Category: pyridine-derivatives

Titi, Abderrahim; Messali, Mouslim; Alqurashy, Bakhet A.; Touzani, Rachid; Shiga, Takuya; Oshio, Hiroki; Fettouhi, Mohammed; Rajabi, Mehdi; Almalki, Faisal A.; Ben Hadda, Taibi published the artcile< Synthesis, characterization, X-ray crystal study and bioactivities of pyrazole derivatives: Identification of antitumor, antifungal and antibacterial pharmacophore sites>, Reference of 21901-29-1, the main research area is pyrazole preparation antitumor antifungal antibacterial human crystal structure mol; pharmacokinetic toxicity pyrazole.

The new pyrazole derivatives I [R = R1 = H, Me; R2 = H, CO2Et; X = C, N; Y = N, CNO2, CCO2H] were synthesized by reaction of hydroxymethyl pyrazole derivatives with primary amines and evaluated for their antifungal, antitumor and antibacterial activities. The structure of synthesized compounds I was identified by FT-IR, UV-visible, proton NMR spectroscopy, mass spectroscopy and single crystal X-ray crystallog. The pyrazoles I [R = R1 = R2 = H, X = Y = N], I [R = R1 = R2 = H, X = C, Y = CCO2H] and I [R = R1 = Me, R2 = CO2Et, X = N, Y = CNO2] were crystallized in space groups C2/c, P21/n and P-1 resp. Crystallog. anal. revealed that N-H of the amine group and nitrogen or oxygen atoms were in-plane with aromatic ring. The aminomethyl chain formed a distorted second plane. The angle between two planes was observed to be 76.07° (N2-C7-N5-N19) for compound I [R = R1 = R2 = H, X = Y = N], 62.12° (N34-C63-N22-N35) for compound I [R = R1 = R2 = H, X = C, Y = CCO2H], 60.84° (N3-C8-N2-N1) and 0.41° (N1-C4-C3-O1/O2) for compound I [R = R1 = Me, R2 = CO2Et, X = N, Y = CNO2]. Theor., phys. and chem. properties calculations had been performed on the pyrazoles I using three different programs: Petra, Osiris and Molinspiration (POM). The geometric parameters of optimized structure were in agreement with exptl. data obtained from X-ray structures.

Journal of Molecular Structure published new progress about Antibacterial agents. 21901-29-1 belongs to class pyridine-derivatives, and the molecular formula is C6H7N3O2, Reference of 21901-29-1.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Connon, Stephen J.; Hegarty, Anthony F. published the artcile< Stabilized 2,3-pyridyne reactive intermediates of exceptional dienophilicity>, Product Details of C6H5BrClNO, the main research area is regioselective lithiation thiophenoxy chloropyridine; thiophenoxy pyridyne preparation; pyridine endoxide preparation.

The enhanced dienophilicity of 4-methoxy, 4-aryloxy and 4-thiophenoxy analogs of 2,3-pyridyne relative to itself is reported. The regioselective lithiation of 4-alkoxy- and 4-thiophenoxy-2-chloropyridine at low temperatures, followed by elimination of lithium chloride affords 4-alkoxy- and 4-thiophenoxypyridynes, which can be trapped in situ in a [4+2] cycloaddition reaction with furan to give endoxides in moderate to good yields (25-58%). In contrast, precursors with a hydrogen or Me substituent at C-4 give no evidence for pyridyne formation under these conditions. Attempts to generate 6-isopropoxy-2,3-pyridyne from the low-temperature lithiation of 2-chloro-6-isopropoxypyridine were unsuccessful due to the instability of the 2-chloro-6-isopropoxy-5-lithiopyridine.

European Journal of Organic Chemistry published new progress about [4+2] Cycloaddition reaction. 777931-67-6 belongs to class pyridine-derivatives, and the molecular formula is C6H5BrClNO, Product Details of C6H5BrClNO.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Uraguchi, Daisuke; Kinoshita, Natsuko; Kizu, Tomohito; Ooi, Takashi published the artcile< Synergistic Catalysis of Ionic Bronsted Acid and Photosensitizer for a Redox Neutral Asymmetric α-Coupling of N-Arylaminomethanes with Aldimines>, COA of Formula: C33H21F3IrN3, the main research area is aldimine arylaminomethane chiral arylaminophosphonium iridium enantioselective coupling visible light; aryl diamine stereoselective preparation; chiral arylaminophosphonium photosensitizer iridium enantioselective coupling synergistic catalyst.

A redox neutral, highly enantioselective coupling between N-arylaminomethanes and N-sulfonyl aldimines was developed by harnessing the efficient catalysis of P-spiro chiral arylaminophosphonium barfate and a transition-metal photosensitizer under visible light irradiation This mode of synergistic catalysis provides a powerful strategy for controlling the bond-forming processes of reactive radical intermediates.

