Tag: M.W=200-250

Palat, K. Jr.; Braunerova, G.; Miletin, M.; Buchta, V. published the artcile< Synthesis and antifungal activity of alkyl and arylsulfanylpyridinylguanidines>, Recommanded Product: 2-Bromo-6-chloropyridin-3-amine, the main research area is pyridinylguanidine alkylsulfanyl derivative preparation antifungal activity; pyridylguanidine arylsulfanyl derivative preparation antimicrobial activity.

A series of alkyl- and arylsulfanylpyridylguanidines was synthesized and their antimicrobial activity was evaluated in vitro against eight potentially pathogenic strains of fungi. Compounds with an alkylsulfanyl substitution have antifungal activity, which improves with increasing length of the aliphatic chain.

Chemical Papers published new progress about Antimicrobial agents. 1050501-88-6 belongs to class pyridine-derivatives, and the molecular formula is C5H4BrClN2, Recommanded Product: 2-Bromo-6-chloropyridin-3-amine.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Caron, Stephane; Do, Nga M.; Sieser, Janice E.; Whritenour, David C.; Hill, Paul D. published the artcile< Preparation of a Corticotropin-Releasing Factor Antagonist by Nucleophilic Aromatic Substitution and Copper-Mediated Ether Formation>, Formula: C9H9Cl2NO2, the main research area is butylamino aryloxy nicotinate preparation process development drug candidate; corticotropin releasing factor antagonist preparation process development drug candidate; nucleophilic aromatic substitution ether formation copper drug candidate preparation.

Several synthetic approaches to a corticotropin-releasing factor (CRF) antagonist containing a tetrasubstituted pyridine (I) were evaluated. In particular, nucleophilic aromatic substitutions on 2,4-dichloropyridine derivatives were attempted using 2,6-dimethyl-4-chlorophenol, (S)-2-aminobutanol, and several sulfur nucleophiles. It was found that a copper-mediated coupling of a phenoxymesylate was preferred for preparation of the diarylether followed by nucleophilic aromatic substitution to introduce the amine side chain, affording the desired drug candidate (I) in two steps from the com. available Me 2,4-dichloro-6-methylnicotinate.

Organic Process Research & Development published new progress about Etherification. 86129-63-7 belongs to class pyridine-derivatives, and the molecular formula is C9H9Cl2NO2, Formula: C9H9Cl2NO2.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

De Bon, Francesco; Abreu, Carlos M. R.; Serra, Armenio C.; Gennaro, Armando; Coelho, Jorge F. J.; Isse, Abdirisak A. published the artcile< Catalytic Halogen Exchange in Supplementary Activator and Reducing Agent Atom Transfer Radical Polymerization for the Synthesis of Block Copolymers>, Related Products of 1762-41-0, the main research area is halogen exchange activator reducing agent ATRP block copolymer; ATRP; block copolymerization; catalytic halogen exchange; copper catalyst; supplemental activator.

Synthesis of block copolymers (BCPs) by catalytic halogen exchange (cHE) is reported, using supplemental activator and reducing agent Atom Transfer Radical Polymerization (SARA ATRP). The cHE mechanism is based on the use of a small amount of a copper catalyst in the presence of a suitable excess of halide ions, for the synthesis of block copolymers from macroinitiators with monomers of mismatching reactivity. cHE overcomes the problem of inefficient initiation in block copolymerizations in which the second monomer provides dormant species that are more reactive than the initiator. Model macroinitiators with low dispersity are prepared and extended to afford well-defined block copolymers of various compositions Combined cHE/SARA ATRP is therefore a simple and potent polymerization tool for the copolymerization of a wide range of monomers allowing the production of tailored block copolymers.

Macromolecular Rapid Communications published new progress about Atom transfer radical polymerization catalysts. 1762-41-0 belongs to class pyridine-derivatives, and the molecular formula is C10H6Cl2N2, Related Products of 1762-41-0.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Mancuso, Raffaella; Novello, Mariangela; Russo, Patrizio; Palumbo Piccionello, Antonio; Gabriele, Bartolo published the artcile< Iodolactonization of 3-Alkynylthiophene-2-Carboxylic and 3-Alkynylpicolinic Acids for the Synthesis of Fused Heterocycles>, Name: Methyl 3-bromo-2-pyridinecarboxylate, the main research area is fused heterocycle preparation iodolactonization alkynylthiophenecarboxylate alkynylpicolinate.

