Month: October 2022

Tear, Westley F.; Bag, Seema; Diaz-Gonzalez, Rosario; Ceballos-Perez, Gloria; Rojas-Barros, Domingo I.; Cordon-Obras, Carlos; Perez-Moreno, Guiomar; Garcia-Hernandez, Raquel; Martinez-Martinez, Maria Santos; Ruiz-Perez, Luis Miguel; Gamarro, Francisco; Gonzalez Pacanowska, Dolores; Caffrey, Conor R.; Ferrins, Lori; Manzano, Pilar; Navarro, Miguel; Pollastri, Michael P. published the artcile< Selectivity and Physicochemical Optimization of Repurposed Pyrazolo[1,5-b]pyridazines for the Treatment of Human African Trypanosomiasis>, Product Details of C4H5N3, the main research area is human african trypanosomiasis Trypanosoma brucei antiparasitic activity trypanosome infection.

From a high-throughput screen of 42 444 known human kinases inhibitors, a pyrazolo[1,5-b]pyridazine scaffold was identified to begin optimization for the treatment of human African trypanosomiasis. Previously reported data for analogous compounds against human kinases GSK-3β, CDK-2, and CDK-4 were leveraged to try to improve the selectivity of the series, resulting in 23a which showed selectivity for T. b. brucei over these three human enzymes. In parallel, properties known to influence the absorption, distribution, metabolism, and excretion (ADME) profile of the series were optimized resulting in 20g being progressed into an efficacy study in mice. Though 20g showed toxicity in mice, it also demonstrated CNS penetration in a PK study and significant reduction of parasitemia in four out of the six mice.

Journal of Medicinal Chemistrypublished new progress about Central nervous system (CNS penetration). 20744-39-2 belongs to class pyridazine, and the molecular formula is C4H5N3, Product Details of C4H5N3.

Referemce:
Pyridazine – Wikipedia,
Pyridazine | C4H4N2 – PubChem

Tong, Chao-Lai; Xu, Xiu-Hua; Qing, Feng-Ling published the artcile< Nucleophilic and Radical Heptafluoroisopropoxylation with Redox-Active Reagents>, Product Details of C9H8ClN3O2, the main research area is heptafluoroisopropyl ether preparation; hydroxylamine oxidative heptafluoroisopropyl silver heptafluoroisopropylation; conformation; heptafluoroisopropoxylation; nucleophilic reactions; radical reactions; redox-active reagents.

The practical and efficient heptafluoroisopropoxylation reactions through the invention of a series of redox-active N-OCF(CF3)2 reagents e.g., I were described. These reagents were readily prepared from the oxidative heptafluoroisopropylation of hydroxylamines e.g., II with AgCF(CF3)2. The substitutions on the nitrogen atom significantly affected the properties and reactivities of N-OCF(CF3)2 reagents. Accordingly, two types of N-OCF(CF3)2 reagents including I and III were used as OCF(CF3)2 anion and radical precursors, resp. This protocol enables the direct heptafluoroisopropoxylation of a range of substrates, delivering the corresponding products in moderate to excellent yields.

Angewandte Chemie, International Editionpublished new progress about Alcohols Role: RCT (Reactant), RACT (Reactant or Reagent). 64067-99-8 belongs to class pyridazine, and the molecular formula is C9H8ClN3O2, Product Details of C9H8ClN3O2.

Referemce:
Pyridazine – Wikipedia,
Pyridazine | C4H4N2 – PubChem

Burton, Rebecca J.; Crowther, Mandy L.; Fazakerley, Neal J.; Fillery, Shaun M.; Hayter, Barry M.; Kettle, Jason G.; McMillan, Caroline A.; Perkins, Paula; Robins, Peter; Smith, Peter M.; Williams, Emma J.; Wrigley, Gail L. published the artcile< Highly regioselective Buchwald-Hartwig amination at C-2 of 2,4-dichloropyridine enabling a novel approach to 2,4-bisanilinopyridine (BAPyd) libraries>, Reference of 20744-39-2, the main research area is Buchwald Hartwig amination dichloropyridine bisanilinopyridine library.

The highly regioselective Buchwald-Hartwig amination at C-2 of the cheap and readily accessible reagent, 2,4-dichloropyridine with a range of anilines and heterocyclic amines is described. This new methodol. is robust and provides a facile access to 4-chloro-N-phenylpyridin-2-amines on 0.25 mol scale. These intermediates undergo a further Buchwald-Hartwig amination at higher temperature to enable rapid exploration of the chem. space at C-4 and to provide a library of 2,4-bisaminopyridines.

Tetrahedron Letterspublished new progress about Buchwald-Hartwig reaction. 20744-39-2 belongs to class pyridazine, and the molecular formula is C4H5N3, Reference of 20744-39-2.

Referemce:
Pyridazine – Wikipedia,
Pyridazine | C4H4N2 – PubChem

Liu, Bin; Xu, Xiaona; Tong, Hongjuan; Zhu, Zhoujing; Tang, Wenqiang; Tang, Chu published the artcile< Synthesis and Antiproliferative Evaluation of Novel 5-Substituted Pyridazin-4-Amine Derivatives>, Quality Control of 20744-39-2, the main research area is aminopyridazine preparation antitumor SAR.

A series of 5-substituted pyridazin-4-amine derivatives were synthesized, characterized and evaluated for antitumor activities. The target compounds exhibited moderate to high anti-proliferative activities depending on the type of substituents of the pyridazine skeleton. Preliminary data on their biol. activity against several cancer cell lines of A549, PC3, MCF-7 and HeLa cells was further reported. Specifically, introduction of bulky aromatic substituents onto the pyridazine skeleton have potential benefit against liver cancer cells.

Organic Preparations and Procedures Internationalpublished new progress about Antitumor agents. 20744-39-2 belongs to class pyridazine, and the molecular formula is C4H5N3, Quality Control of 20744-39-2.

Referemce:
Pyridazine – Wikipedia,
Pyridazine | C4H4N2 – PubChem

Harcken, Christian; Riether, Doris; Kuzmich, Daniel; Liu, Pingrong; Betageri, Raj; Ralph, Mark; Emmanuel, Michel; Reeves, Jonathan T.; Berry, Angela; Souza, Donald; Nelson, Richard M.; Kukulka, Alison; Fadra, Tazmeen N.; Zuvela-Jelaska, Ljiljana; Dinallo, Roger; Bentzien, Jorg; Nabozny, Gerald H.; Thomson, David S. published the artcile< Identification of Highly Efficacious Glucocorticoid Receptor Agonists with a Potential for Reduced Clinical Bone Side Effects>, Formula: C4H5N3, the main research area is nonsteroidal glucocorticoid receptor agonist antiinflammatory reduced bone side effect.

Synthesis and structure-activity relationship (SAR) of a series of nonsteroidal glucocorticoid receptor (GR) agonists are described. These compounds contain “”diazaindole”” moieties and display different transcriptional regulatory profiles in vitro and are considered “”dissociated”” between gene transrepression and transactivation. The lead optimization effort described in this article focused in particular on limiting the transactivation of genes which result in bone side effects and these were assessed in vitro in MG-63 osteosarcoma cells, leading to the identification of the R enantiomers of I and II. These compounds maintained anti-inflammatory activity in vivo in collagen induced arthritis studies in mouse but had reduced effects on bone relevant parameters compared to the widely used synthetic glucocorticoid prednisolone in vivo. To our knowledge, we are the first to report on selective glucocorticoid ligands with reduced bone loss in a preclin. in vivo model.

Journal of Medicinal Chemistrypublished new progress about Anti-inflammatory agents. 20744-39-2 belongs to class pyridazine, and the molecular formula is C4H5N3, Formula: C4H5N3.

Referemce:
Pyridazine – Wikipedia,
Pyridazine | C4H4N2 – PubChem