Journal of the American Chemical Society published new progress about Aldimines Role: RCT (Reactant), RACT (Reactant or Reagent). 370878-69-6 belongs to class pyridine-derivatives, and the molecular formula is C33H21F3IrN3, COA of Formula: C33H21F3IrN3.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

McCammant, Matthew S.; Sigman, Matthew S. published the artcile< Development and investigation of a site selective palladium-catalyzed 1,4-difunctionalization of isoprene using pyridine-oxazoline ligands>, Category: pyridine-derivatives, the main research area is pyridine oxazoline ligand preparation; polyene regioselective diastereoselective preparation; isoprene vinyl triflate vinylboronic acid palladium catalyst difunctionalization.

Palladium-catalyzed 1,4-difunctionalizations of isoprene that produce skipped polyenes were reported. Complex isomeric product mixtures were possible as a result of the difficult-to-control migratory insertion of isoprene into a Pd-alkenyl bond, but good site selectivity was achieved using easily accessible pyrox ligands. Mechanistic studies suggest that the control of insertion was the result of the unique electronic asymmetry and steric properties of the ligand.

Chemical Science published new progress about Addition reaction catalysts, stereoselective (regioselective). 1416819-91-4 belongs to class pyridine-derivatives, and the molecular formula is C13H15F3N2O, Category: pyridine-derivatives.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Rai, Roopa; Kolesnikov, Aleksandr; Sprengeler, Paul A.; Torkelson, Steven; Ton, Tony; Katz, Bradley A.; Yu, Christine; Hendrix, John; Shrader, William D.; Stephens, Robin; Cabuslay, Ronnell; Sanford, Ellen; Young, Wendy B. published the artcile< Discovery of novel heterocyclic factor VIIa inhibitors>, Category: pyridine-derivatives, the main research area is aminopyrrolopyridine preparation factor VIIa inhibitor SAR.

Structure-activity relationships and binding mode of novel heterocyclic factor VIIa inhibitors will be described. In these inhibitors, a highly basic 5-amidinoindole moiety has been successfully replaced with a less basic 5-aminopyrrolo[3,2-b]pyridine scaffold.

Bioorganic & Medicinal Chemistry Letters published new progress about Anticoagulants. 220731-04-4 belongs to class pyridine-derivatives, and the molecular formula is C10H15N3O2, Category: pyridine-derivatives.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Cheng, Kaiwu; Li, Yaojia; Gao, Zhiguo; Chen, Fanghui; You, Chaoqun; Sun, Baiwang published the artcile< Two-dimensional metal organic framework for effective gas absorption>, Safety of 2,4-Bipyridine, the main research area is soft phys exfoliation method preparation cadmium bipyridine MOF; crystal structure cadmium bipyridine MOF; gas adsorption thermal decomposition cadmium bipyridine MOF.

Herein, crystalline metal organic framework (MOF) nanosheets were fabricated through using a modified soft phys. exfoliation method from bulk crystals of a layered MOF, [Cd(4,4′-bpy)2(H2O)2](ClO4)2·(2,4′-bpy)2·H2O (MOF-1, 1), and fully characterized via transmission electron microscope (TEM), SEM, and at. force microscope (AFM). The delaminated MOF-1 nanosheets with porous structure showed good growth potential in selective gas adsorption.

Inorganic Chemistry Communications published new progress about Crystal structure. 581-47-5 belongs to class pyridine-derivatives, and the molecular formula is C10H8N2, Safety of 2,4-Bipyridine.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Hai, Yang; Geng, Jia-Jia; Li, Peng-Jie; Ma, Wei-Ping; Wang, Cui-Fang; Wei, Mei-Yan; Hou, Xue-Mei; Chen, Guang-Ying; Gu, Yu-Cheng; Liu, Ming; Shao, Chang-Lun published the artcile< Semisynthesis and biological evaluation of (+)-sclerotiorin derivatives as antitumor agents for the treatment of hepatocellular carcinoma>, Recommanded Product: 3-(Aminomethyl)-6-(trifluoromethyl)pyridine, the main research area is hepatocellular cervical carcinoma sclerotiorin antitumor cytotoxicity pharmacokinetics signaling; (+)-Sclerotiorin; AKT and ERK proteins; Antitumor; Hepatocellular carcinoma; Mouse xenograft model.

Hepatocellular carcinoma is one of the most common primary hepatic malignancy. Herein, a series of semisynthesized derivatives (2-30) of the natural product (+)-sclerotiorin (1) was prepared and evaluated the cytotoxic activities against six cancer cell lines. Among them, 3 and 5 were the most effective compounds against human hepatocellular carcinoma Bel-7402 cell line with IC50 values of 1.45 and 1.15 μM, resp. Mol. mechanism study showed that 5 disrupted the mitochondrial membrane potential and induced apoptosis in a caspase-dependent manner. In addition, 5 affected AKT and ERK signaling pathways and induced AKT and ERK proteins degradation through ubiquitin-proteasome system. Furthermore, 5 displayed significant in vivo anticancer effects in the xenograft models with decreasing the tumor mass by 52.5%. The safety evaluation was confirmed by acute toxicity subchronic toxicity tests, paraffin sections of mice organ and blood routine examination Taken together, 5 can be developed as a potential therapeutic agent for hepatocellular carcinoma.

European Journal of Medicinal Chemistry published new progress about Antiproliferative agents. 387350-39-2 belongs to class pyridine-derivatives, and the molecular formula is C7H7F3N2, Recommanded Product: 3-(Aminomethyl)-6-(trifluoromethyl)pyridine.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Jiang, Xiaoyue; Ye, Weidong; Song, Xiaohua; Ma, Wenxin; Lao, Xuejun; Shen, Runpu published the artcile< Novel ionic liquid with both Lewis and Bronsted acid sites for Michael addition>, Reference of 21876-43-7, the main research area is ionic liquid Lewis Bronsted acid preparation Michael addition; Lewis and Brønsted acid sites; Michael addition; novel ionic liquid.

Ionic liquid with both Lewis and Bronsted acid sites has been synthesized and its catalytic activities for Michael addition were carefully studied. The novel ionic liquid was stable to water and could be used in aqueous solution The molar ratio of the Lewis and Bronsted acid sites could be adjusted to match different reactions. The results showed that the novel ionic liquid was very efficient for a Michael addition and the synthesis of the target compounds was achieved in good to excellent yield within several min. Operational simplicity, high stability to water and air, small amount used, low cost of the catalyst used, high yields, chemoselectivity, applicability to large-scale reactions and reusability are the key features of this methodol., which indicated that this novel ionic liquid also holds great potential for environmentally friendly processes (green chem. methods).

International Journal of Molecular Sciences published new progress about Alkenes Role: RCT (Reactant), RACT (Reactant or Reagent). 21876-43-7 belongs to class pyridine-derivatives, and the molecular formula is C9H13NO3S, Reference of 21876-43-7.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Mizukawa, Yuki; Ikegami-Kawai, Mayumi; Horiuchi, Masako; Kaiser, Marcel; Kojima, Masayoshi; Sakanoue, Seiki; Miyagi, Seiya; Nanga Chick, Christian; Togashi, Hiroyuki; Tsubuki, Masayoshi; Ihara, Masataka; Usuki, Toyonobu; Itoh, Isamu published the artcile< Quest for a potent antimalarial drug lead: Synthesis and evaluation of 6,7-dimethoxyquinazoline-2,4-diamines>, Reference of 3731-53-1, the main research area is dimethoxyquinazolinediamine preparation antimalarial; Antimalarial drug; Derivatization; Quinazoline-2,4-diamines; SAR.

Quinazolines have long been known to exert varied pharmacol. activities that make them suitable for use in treating hypertension, viral infections, tumors, and malaria. Since 2014, author’s have synthesized approx. 150 different 6,7-dimethoxyquinazoline-2,4-diamines and evaluated their antimalarial activity via structure-activity relationship studies. Here, author’s summarize the results and report the discovery of 6,7-dimethoxy-N4-(1-phenylethyl)-2-(pyrrolidin-1-yl)quinazolin-4-amine, which exhibits high antimalarial activity as a promising antimalarial drug lead.

Bioorganic & Medicinal Chemistry published new progress about Amines Role: RCT (Reactant), RACT (Reactant or Reagent). 3731-53-1 belongs to class pyridine-derivatives, and the molecular formula is C6H8N2, Reference of 3731-53-1.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Wu, Yue; Jiang, Zhensheng; Li, Zhihong; Gu, Jing; You, Qidong; Zhang, Xiaojin published the artcile< Click Chemistry-Based Discovery of [3-Hydroxy-5-(1H-1,2,3-triazol-4-yl)picolinoyl]glycines as Orally Active Hypoxia-Inducing Factor Prolyl Hydroxylase Inhibitors with Favorable Safety Profiles for the Treatment of Anemia>, Synthetic Route of 870997-85-6, the main research area is preparation hydroxytriazolyl picolinoyl glycine derivative HIF PHD2 inhibitor anemia.

As a gene associated with anemia, the erythropoiesis gene is physiol. expressed under hypoxia regulated by †hypoxia-inducing factor-α (HIF-α). Thus, stabilizing HIF-α is a potent strategy to stimulate the expression and secretion of erythropoiesis. In this study, we applied click chem. to the discovery of HIF prolyl hydroxylase 2 (HIF-PHD2) inhibitors for the first time, and a series of triazole compounds showed preferable inhibitory activity in fluorescence polarization assays. Of particular note was the orally active HIF-PHD inhibitor 15i (IC50 = 62.23 nM), which was almost ten times more active than the phase III drug FG-4592 (IC50 = 591.4 nM). Furthermore, it can upregulate the Hb of cisplatin-induced anemia mice (120 g/L) to normal levels (160 g/L) with no apparent toxicity observed in vivo. These results confirm that triazole compound 15i is a promising candidate for the treatment of renal anemia.

Journal of Medicinal Chemistry published new progress about Anemia. 870997-85-6 belongs to class pyridine-derivatives, and the molecular formula is C6H5BrN2O2, Synthetic Route of 870997-85-6.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem