronic acid and ester,Amide,Boronic Acids,Boronic Acids,Boronic acid and ester,, name is (1-(1-(tert-Butoxycarbonyl)piperidin-4-yl)-1H-pyrazol-4-yl)boronic acid, and the molecular formula is C13H22BN3O4, HPLC of Formula: 1190875-39-8.

Referemce:
https://en.wikipedia.org/wiki/Pyrazole,
Pyrazoles – an overview | ScienceDirect Topics

Ryu, Jae Wook published the artcileDesign and synthesis of triazolopyridazines substituted with methylisoquinolinone as selective c-Met kinase inhibitors, Recommanded Product: (1-(1-(tert-Butoxycarbonyl)piperidin-4-yl)-1H-pyrazol-4-yl)boronic acid, the publication is Bioorganic & Medicinal Chemistry Letters (2011), 21(23), 7185-7188, database is CAplus and MEDLINE.

A series of triazolopyridazines substituted with methylisoquinolinone, e.g. I (R = Ph, pyrrolidin-1-yl, thiazol-3-yl, 3-FC₆H₄), were designed and synthesized. Some of the triazolopyridazines strongly inhibited c-Met kinase and showed good anti-proliferative activity against a panel of c-Met-amplified gastric cancer cell lines (MKN-45, SNU-5 and Hs746T).

Bioorganic & Medicinal Chemistry Letters published new progress about 1190875-39-8. 1190875-39-8 belongs to pyrazoles-derivatives, auxiliary class Pyrazole,Piperidine,Boronic acid and ester,Amide,Boronic Acids,Boronic Acids,Boronic acid and ester,, name is (1-(1-(tert-Butoxycarbonyl)piperidin-4-yl)-1H-pyrazol-4-yl)boronic acid, and the molecular formula is C13H22BN3O4, Recommanded Product: (1-(1-(tert-Butoxycarbonyl)piperidin-4-yl)-1H-pyrazol-4-yl)boronic acid.

Referemce:
https://en.wikipedia.org/wiki/Pyrazole,
Pyrazoles – an overview | ScienceDirect Topics