The iodolactonization of 3-alkynylthiophene-2-carboxylic acids and 3-alkynylpicolinic acids was studied. Using I2 as the iodine source and NaHCO3 as the base in MeCN, the process took place smoothly to afford thienopyranones and pyranopyridinones, resp., from 6-endo-dig cyclization. The method also worked nicely for the transformation of 2-(phenylethynyl)thiophene-3-carboxylic acid and 3-(phenylethynyl)isonicotinic acid into 7-iodo-6-phenyl-4H-thieno[3,2-c]pyran-4-one and 4-iodo-3-phenyl-1H-pyrano[4,3-c]pyridin-1-one, resp. Although with some 3-alkynylpicolinic acids the process led to a mixture of the 6-endo-dig and 5-exo-dig products, it could be still made selective toward the pyranopyridinone compound working in 1-ethyl-3-methylimidazolium Et sulfate as the solvent. However, the exclusive formation of the 5-exo-dig product was observed in N-ethyl-N-methylmorpholinium dicyanamide starting from 3-(3,3-dimethylbut-1-yn-1-yl)picolinic acid. Some representative iodinated thienopyridinone products were successfully used as substrates for Pd-catalyzed Suzuki and Sonogashira reactions.

European Journal of Organic Chemistry published new progress about Carboxylic acids Role: RCT (Reactant), RACT (Reactant or Reagent) (3-Alkynylthiophene-2-Carboxylic Acids). 53636-56-9 belongs to class pyridine-derivatives, and the molecular formula is C7H6BrNO2, Name: Methyl 3-bromo-2-pyridinecarboxylate.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Ager, E.; Chivers, G. E.; Suschitzky, H. published the artcile< Photolysis of pentachloropyridine and pentachloropyridine 1-oxide>, Related Products of 14121-36-9, the main research area is chloropyridine irradiation; lithium chloropyridine; substitution nucleophilic chloropyridine; cleavage chloropyridine oxide photolysis.

Irradiation of pentachloropyridine in dioxane, Et2O, or cyclohexane gave 2,3,4,6-tetrachloropyridine (I), but irradiation of pentachloropyridine N-oxide in CCl4 gave Cl2C:CClCCl:CClNCO. I and BuLi gave (tetrachloro-3-pyridyl)lithium. With nucleophilic reagents I underwent substitution reactions; e.g., I with NaOH-MeOH gave 61% 2,3,6-trichloro-4-methoxypyridine.

Journal of the Chemical Society, Chemical Communications published new progress about Ring opening. 14121-36-9 belongs to class pyridine-derivatives, and the molecular formula is C5HCl4N, Related Products of 14121-36-9.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Remya, Chandran; Dileep, K. V.; Koti Reddy, Eeda; Mantosh, Kumar; Lakshmi, Kesavan; Sarah Jacob, Reena; Sajith, Ayyiliyath M.; Jayadevi Variyar, E.; Anwar, Shaik; Zhang, Kam Y. J.; Sadasivan, C.; Omkumar, R. V. published the artcile< Neuroprotective derivatives of tacrine that target NMDA receptor and acetyl cholinesterase - Design, synthesis and biological evaluation>, SDS of cas: 329214-79-1, the main research area is aminotetrahydroacridine preparation NMDA receptor antagonist cholinesterase inhibition SAR docking; AChE, acetylcholinesterase; AChEIs, acetylcholinesterase inhibitors; AChT, acetylthiocholine; AD, Alzheimer’s disease; ADME, absorption, distribution, metabolism and excretion; Acetylcholinesterase; Alzheimer’s disease; BBB, blood brain barrier; Ca2+, calcium; ChE, Cholinesterases; DMEM, Dulbecco’s modified Eagle’s medium; DTNB, 5,5-dithiobis-(2-nitrobenzoic acid); ENM, elastic network modeling; ER, endoplasmic reticulum; FRET, fluorescence resonance energy transfer; G6PD, glucose-6-phosphate dehydrogenase; HBSS, Hank’s balanced salt solution; IP, intraperitoneal; LBD, Ligand binding domain; LC-MS, Liquid chromatography-mass spectrometry; LiCABEDS, Ligand Classifier of Adaptively Boosting Ensemble Decision Stumps; MAP2, microtubule associated protein 2; MD, Molecular dynamics; MTDLs; MTDLs, multi-target directed ligands; MWM, Morris water maze; NBM, neurobasal medium; NMA, normal mode analysis; NMDA receptor; NMDAR, N-methyl-D-aspartate receptor; Neuroprotection; OPLS, Optimized potential for liquid simulations; PBS, phosphate-buffered saline; PFA, paraformaldehyde; Polypharmacology; RMSD, root mean square deviation; SAR, structure-activity relationships; SD, standard deviation; SVM, support vector machine; Structure-based drug design; TBI, traumatic brain injury; TMD, transmembrane domain; Tacrine; h-NMDAR, human NMDAR; hAChE, human AChE; ppm, parts per million.

An novel high affinity multi-target directed ligands (MTDLs) against AChE and NMDAR, with reduced hepatotoxicity, performed in-silico structure-based modifications on tacrine, chem. synthesis of the derivatives and in-vitro validation of their activities. Nineteen such derivatives I [R = H, methylcarbamoyl, hydrazinecarbonyl, ethoxycarbonyl; R1 = 2-furanyl, 1-methylpyrazol-4-yl, 2-FC6H4, etc.] showed inhibition with IC50 values in the range of 18.53 ± 2.09 – 184.09 ± 19.23 nM against AChE and 0.27 ± 0.05 – 38.84 ± 9.64μM against NMDAR. Some of the selected compounds protected rat primary cortical neurons from glutamate induced excitotoxicity. Two of the tacrine derived MTDLs, I [R = H, R1 = 1-methylpyrazol-4-yl; R = H, R1 = 2-FC6H4] exhibited in-vivo efficacy in rats by protecting against behavioral impairment induced by administration of the excitotoxic agent, monosodium glutamate. Addnl., several of these synthesized compounds also exhibited promising inhibitory activitiy against butyrylcholinesterase. MTDL-201 I [R = H, R1 = 1-methylpyrazol-4-yl] was also devoid of hepatotoxicity in-vivo. Given the therapeutic potential of MTDLs in disease-modifying therapy, studies revealed several promising MTDLs among which I [R = H, R1 = 1-methylpyrazol-4-yl] appeared to be a potential candidate for immediate preclin. evaluations.

Computational and Structural Biotechnology Journal published new progress about Aminoacridines Role: PAC (Pharmacological Activity), RCT (Reactant), SPN (Synthetic Preparation), THU (Therapeutic Use), BIOL (Biological Study), RACT (Reactant or Reagent), PREP (Preparation), USES (Uses). 329214-79-1 belongs to class pyridine-derivatives, and the molecular formula is C11H16BNO2, SDS of cas: 329214-79-1.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Noori, Maryam; Shafaatian, Bita; Notash, Behrouz published the artcile< Synthesis of new platinum(IV) complexes through breaking disulfide bond; crystal structure determination, electrochemical, photoluminescence and DNA interaction investigation>, Recommanded Product: 1,2-Di(pyridin-2-yl)disulfane, the main research area is mercaptopyridinyl platinacycle preparation electrochem fluorescence DNA binding; crystal structure aryl mercaptopyridinyl platinacycle; mol structure aryl mercaptopyridinyl platinacycle.

New Pt(IV) complexes containing N2S2 donor atoms were synthesized by the reactions of [Pt(p-MeC6H4)2(SMe2)2] and [PtCl2(DMSO)2] with 2,2′-dithiopyridine (dtp) in 1:1 M ratio. In these reactions, 2-mercaptopyridine (mpy) ligands were formed through the cleavage of the disulfide bond in 2,2′-dithiopyridine. The mpy ligands were coordinated to the Pt center via the N and S atoms and the obtained Pt(IV) complexes exhibited octahedral geometry. The complexes were characterized by FTIR, 1H NMR, UV-visible, elemental analyses and conductometry. The crystal structure of the arylplatinum(IV) complex containing C2N2S2 donor atoms was determined by single crystal x-ray diffraction. The obtained molar conductance values revealed that the Pt(IV) complexes were nonelectrolytes. The interactions of the complexes with calf thymus DNA (CT-DNA) were studied by absorption and fluorescence spectroscopy, cyclic voltammetry and viscometry methods. The intrinsic binding constants (Kb) of the complexes with CT-DNA, obtained from UV-visible absorption data, were 9.60 × 104 M-1 and 11.56 × 104 M-1. Also, the enthalpy and entropy of the interaction between the Pt(IV) complexes and CT-DNA were calculated The obtained data revealed pos. enthalpy and entropy changes indicating a hydrophobic interaction between these complexes and CT-DNA.

