Tag: M.W=150-200

Pavia, Michael R. published the artcileN,N-Disubstituted 6-alkoxy-2-pyridinamines as anticonvulsant agents, HPLC of Formula: 42144-78-5, the main research area is alkoxypyridinamine preparation anticonvulsant; chloropyridine alkoxylation; alkoxychloropyridine aminolysis piperazine piperidine morpholine; pyridinamine alkoxy preparation anticonvulsant; aminopyridine alkoxy preparation anticonvulsant.

The anticonvulsant effect of a series of title compounds I (R = Me, Et, Me2CH, Me2CHCH2, Me2NCH2CH2, cyclopropylmethyl, cyclohexyl, cyclohexylmethyl; R1 = e.g., piperazino, piperidino, morpholino) is described. The activity/side-effect ratio in this series of compounds was optimized. I (R = Me2CHCH2; R1 = piperazino) (II) showed the most desirable profile, and was selected for a more complete pharmacol. evaluation. Overall, the pharmacol. profile of II is very similar to that of diphenylhydantoin (phenytoin). While II is nearly equipotent to phenytoin, animal studies suggest a fairly short duration of action. In addition, II exhibited some troublesome side effects including central nervous system depression and hypothermia.

Journal of Medicinal Chemistry published new progress about Alkoxylation. 42144-78-5 belongs to class pyridine-derivatives, name is 2-Chloro-6-ethoxypyridine, and the molecular formula is C7H8ClNO, HPLC of Formula: 42144-78-5.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Yao, Jianwen published the artcileDesign, synthesis and biological activities of sorafenib derivatives as antitumor agents, Recommanded Product: Methyl 4-chloropicolinate, the main research area is sorafenib derivative preparation antitumor antiangiogenesis activity.

A series of novel sorafenib derivatives was designed and synthesized in high yields using various substituted anilines, and their antiproliferative activities against HCT116, PC-3 and MDA-MB-231 cell lines were also evaluated and described. All compounds exhibited potent antiproliferative activity against HCT116 and PC-3 cells with IC50 = 2.8-52.0 and 2.2-45.6 μM; compounds I [R = Et, cyclopropyl] demonstrated competitive antiproliferative activities to sorafenib against all three cancer cell lines; the cytotoxicity of compound I [R = cyclohexyl] is more potent than that of sorafenib. Some compounds were chosen for further evaluation of the anti-angiogenesis activity, and showed the inhibition of sprout formation from aortic ring ex vivo. The structures of all the newly synthesized compounds were determined by 1H NMR, 13C NMR and HRMS.

Bioorganic & Medicinal Chemistry Letters published new progress about Angiogenesis. 24484-93-3 belongs to class pyridine-derivatives, name is Methyl 4-chloropicolinate, and the molecular formula is C7H6ClNO2, Recommanded Product: Methyl 4-chloropicolinate.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Tu, Xijuan published the artcileMiniaturized salting-out assisted liquid-liquid extraction combined with disposable pipette extraction for fast sample preparation of neonicotinoid pesticides in bee pollen, SDS of cas: 21190-89-6, the main research area is neonicotinoid pesticide bee pollen pipet salting out liquid extraction; HPLC; bee pollen; disposable pipette extraction; neonicotinoid pesticides; salting-out assisted liquid-liquid extraction; sample preparation.

As the main source of nutrients for the important pollinator honeybee, bee pollen is crucial for the health of the honeybee and the agro-ecosystem. In the present study, a new sample preparation procedure has been developed for the determination of neonicotinoid pesticides in bee pollen. The neonicotinoid pesticides were extracted using miniaturized salting-out assisted liquid-liquid extraction (mini-SALLE), followed by disposable pipet extraction (DPX) for the clean-up of analytes. Effects of DPX parameters on the clean-up performance were systematically investigated, including sorbent types (PSA, C18, and silica gel), mass of sorbent, loading modes, and elution conditions. In addition, the clean-up effect of classical dispersive solid-phase extraction (d-SPE) was compared with that of the DPX method. Results indicated that PSA-based DPX showed excellent clean-up ability for the high performance liquid chromatog. (HPLC) anal. of neonicotinoid pesticides in bee pollen. The proposed DPX method was fully validated and demonstrated to provide the advantage of simple and rapid clean-up with low consumption of solvent. This is the first report of DPX method applied in bee pollen matrix, and would be valuable for the development of a fast sample preparation method for this challenging and important matrix.

Molecules published new progress about Apis mellifera. 21190-89-6 belongs to class pyridine-derivatives, name is Ethyl 6-chloropicolinate, and the molecular formula is C8H8ClNO2, SDS of cas: 21190-89-6.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Yang, Min published the artcilePalladium-Catalyzed C-4 Selective Coupling of 2,4-Dichloropyridines and Synthesis of Pyridine-Based Dyes for Live-Cell Imaging, Application In Synthesis of 132097-09-7, the main research area is palladium catalyst coupling dichloropyridine boronic ester toxicity cell imaging; pyridine dye palladium catalyst coupling dichloropyridine boronic ester.

An alternative process of Pd-catalyzed C-4 selective coupling of 2,4-dichloropyridines with boronic esters was developed, which afforded 24 examples of C-4 coupled pyridines in moderate to good yields. After further arylation, 21 examples of C-2, C-4 diarylated pyridines with a significant photophys. property were obtained, which were applied as pyridine-based dyes into live-cell imaging with good biocompatibility and low toxicity.

Journal of Organic Chemistry published new progress about Biocompatibility. 132097-09-7 belongs to class pyridine-derivatives, name is 2,4-Dichloro-3-methylpyridine, and the molecular formula is C6H5Cl2N, Application In Synthesis of 132097-09-7.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Ghiazza, Clement published the artcileDeaminative chlorination of aminoheterocycles, HPLC of Formula: 24484-93-3, the main research area is chloro heterocycle selective preparation; aminoheterocycle deaminative chlorination.

Herein we present a simple methodol. that enabled the NH2 groups in aminoheterocycles to be conceived as masked modification handles. With the aid of a simple pyrylium reagent and a cheap chloride source, C(sp2)-NH2 could be converted into C(sp2)-Cl bonds. The method was characterized by its wide functional group tolerance and substrate scope, allowing the modification of different classes of heteroaromatic motifs (five- and six-membered heterocycles), bearing numerous sensitive motifs. The facile conversion of NH2 into Cl in a late-stage fashion enabled practitioners to apply Sandmeyer- and Vilsmeier-type transforms without the burden of explosive and unsafe diazonium salts, stoichiometric transition metals or highly oxidizing and unselective chlorinating agents.

Nature Chemistry published new progress about Chemoselectivity. 24484-93-3 belongs to class pyridine-derivatives, name is Methyl 4-chloropicolinate, and the molecular formula is C7H6ClNO2, HPLC of Formula: 24484-93-3.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Perry, Matthew W. D. published the artcileDiscovery of AZD8154, a Dual PI3Kγδ Inhibitor for the Treatment of Asthma, Related Products of pyridine-derivatives, the main research area is AZD8154 PI3K gamma delta inhibitor asthma inhaled.

Starting from our previously described PI3Kγ inhibitors, we describe the exploration of structure-activity relationships that led to the discovery of highly potent dual PI3Kγδ inhibitors. We explored changes in two positions of the mols., including macrocyclization, but ultimately identified a simpler series with the desired potency profile that had suitable physicochem. properties for inhalation. We were able to demonstrate efficacy in a rat ovalbumin challenge model of allergic asthma and in cells derived from asthmatic patients. The optimized compound, AZD8154, has a long duration of action in the lung and low systemic exposure coupled with high selectivity against off-targets.

Journal of Medicinal Chemistry published new progress about Allergic asthma. 21190-89-6 belongs to class pyridine-derivatives, name is Ethyl 6-chloropicolinate, and the molecular formula is C8H8ClNO2, Related Products of pyridine-derivatives.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Manteau, Baptiste published the artcileA General Approach to (Trifluoromethoxy)pyridines: first X-ray Structure Determinations and Quantum Chemistry Studies, Recommanded Product: 2-Chloro-3-(trifluoromethoxy)pyridine, the main research area is general approach synthesis Trifluoromethoxy pyridines crystal structure; ab initio energy profiles rotation trifluoromethoxy methoxy pyridines.

The previously unknown 2-, 3-, and 4-(trifluoromethoxy)pyridines have now become readily accessible by means of an efficient and straightforward large-scale synthesis. Their regioselective functionalization by organometallic methods has been studied and has afforded new and highly important building blocks for life-sciences-oriented research. In addition, the first X-ray crystallog. structure determinations of (trifluoromethoxy)pyridines have been performed. Lowest-energy conformations of (trifluoromethoxy)pyridines and (trifluoromethoxy)pyridinium cations were determined by in silico studies.

European Journal of Organic Chemistry published new progress about Anomeric effect. 1206980-39-3 belongs to class pyridine-derivatives, name is 2-Chloro-3-(trifluoromethoxy)pyridine, and the molecular formula is C6H3ClF3NO, Recommanded Product: 2-Chloro-3-(trifluoromethoxy)pyridine.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Ohmi, Masashi published the artcileIdentification of a novel 2-pyridyl-benzensulfonamide derivative, RQ-00203078, as a selective and orally active TRPM8 antagonist, Safety of 2-Chloro-3-fluoro-5-(trifluoromethyl)pyridine, the main research area is pyridylbenzensulfonamide derivative RQ00203078 preparation TRPM8 antagonist cold allodynia; structure activity TRPM8 antagonist pyridylbenzensulfonamide derivative RQ00203078; Cold allodynia; RQ-00203078; Sulfonamide; TRPM8 antagonist; Wet-dog shakes.

A novel series of 2-pyridyl-benzensulfonamide derivatives have been identified as selective and orally active TRPM8 antagonists via high throughput screening (HTS). Exploration of the structure-activity relationships of compound (I) has led to the identification of RQ-00203078 (compound 36) as a highly selective, potent and orally available TRPM8 antagonist. RQ-00203078 demonstrated excellent in vivo activity in a dose dependent manner with an ED50 value of 0.65 mg/kg in the icilin-induced wet-dog shakes model in rats after oral administration and may become an important pharmacol. tool for fully assessing the potential therapeutic use of the targets activated by cold stimulation.

Bioorganic & Medicinal Chemistry Letters published new progress about Allodynia (cold). 72600-67-0 belongs to class pyridine-derivatives, name is 2-Chloro-3-fluoro-5-(trifluoromethyl)pyridine, and the molecular formula is C6H2ClF4N, Safety of 2-Chloro-3-fluoro-5-(trifluoromethyl)pyridine.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Yang, Jie published the artcileThree water-soluble acylhydrazone tetranuclear transition metal complexes: Crystal structures, DNA/BSA interactions and cytotoxicity studies, Computed Properties of 24484-93-3, the main research area is transition metal acetylpyridinechloropyridinecarbonylhydrazone complex preparation DNA BSA binding anticancer; crystal structure transition metal acetylpyridinechloropyridinecarbonylhydrazone complex; Acylhydrazone; CT-DNA/BSA interaction; Cytotoxic activity; Transition metal complex.

2-Acetylpyridine-4-chloropyridine-2-carbonylhydrazone (C13H11ClN4O, HL) and its three water-soluble tetranuclear complexes [Cu4(NO3)2(L)4]·(NO3)2 (1), [Co4(NO3)2(H2O)(C2H5OH)(L)4]·(NO3)2 (2) and [Zn4(NO3)2(H2O)(C2H5OH)(L)4]·(NO3)2 (3) were synthesized and characterized showing that 1-3 were all tetranuclear complexes. The interactions of HL, 1-3 with calf thymus DNA (CT-DNA) and bovine serum albumin (BSA) were explored using UV-visible (UV-Vis) titration, fluorescence spectroscopy, microcalorimetry and mol. docking techniques. The UV-Vis spectroscopy measurements showed that complexes 1-3 could strongly bind to CT-DNA by the intercalation mode, while HL interacted with CT-DNA through groove binding. From the fluorescence spectroscopy results, the interaction between HL, 1-3 and BSA was a static quenching procedure, in which complexes 1-3 had two binding sites near Trp residues of BSA while HL only had one. The microcalorimetric studies revealed that the interactions of HL and 1-3 to CT-DNA/BSA were all endothermic and the duration of each interaction was all less than 30 min. The in silico mol. docking illustrated intermol. interactions of 1-3 binding with DNA/BSA included hydrogen bond, halogen bond, hydrophobic and electrostatic interactions. 3-(4,5-Dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay indicated that complex 1 possessed better cytotoxicity against HeLa, A549, MCF7 and HCT-116 than cisplatin and could be used as an alternative anticancer drug.

Journal of Inorganic Biochemistry published new progress about Antitumor agents. 24484-93-3 belongs to class pyridine-derivatives, name is Methyl 4-chloropicolinate, and the molecular formula is C7H6ClNO2, Computed Properties of 24484-93-3.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Chessari, Gianni published the artcileFragment-Based Drug Discovery Targeting Inhibitor of Apoptosis Proteins: Discovery of a Non-Alanine Lead Series with Dual Activity Against cIAP1 and XIAP, COA of Formula: C9H11ClN2, the main research area is inhibitor apoptosis protein antitumor neoplasm.

Inhibitor of apoptosis proteins (IAPs) are important regulators of apoptosis and pro-survival signaling pathways whose deregulation is often associated with tumor genesis and tumor growth. IAPs have been proposed as targets for anticancer therapy, and a number of peptidomimetic IAP antagonists have entered clin. trials. Using the fragment-based screening approach, the authors identified nonpeptidic fragments binding with millimolar affinities to both cellular inhibitor of apoptosis protein 1 (cIAP1) and X-linked inhibitor of apoptosis protein (XIAP). Structure-based hit optimization together with an anal. of protein-ligand electrostatic potential complementarity allowed us to significantly increase binding affinity of the starting hits. Subsequent optimization gave a potent nonalanine IAP antagonist I structurally distinct from all IAP antagonists previously reported. The lead compound had activity in cell-based assays and in a mouse xenograft efficacy model and represents a highly promising start point for further optimization.

Journal of Medicinal Chemistry published new progress about Antitumor agents. 1403899-44-4 belongs to class pyridine-derivatives, name is 6-Chloro-3,3-dimethyl-2,3-dihydro-1H-pyrrolo[3,2-c]pyridine, and the molecular formula is C9H11ClN2, COA of Formula: C9H11ClN2.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem