Tag: M.W=100-150

East, Stephen P. published the artcileDNA gyrase (GyrB)/topoisomerase IV (ParE) inhibitors: Synthesis and antibacterial activity, Product Details of C3H5BN2O2, the publication is Bioorganic & Medicinal Chemistry Letters (2009), 19(3), 894-899, database is CAplus and MEDLINE.

The synthesis and antibacterial activities of three chemotypes of DNA supercoiling inhibitors based on imidazo[1,2-a]pyridine and [1,2,4]triazolo[1,5-a]pyridine scaffolds, e.g. I (R = H, Ph, 2-HOC₆H₄, 2-pyridyl, 5-pyrimidyl, 1-imidazolyl, CO₂Me, CONHEt, etc.), that target the ATPase subunits of DNA gyrase and topoisomerase IV (GyrB/ParE) is reported. The most potent scaffold was selected for optimization leading to a series with potent Gram-pos. antibacterial activity and a low resistance frequency.

Bioorganic & Medicinal Chemistry Letters published new progress about 763120-58-7. 763120-58-7 belongs to pyrazoles-derivatives, auxiliary class Pyrazole,Boronic acid and ester,Boronic Acids,Boronic acid and ester, name is 1H-Pyrazole-4-boronic acid, and the molecular formula is C3H5BN2O2, Product Details of C3H5BN2O2.

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

Liang, Yanke published the artcileStructure-Activity Relationship study of QL47-a Broad-spectrum Antiviral agent, Recommanded Product: 1H-Pyrazole-4-boronic acid, the publication is ACS Medicinal Chemistry Letters (2017), 8(3), 344-349, database is CAplus and MEDLINE.

Here the authors report the structure-activity relationship (SAR) investigations of QL-XII-47 (QL47), a compound that possesses broad-spectrum antiviral activity against dengue virus and other RNA viruses. A medicinal chem. campaign initiated from QL47, a previously reported covalent BTK inhibitor, to derive YKL-04-085 which is devoid of any kinase activity when screened against a panel of 468 kinases and with imprundooved pharmacokinetic properties. Both QL47 and YKL-04-085 are potent inhibitors of viral translation and exhibit cellular anti-viral activity at 35-fold lower concentrations relative to inhibition of host-cell proliferation.

ACS Medicinal Chemistry Letters published new progress about 763120-58-7. 763120-58-7 belongs to pyrazoles-derivatives, auxiliary class Pyrazole,Boronic acid and ester,Boronic Acids,Boronic acid and ester, name is 1H-Pyrazole-4-boronic acid, and the molecular formula is C3H5BN2O2, Recommanded Product: 1H-Pyrazole-4-boronic acid.

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

Hynes, John Jr. published the artcileDiscovery of potent and efficacious pyrrolopyridazines as dual JAK1/3 inhibitors, Application In Synthesis of 724710-02-5, the publication is Bioorganic & Medicinal Chemistry Letters (2017), 27(14), 3101-3106, database is CAplus and MEDLINE.

A series of potent dual JAK1/3 inhibitors have been developed from a moderately selective JAK3 inhibitor. Substitution at the C6 position of the pyrrolopyridazine core with aryl groups provided exceptional biochem. potency against JAK1 and JAK3 while maintaining good selectivity against JAK2 and Tyk2. Translation to in vivo efficacy was observed in a murine model of chronic inflammation. X-ray co-crystal structure determination confirmed the presumed inhibitor binding orientation in JAK3. Efforts to reduce hERG channel inhibition will be described.

Bioorganic & Medicinal Chemistry Letters published new progress about 724710-02-5. 724710-02-5 belongs to pyrazoles-derivatives, auxiliary class Pyrazole,Boronic acid and ester,Pyrazole,Boronic Acids,Boronic acid and ester, name is (1H-Pyrazol-5-yl)boronic acid, and the molecular formula is C3H5BN2O2, Application In Synthesis of 724710-02-5.

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

Zhang, Qingwei published the artcileHit to Lead optimization of a novel class of squarate-containing polo-like kinase inhibitors, COA of Formula: C3H5BN2O2, the publication is Bioorganic & Medicinal Chemistry Letters (2012), 22(24), 7615-7622, database is CAplus and MEDLINE.

Aminodioxocyclobutenylamino pyrimidineamines (aminopyrimidine squaramides) such as I, derived from a squaramide identified through high-throughput screening, were prepared as selective Polo-like kinase 1 (Plk1) inhibitors for potential use as antitumor agents. Using mol. modeling and extensive structure-activity studies, I (Plk1 K_i = 5 nM; EC₅₀ = 1.05 μM) was identified; its inhibition of Plk1 and of a panel of kinases, its lipophilicity, and its pharmacokinetics were determined I demonstrated moderate efficacy at dosages of 100 mg/kg in a murine pancreatic cancer xenograft tumor model and no overt toxicity.

Bioorganic & Medicinal Chemistry Letters published new progress about 763120-58-7. 763120-58-7 belongs to pyrazoles-derivatives, auxiliary class Pyrazole,Boronic acid and ester,Boronic Acids,Boronic acid and ester, name is 1H-Pyrazole-4-boronic acid, and the molecular formula is C9H17NO, COA of Formula: C3H5BN2O2.

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

Caldwell, John J. published the artcileDesign and synthesis of 2(1H)-pyrazinones as inhibitors of protein kinases, Category: pyrazoles-derivatives, the publication is Tetrahedron (2012), 68(47), 9713-9728, database is CAplus.

Kinase enzymes play a key role in the development and progression of cancer. Inhibitors of deregulated kinases are effective small mol. anticancer drugs. The 2(1H)-pyrazinone heterocycle is a previously unexploited motif that can fulfil the structural requirements for ATP-competitive inhibition of kinases. Rapid solution-phase syntheses of novel 3,5- and 3,6-disubstituted-2(1H)-pyrazinones were developed through selective, sequential substitution of 2,5-dihalo-3-benzyloxypyrazine and 3,5-dihalo-2(1H)-pyrazinone intermediates. Palladium-catalyzed cross-couplings and S_NAr reactions were used to introduce substituents chosen on the basis of the calculated physicochem. properties of the target pyrazinones. Representative compounds, e.g., I, demonstrated good solubility, kinase inhibitory activity and antiproliferative activity in human tumor cells, confirming the suitability of this chem. class as a kinase-focused library.

Tetrahedron published new progress about 724710-02-5. 724710-02-5 belongs to pyrazoles-derivatives, auxiliary class Pyrazole,Boronic acid and ester,Pyrazole,Boronic Acids,Boronic acid and ester, name is (1H-Pyrazol-5-yl)boronic acid, and the molecular formula is C3H5BN2O2, Category: pyrazoles-derivatives.

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

Caldwell, John J. published the artcileDesign and synthesis of 2(1H)-pyrazinones as inhibitors of protein kinases, Category: pyrazoles-derivatives, the publication is Tetrahedron (2012), 68(47), 9713-9728, database is CAplus.

Kinase enzymes play a key role in the development and progression of cancer. Inhibitors of deregulated kinases are effective small mol. anticancer drugs. The 2(1H)-pyrazinone heterocycle is a previously unexploited motif that can fulfil the structural requirements for ATP-competitive inhibition of kinases. Rapid solution-phase syntheses of novel 3,5- and 3,6-disubstituted-2(1H)-pyrazinones were developed through selective, sequential substitution of 2,5-dihalo-3-benzyloxypyrazine and 3,5-dihalo-2(1H)-pyrazinone intermediates. Palladium-catalyzed cross-couplings and S_NAr reactions were used to introduce substituents chosen on the basis of the calculated physicochem. properties of the target pyrazinones. Representative compounds, e.g., I, demonstrated good solubility, kinase inhibitory activity and antiproliferative activity in human tumor cells, confirming the suitability of this chem. class as a kinase-focused library.

Tetrahedron published new progress about 763120-58-7. 763120-58-7 belongs to pyrazoles-derivatives, auxiliary class Pyrazole,Boronic acid and ester,Boronic Acids,Boronic acid and ester, name is 1H-Pyrazole-4-boronic acid, and the molecular formula is C3H5BN2O2, Category: pyrazoles-derivatives.

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

Giordanetto, Fabrizio published the artcileDiscovery of phosphoinositide 3-kinases (PI3K) p110β isoform inhibitor 4-[2-hydroxyethyl(1-naphthylmethyl)amino]-6-[(2S)-2-methylmorpholin-4-yl]-1H-pyrimidin-2-one, an effective antithrombotic agent without associated bleeding and insulin resistance, Application of 1H-Pyrazole-4-boronic acid, the publication is Bioorganic & Medicinal Chemistry Letters (2012), 22(21), 6671-6676, database is CAplus and MEDLINE.

Structure-based evolution of the original fragment leads resulted in the identification of 4-[2-hydroxyethyl(1-naphthylmethyl)amino]-6-[(2S)-2-methylmorpholin-4-yl]-1H-pyrimidin-2-one, (S)-21, a potent, selective phosphoinositide 3-kinases (PI3K) p110β isoform inhibitor with favorable in vivo antiplatelet effect. Despite its antiplatelet action, (S)-21 did not significantly increase bleeding time in dogs. Addnl., due to its enhanced selectivity over p110α, (S)-21 did not induce any insulin resistance in rats.

Bioorganic & Medicinal Chemistry Letters published new progress about 763120-58-7. 763120-58-7 belongs to pyrazoles-derivatives, auxiliary class Pyrazole,Boronic acid and ester,Boronic Acids,Boronic acid and ester, name is 1H-Pyrazole-4-boronic acid, and the molecular formula is C3H5BN2O2, Application of 1H-Pyrazole-4-boronic acid.

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

Bardhan, Sujata published the artcileHeteroaryl ethers by oxidative palladium catalysis of pyridotriazol-1-yloxy pyrimidines with arylboronic acids, Formula: C3H5BN2O2, the publication is Organic Letters (2009), 11(12), 2511-2514, database is CAplus and MEDLINE.

The oxidative palladium-catalyzed cross-coupling of pyrimidines containing pyridotriazol-1-yloxy (OPt) as either a urea or an amide functional group with arylboronic acids in the presence of Cs₂CO₃ in DME containing 0.6-1.0% H₂O is described for the preparation of heteroaryl ethers. The bromo substitution in the case of 3-(5-bromo-pyrimidin-2-yloxy)-3H-[1,2,3]triazolo[4,5-b]pyridine could serve as a handle for further elaborations such as Suzuki coupling for attaching varied aryl groups.

Organic Letters published new progress about 763120-58-7. 763120-58-7 belongs to pyrazoles-derivatives, auxiliary class Pyrazole,Boronic acid and ester,Boronic Acids,Boronic acid and ester, name is 1H-Pyrazole-4-boronic acid, and the molecular formula is C3H5BN2O2, Formula: C3H5BN2O2.

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

Pham, Thanh Truc published the artcileNovel 1,2-dihydroquinazolin-2-ones: Design, synthesis, and biological evaluation against Trypanosoma brucei, Name: (1H-Pyrazol-5-yl)boronic acid, the publication is Bioorganic & Medicinal Chemistry Letters (2017), 27(16), 3629-3635, database is CAplus and MEDLINE.

In 2014, a published report of the high-throughput screen of >42,000 kinase inhibitors from GlaxoSmithKline against T. brucei identified 797 potent and selective hits. From this rich data set, the authors selected NEU-<0001101≥(1) for hit-to-lead optimization. Through the authors’ preliminary compound synthesis and SAR studies, the authors confirmed the previously reported activity of 4-phenyl-6-(pyridin-4-yl)quinazolin-2(1H)-one in a T. brucei cell proliferation assay and have identified alternative groups to replace the pyridyl ring in 4-phenyl-6-(pyridin-4-yl)quinazolin-2(1H)-one. Pyrazole 24 achieves improvements in both potency and lipophilicity relative to 4-phenyl-6-(pyridin-4-yl)quinazolin-2(1H)-one , while also showing good in vitro metabolic stability. The SAR developed on 24 provides new directions for further optimization of this novel scaffold for anti-trypanosomal drug discovery.

Bioorganic & Medicinal Chemistry Letters published new progress about 724710-02-5. 724710-02-5 belongs to pyrazoles-derivatives, auxiliary class Pyrazole,Boronic acid and ester,Pyrazole,Boronic Acids,Boronic acid and ester, name is (1H-Pyrazol-5-yl)boronic acid, and the molecular formula is C3H5BN2O2, Name: (1H-Pyrazol-5-yl)boronic acid.

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

Pham, Thanh Truc published the artcileNovel 1,2-dihydroquinazolin-2-ones: Design, synthesis, and biological evaluation against Trypanosoma brucei, Category: pyrazoles-derivatives, the publication is Bioorganic & Medicinal Chemistry Letters (2017), 27(16), 3629-3635, database is CAplus and MEDLINE.

In 2014, a published report of the high-throughput screen of >42,000 kinase inhibitors from GlaxoSmithKline against T. brucei identified 797 potent and selective hits. From this rich data set, the authors selected NEU-<0001101≥(1) for hit-to-lead optimization. Through the authors’ preliminary compound synthesis and SAR studies, the authors confirmed the previously reported activity of 4-phenyl-6-(pyridin-4-yl)quinazolin-2(1H)-one in a T. brucei cell proliferation assay and have identified alternative groups to replace the pyridyl ring in 4-phenyl-6-(pyridin-4-yl)quinazolin-2(1H)-one. Pyrazole 24 achieves improvements in both potency and lipophilicity relative to 4-phenyl-6-(pyridin-4-yl)quinazolin-2(1H)-one , while also showing good in vitro metabolic stability. The SAR developed on 24 provides new directions for further optimization of this novel scaffold for anti-trypanosomal drug discovery.

Bioorganic & Medicinal Chemistry Letters published new progress about 763120-58-7. 763120-58-7 belongs to pyrazoles-derivatives, auxiliary class Pyrazole,Boronic acid and ester,Boronic Acids,Boronic acid and ester, name is 1H-Pyrazole-4-boronic acid, and the molecular formula is C3H5BN2O2, Category: pyrazoles-derivatives.

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