Inorganica Chimica Acta published new progress about Bond cleavage (disulfide). 2127-03-9 belongs to class pyridine-derivatives, and the molecular formula is C10H8N2S2, Recommanded Product: 1,2-Di(pyridin-2-yl)disulfane.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Degorce, Sebastien L.; Aagaard, Anna; Anjum, Rana; Cumming, Iain A.; Diene, Coura R.; Fallan, Charlene; Johnson, Tony; Leuchowius, Karl-Johan; Orton, Alexandra L.; Pearson, Stuart; Robb, Graeme R.; Rosen, Alan; Scarfe, Graeme B.; Scott, James S.; Smith, James M.; Steward, Oliver R.; Terstiege, Ina; Tucker, Michael J.; Turner, Paul; Wilkinson, Stephen D.; Wrigley, Gail L.; Xue, Yafeng published the artcile< Improving metabolic stability and removing aldehyde oxidase liability in a 5-azaquinazoline series of IRAK4 inhibitors>, Electric Literature of 329214-79-1, the main research area is preparation azaquinazoline derivative IRAK4 inhibitor pharmacokinetics; 5-Azaquinazoline; Aldehyde oxidase; DLBCL; IRAK4.

In this article, we report our efforts towards improving in vitro human clearance in a series of 5-azaquinazolines through a series of C4 truncations and C2 expansions. Extensive DMPK studies enabled us to tackle high Aldehyde Oxidase (AO) metabolism and unexpected discrepancies in human hepatocyte and liver microsomal intrinsic clearance. Our efforts culminated with the discovery of 5-azaquinazoline I, which also displayed exquisite selectivity for IRAK4, and showed synergistic in vitro activity against MyD88/CD79 double mutant ABC-DLBCL in combination with the covalent BTK inhibitor acalabrutinib.

Bioorganic & Medicinal Chemistry published new progress about Amines Role: RCT (Reactant), RACT (Reactant or Reagent). 329214-79-1 belongs to class pyridine-derivatives, and the molecular formula is C11H16BNO2, Electric Literature of 329214-79-1.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Podeschwa, Michael A. L.; Rossen, Kai published the artcile< Efficient Access to Methyl-1-hydroxy-2-naphthoates and Heterocyclic Analogues>, HPLC of Formula: 53636-56-9, the main research area is naphthoate hydroxy heterocyclic analog preparation; Heck coupling halobenzoate butenoate Dieckmann cyclization.

We report the synthesis of Me 1-hydroxy-2-naphthoate derivatives and heterocyclic analogs using a two-step approach. This short route employs a Heck coupling of a 2-halobenzoate with Me 3-butenoate followed by a Dieckmann cyclization, yielding the 1-hydroxynaphthalene-2-carboxylic acid derivatives in the multigram scale.

Organic Process Research & Development published new progress about Dieckmann condensation. 53636-56-9 belongs to class pyridine-derivatives, and the molecular formula is C7H6BrNO2, HPLC of Formula: 53636-56-9.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Epsztajn, J.; Plotka, M. W.; Grabowska, A. published the artcile< Application of organolithium compounds in organic synthesis. Part 19. Synthetic strategies based on aromatic metalation. A concise regiospecific synthesis of 3-halogenated picolinic and isonicotinic acids>, Reference of 53636-56-9, the main research area is picolinic acid halogenated preparation; isonicotinic acid halogenated preparation; halogenated picolinic isonicotinic acid preparation.

The synthesis of the halogenated picolin- and isonicotinanilides I (R = Cl, Br, iodo, X = N, Y = CH; X = CH, Y = N) (II) via metalation (n-BuLi) of the anilides I (R = H) and then the reaction of the generated bis-lithiated anilides with halogenating agents (CCl3-CCl3, CH2Br-CH2Br, I2) followed by subsequent acidic hydrolysis of II, as a way of regiospecific transformation of picolinic and isonicotinic acids into their C3-halogenated derivatives, is described.

Synthetic Communications published new progress about Regiochemistry. 53636-56-9 belongs to class pyridine-derivatives, and the molecular formula is C7H6BrNO2, Reference of 53636-56-9.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem