Category: 22280-62-2

Lougiakis, Nikolaos; Marakos, Panagiotis; Poul, Nicole; Balzarini, Jan published the artcile< Synthesis and antiviral activity evaluation of some novel acyclic C-nucleosides>, Formula: C6H7N3O2, the main research area is pyrazolopyridine acyclonucleoside preparation antiviral antitumor.

The preparation of novel 5-amino or 7-hydroxy substituted pyrazolo[4,3-b]pyridine and pyrazolo[3,4-c]pyridine acyclic C-nucleosides is described. Their synthesis was carried out by condensation of suitably substituted lithiated picolines with 2-benzyloxyethoxymethylchloride followed by pyrazole ring annulation. The compounds were evaluated for their antiviral activity against a wide panel of viruses, but were found inactive at subtoxic concentrations

Chemical & Pharmaceutical Bulletin published new progress about Acyclonucleosides Role: PAC (Pharmacological Activity), SPN (Synthetic Preparation), BIOL (Biological Study), PREP (Preparation). 22280-62-2 belongs to class pyridine-derivatives, and the molecular formula is C6H7N3O2, Formula: C6H7N3O2.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Ritter, Helmut; Kaiser, M. published the artcile< Proton NMR spectra of nitrated aminopyridines>, Recommanded Product: 6-Amino-3-nitro-2-picoline, the main research area is NMR nitrated aminopyridine hydrogen bond; pyridine aminonitro NMR; steric hindrance hydrogen bond aminonitropyridine.

The 1H NMR spectra of 26 nitrated aminopyridines were measured and interpreted. Chem. shift assignments were based on existing chem. shift rules for substituted pyridines and spectral comparison with compounds of similar structure. Some o-aminonitropyridines were found to give a splitting of the amino signals due to intermol. hydrogen bonding; steric hindrance is shown to influence this bonding.

Magnetic Resonance in Chemistry published new progress about Intramolecular hydrogen bond. 22280-62-2 belongs to class pyridine-derivatives, and the molecular formula is C6H7N3O2, Recommanded Product: 6-Amino-3-nitro-2-picoline.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Weglinski, Zbigniew; Talik, Tadeusz published the artcile< Carboxylation of 2-hydroxypicolines>, Safety of 6-Amino-3-nitro-2-picoline, the main research area is carboxylation hydroxypicoline; pyridinol methyl carboxylation; picoline hydroxy carboxylation; pyridinecarboxylic acid hydroxymethyl.

Treatment of a mixture of 2-hydroxy-3-methylpyridine (I) and anhydrous K2CO3 with 55 atm CO2 at 220° for 9 h gave 87% 2-hydroxy-3-methyl-5-pyridinecarboxylic acid (II). Carboxylation of the Na and K salts of I gave 49.5 and 53% II, resp. Similarly, 2-hydroxy-5-methyl-, 2-hydroxy-6-methyl-, and 2-hydroxy-4-methylpyridine gave 2-hydroxy-5-methyl-3-pyridinecarboxylic acid, 2-hydroxy-6-methyl-3-pyridinecarboxylic acid, and 2-hydroxy-4-methyl-5-pyridinecarboxylic acid, resp. The isomeric hydroxymethylpyridinecarboxylic acids were also prepared by hydrolysis of the corresponding isomeric chlorocyanopicolines. The latter were obtained from isomeric aminopicolines by successive nitration, hydroxylation, chlorination, reduction, and Sandmeyer cyanation.

Roczniki Chemii published new progress about Carboxylation. 22280-62-2 belongs to class pyridine-derivatives, and the molecular formula is C6H7N3O2, Safety of 6-Amino-3-nitro-2-picoline.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Palasek, B.; Puszko, A.; Biedrzycka, Z.; Sicinska, W.; Witanowski, M. published the artcile< Nitrogen NMR shieldings of 2-amino-5-nitro-6-methylpyridines>, Application In Synthesis of 22280-62-2, the main research area is aminonitromethylpyridine NMR shielding.

Nitrogen NMR shieldings (chem. shifts) of 2-amino-5-nitro-6-methylpyridine derivatives are assessed from the point of view of substituent-induced effects under conditions where alkyl, aryl, nitro, and nitroso moieties are substituents at the amino nitrogen. The nitro nitrogen shielding reveals only little variation upon varying the substituents, and this seems to indicate that steric hindrance which is likely to force the nitro group out of the plane of the aromatic ring reduces the π-electron conjugation with the latter, and with the amino group as well. On the other side, the pyridine nitrogen shielding shows large effects of substituents at the amino moiety, which suggests a significant conjugation between the ring and the amino group. The latter effects produce a remarkable deshielding of the pyridine nitrogen in the case of nitro and nitroso substituents at the amino group.

Spectroscopy (Amsterdam) published new progress about NMR (nuclear magnetic resonance). 22280-62-2 belongs to class pyridine-derivatives, and the molecular formula is C6H7N3O2, Application In Synthesis of 22280-62-2.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Lougiakis, Nikolaos; Marakos, Panagiotis; Pouli, Nicole; Balzarini, Jan published the artcile< Synthesis and antiviral activity evaluation of some novel acyclic C-nucleosides [Erratum to document cited in CA149:402608]>, Quality Control of 22280-62-2, the main research area is erratum pyrazolopyridine acyclonucleoside preparation antiviral antitumor.

On page 775, in the author list, the third author, Nicole Pouli, was incorrectly given as “”Nicole Poul””.

Chemical & Pharmaceutical Bulletin published new progress about Acyclonucleosides Role: PAC (Pharmacological Activity), SPN (Synthetic Preparation), BIOL (Biological Study), PREP (Preparation). 22280-62-2 belongs to class pyridine-derivatives, and the molecular formula is C6H7N3O2, Quality Control of 22280-62-2.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Romines, Karen R.; Freeman, George A.; Schaller, Lee T.; Cowan, Jill R.; Gonzales, Steve S.; Tidwell, Jeffrey H.; Andrews, Clarence W. III; Stammers, David K.; Hazen, Richard J.; Ferris, Robert G.; Short, Steven A.; Chan, Joseph H.; Boone, Lawrence R. published the artcile< Structure-Activity Relationship Studies of Novel Benzophenones Leading to the Discovery of a Potent, Next Generation HIV Nonnucleoside Reverse Transcriptase Inhibitor>, Synthetic Route of 22280-62-2, the main research area is AntiAIDS reverse transcriptase inhibitor benzophenone preparation structure activity HIV1; AIDS antiviral reverse transcriptase inhibitor benzophenone preparation HIV1.

Despite the progress of the past two decades, there is still considerable need for safe, efficacious drugs that target human immunodeficiency virus (HIV). This is particularly true for the growing number of patients infected with virus resistant to currently approved HIV drugs. Our high throughput screening effort identified a benzophenone template as a potential nonnucleoside reverse transcriptase inhibitor (NNRTI). This manuscript describes our extensive exploration of the benzophenone structure-activity relationships, which culminated in the identification of several compounds with very potent inhibition of both wild type and clin. relevant NNRTI-resistant mutant strains of HIV. These potent inhibitors include 70h (GW678248), which has in vitro antiviral assay IC50 values of 0.5 nM against wild-type HIV, 1 nM against the K103N mutant associated with clin. resistance to efavirenz, and 0.7 nM against the Y181C mutant associated with clin. resistance to nevirapine. Compound 70h has also demonstrated relatively low clearance in i.v. pharmacokinetic studies in three species, and it is the active component of a drug candidate which has progressed to phase 2 clin. studies.

Journal of Medicinal Chemistry published new progress about AIDS (disease). 22280-62-2 belongs to class pyridine-derivatives, and the molecular formula is C6H7N3O2, Synthetic Route of 22280-62-2.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Filla, Sandra A.; Mathes, Brian M.; Johnson, Kirk W.; Phebus, Lee A.; Cohen, Marlene L.; Nelson, David L.; Zgombick, John M.; Erickson, Jon A.; Schenck, Kathryn W.; Wainscott, David B.; Branchek, Theresa A.; Schaus, John M. published the artcile< Novel Potent 5-HT1F Receptor Agonists: Structure-Activity Studies of a Series of Substituted N-[3-(1-Methyl-4-piperidinyl)-1H-pyrrolo[3,2-b]pyridin-5-yl]amides>, Formula: C6H7N3O2, the main research area is pyrrolopyridine amido sulfonamido preparation 5HT receptor agonist migraine; pyrrolopyrimidine amido preparation 5HT receptor agonist migraine.

5-Amidoindole I [X = Y = CH, R = 4-FC6H4; (II)] (LY334370), a selective 5-HT1F receptor agonist (SSOFRA), inhibited dural inflammation in the neurogenic plasma protein extravasation model of migraine and demonstrated clin. efficacy for the acute treatment of migraine. Although II was greater than 100-fold selective over both the 5-HT1B and 5-HT1D receptors, it exhibited appreciable 5-HT1A receptor affinity. Thus, a series of pyrrolo[2,3-c]pyridines I (X = N; Y = CH; R = Me, 4-FC6H4) and pyrrolo[3,2-b]pyridines I (X = CH; Y = N; R = Me, Et, Ph, 3-thienyl, 2-furyl, 2-pyridyl, cyclopropyl, etc.) as well as pyrrolo[3,2-d]pyrimidines I (X = Y = N; R = Me, 4-FC6H4) were synthesized as analogs of II and evaluated in an effort to identify SSOFRAs with improved selectivity over other 5-HT1 receptor subtypes. I (X = CH, Y = N, R = 4-FC6H4) showed high 5-HT1F receptor affinity but offered no improvement in selectivity compared to II; however, I (X = CH, Y = N, R = Me) was greater than 100-fold selective over the 5-HT1A, 5-HT1B, and 5-HT1D receptors. SAR studies of this series determined that alkylamides in particular exhibited high selectivity for the 5-HT1F receptor. These SAR studies identified SSOFRAs that demonstrated oral activity in the neurogenic plasma protein extravasation model, a model indicative of antimigraine activity.

Journal of Medicinal Chemistry published new progress about 5-HT1 agonists. 22280-62-2 belongs to class pyridine-derivatives, and the molecular formula is C6H7N3O2, Formula: C6H7N3O2.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Smolyar, N. N.; Yutilov, Yu. M. published the artcile< Reduction of 2-amino-3- and -5-nitropyridine derivatives with hydrazine hydrate>, Name: 6-Amino-3-nitro-2-picoline, the main research area is nitropyridinamine reduction hydrazine hydrate; pyridinamine preparation.

The reactions of 3- and 5-nitro-2-pyridinamine with N2H4.H2O resulted in elimination of the NH2 group and reduction of the NO2 group with formation of 3-pyridinamine. A probable reaction mechanism involves addition of N2H4.H2O to the N-C(2) bond, followed by elimination of NH3 and reduction of the NO2 group to NH2. 4- And 5-methyl-3-nitro-2-pyridinamine reacted with N2H4.H2O in a similar way.

Russian Journal of Organic Chemistry published new progress about Aromatic amines Role: RCT (Reactant), SPN (Synthetic Preparation), RACT (Reactant or Reagent), PREP (Preparation). 22280-62-2 belongs to class pyridine-derivatives, and the molecular formula is C6H7N3O2, Name: 6-Amino-3-nitro-2-picoline.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Timperley, Christopher M.; Banks, R. Eric; Young, Ian M.; Haszeldine, Robert N. published the artcile< Synthesis of some fluorine-containing pyridinealdoximes of potential use for the treatment of organophosphorus nerve-agent poisoning>, SDS of cas: 22280-62-2, the main research area is fluorinated pyridinealdoxime preparation treatment organophosphorus nerve agent poisoning; sarin poisoning fluorinated pyridinealdoxime preparation treatment.

Fluoroheterocyclic aldoximes were screened as therapeutic agents for the treatment of anticholinesterase poisoning. 2-Fluoropyridine-3- and -6-aldoxime and 3-fluoropyridine-2- and -4-aldoxime were synthesized. Attempts to obtain 3,5,6-trifluoropyridine-2,4-bis(aldoxime) and -2-aldoxime, however, proved unsuccessful. Pentafluorobenzaldoxime was prepared by oximation of pentafluorobenzaldehyde. Acid dissociation constants (pKa) and second-order rate constants (kox-) of the fluorinated pyridinealdoximes towards sarin were measured. 2,3,5,6-Tetrafluoropyridine-4-aldoxime had the best profile: its kox- approached that of the therapeutic oxime P2S (310 vs. 120 l mol-1 min-1), but its higher pKa (9.1 vs. 7.8) fell short of the target figure of 8 required for reactivation of inhibited acetylcholinesterase in vivo. N-alkylation of the fluorinated pyridine-aldoximes may reduce their pKa nearer to 8 and enhance their therapeutic potential.

Journal of Fluorine Chemistry published new progress about Antidotes. 22280-62-2 belongs to class pyridine-derivatives, and the molecular formula is C6H7N3O2, SDS of cas: 22280-62-2.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Blache, Yves; Gueiffier, Alain; Chavignon, Olivier; Viols, Henry; Teulade, Jean Claude; Chapat, Jean Pierre published the artcile< Compared reactivity of 3-, 5-, 6-, and 8-aminoimidazo[1,2-α]pyridines in Combes reaction: access to imidazonaphthyridines and dipyrido[1,2-a:3',2'-d]imidazole>, Application of C6H7N3O2, the main research area is aminoimidazopyridine Combes reaction; imidazonaphthyridine; dipyridoimidazole.

The synthesis of imidazo[1,2-a][1,8]naphthyridines and dipyrido[1,2-a:3′,2′-d]imidazole by treatment of aminoimidazo[1,2-a]pyridines following the Combes procedure is described.

Heterocycles published new progress about 22280-62-2. 22280-62-2 belongs to class pyridine-derivatives, and the molecular formula is C6H7N3O2, Application of C6H7N3O2.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem