Tag: M.W=100-150

Pavia, Michael R. published the artcileN-Phenyl-N’-pyridinylureas as anticonvulsant agents, Recommanded Product: 4-Amino-2-picoline, the publication is Journal of Medicinal Chemistry (1990), 33(2), 854-61, database is CAplus and MEDLINE.

A series of N-phenyl-N‘-pyridinylureas, e.g., I (R, R¹, R², R³ = H, Cl, Br, F, CF₃, Me, Et, CHMe₂, NO₂, NH₂, OMe, etc.) was prepared by the reaction of aryl isocyanates with 2-, 3-, of 4-aminopyridine. They were examined for anticonvulsant activity. Extensive structure/activity investigations revealed optimal activity in the N-(2,6-disubstituted-phenyl)-N‘-(4-pyridinyl)urea series, with I (R = Cl, R¹ = R² = H, R³ = Me) (II) exhibiting the best overall anticonvulsant profile. II was effective against seizures induced by maximal electroshock but did not protect mice from clonic seizures produced by the convulsant pentylenetetrazol. The overall pharmacol. profile suggests that II would be of therapeutic use in the treatment of generalized tonic-clonic and partial seizures. II was selected for Phase 1 clin. trials.

Journal of Medicinal Chemistry published new progress about 18437-58-6. 18437-58-6 belongs to pyridine-derivatives, auxiliary class Pyridine,Amine, name is 4-Amino-2-picoline, and the molecular formula is C6H8N2, Recommanded Product: 4-Amino-2-picoline.

Referemce:
https://en.wikipedia.org/wiki/Pyridine,
Pyridine | C5H5N – PubChem

Tite, Tony published the artcileThe synthesis of 6-deazaformycin A, HPLC of Formula: 18437-58-6, the publication is Synlett (2009), 2927-2930, database is CAplus.

The synthesis of the new C-nucleoside 6-deazaformycin A was achieved through: the condensation of a suitably substituted lithiated 2-picoline with 2,3,5-tri-O-benzyl-D-ribonolactone; borohydride reduction of the resulting hemiacetals; followed by intramol. Mitsunobu cyclization of the carbinols; manipulation of the protecting groups, and subsequent ring closure to result in the formation of 7-amino-3-(β-D-ribofuranosyl)pyrazolo[4,3-b]pyridine.

Synlett published new progress about 18437-58-6. 18437-58-6 belongs to pyridine-derivatives, auxiliary class Pyridine,Amine, name is 4-Amino-2-picoline, and the molecular formula is C14H18BNO2S, HPLC of Formula: 18437-58-6.

Referemce:
https://en.wikipedia.org/wiki/Pyridine,
Pyridine | C5H5N – PubChem

Yang, Shaoning published the artcileDesign, synthesis and evaluation of substituted piperidine based KCNQ openers as novel antiepileptic agents, Computed Properties of 197958-29-5, the publication is Bioorganic & Medicinal Chemistry Letters (2018), 28(10), 1731-1735, database is CAplus and MEDLINE.

Epilepsy is a kind of disease with complicated pathogenesis. KCNQ (Kv7) is a voltage dependent potassium channel that is mostly associated with epilepsy and thus becomes an important target in the treatment of epilepsy. In this paper, a series of substituted piperidine derivatives targeting KCNQ were designed and synthesized by using scaffold hopping and active substructure hybridization. Compounds were evaluated by fluorescence-based thallium influx assay, Rb⁺ flow assay and electrophysiol. patch-clamp assay. Results showed that some compounds possessed more potent potassium channel opening activity than Retigabine. More significantly, compound I was found to have good pharmacokinetic profiles in vivo.

Bioorganic & Medicinal Chemistry Letters published new progress about 197958-29-5. 197958-29-5 belongs to pyridine-derivatives, auxiliary class Pyridine,Boronic acid and ester, name is 2-Pyridinylboronic acid, and the molecular formula is C8H11NO, Computed Properties of 197958-29-5.

Referemce:
https://en.wikipedia.org/wiki/Pyridine,
Pyridine | C5H5N – PubChem

Shi, Zhaojiang published the artcileElectrochemical oxidative dearomatization of 2-arylthiophenes, Application In Synthesis of 197958-29-5, the publication is Organic Chemistry Frontiers (2022), 9(11), 2921-2925, database is CAplus.

A green and sustainable electrochem. oxidative dearomatization of 2-arylthiophenes was reported. The variation of substitution patterns afforded easy access to both C2/C3 and C2/C5 difunctionalized dearomative dihydrothiophenes such as I [R = Ph, 3-FC₆H₄, 2-pyridyl, etc.; R¹ = OAc, OC(O)Et]. The synthetic utility of the resulting dihydrothiophenes was further demonstrated by the concise synthesis of a pyridazinone analog with interesting vasodilator activity.

Organic Chemistry Frontiers published new progress about 197958-29-5. 197958-29-5 belongs to pyridine-derivatives, auxiliary class Pyridine,Boronic acid and ester, name is 2-Pyridinylboronic acid, and the molecular formula is C18H28B2O4, Application In Synthesis of 197958-29-5.

Referemce:
https://en.wikipedia.org/wiki/Pyridine,
Pyridine | C5H5N – PubChem

Barraclough, Paul published the artcileInotropic ‘A’ ring substituted sulmazole and isomazole analogs, Synthetic Route of 33631-04-8, the main research area is inotropic sulmazole isomazole analog; imidazopyridine preparation inotropic.

A series of “”A”” ring substituted sulmazole I [R = 4-, 5-, 6-MeO, 5-NO2, 5-Cl, 5-Me, 5-Ac; X = S, S(O), O] and isomazole analogs II [R = 2-, 5-, 6-MeO, 5-NH2, 5-NO2; X = S, S(O), O] were prepared and evaluated as inotropic agents. Thus, 5-methoxy-2,3-pyridinediamine was cyclized with 2-methoxy-4-(methylthio)benzoic acid to give I (R = 5-MeO, X = S), which was oxidized to give I [R = 5-MeO, X = S(O)]. PKA’s, protonation sites, and log P values were measured for selected compounds and their electronic properties were calculated No simple correlation between inotropic activity and pKA, protonation site, or log P value was observed However, in vitro inotropism did correlate with the calculated charge d. of the “”B”” ring imidazo nitrogen atom. The 6-position of sulmazole appeared to be the most tolerant toward substituents, the 6-amino derivative I [R = 6-NH, X = S(O)] being a more potent inotrope than sulmazole itself. 4-Methoxyisomazole had comparable in vivo inotropic properties to those of isomazole.

Journal of Medicinal Chemistry published new progress about Inotropics. 33631-04-8 belongs to class pyridine-derivatives, name is 2-Methoxypyridine-3,4-diamine, and the molecular formula is C6H9N3O, Synthetic Route of 33631-04-8.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Barlin, G. B. published the artcileIonization constants of heterocyclic substances. IX. Protonation of aminopyridines and aminopyrimidinones, Product Details of C6H9N3O, the main research area is pyridines aminohydroxy ionization UV; basicity pyridines aminohydroxy; aminohydroxypyridine ionization UV; pyrimidines aminohydroxy ionization UV; protonation aminohydroxypyridine.

Ionization constants and uv spectra are reported for amino-2-hydroxypyridines (amino-2-pyridones), amino-4-hydroxypyridines(amino-4-pyridones), and amino-2,4-di-hydroxypryimidines (amino-2,4-pyrimidinediones) and their O-and ring N-Me derivatives Protonation of 3- and 5-amino-2-hydroxypyridines and 3,4-diamino-2-hydroxypyridine (I) occurs first at the amino group (the 3-NH2 of I), but 4- and 6-amino-2-hydroxypyridines and 2- and 3-amino-4-hydroxypyridines are protonated first at O. The most basic center of 4,5-diamino-2,6-dihydroxypyrimidine is the 5-NH2 group.

Journal of the Chemical Society [Section] B: Physical Organic published new progress about Ionization. 33631-04-8 belongs to class pyridine-derivatives, name is 2-Methoxypyridine-3,4-diamine, and the molecular formula is C6H9N3O, Product Details of C6H9N3O.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Roy, Patrick J. published the artcileThe Hemetsberger-Knittel synthesis of substituted 5-, 6-, and 7-azaindoles, HPLC of Formula: 71255-09-9, the main research area is pyrrolo pyridine azaindole preparation cyclization thermolysis pyridinyl azido propenoate; azido pyridine acrylate preparation thermal cyclization Hemetsberger Knittel; Hemetsberger Knittel synthesis azaindole thermolysis cyclization template.

A series of substituted 5-, 6-, and 7-azaindoles were prepared via the Hemetsberger-Knittel reaction. In general, better yields were obtained at higher temperatures and shorter reaction times than required for the formation of the analogous indoles, and in some cases, only decomposition occurred below a min. temperature The resulting templates offer up to five sites for subsequent functionalization to allow a wide range of chem. diversity.

Synthesis published new progress about Cyclization. 71255-09-9 belongs to class pyridine-derivatives, name is 2-Methoxynicotinaldehyde, and the molecular formula is C7H7NO2, HPLC of Formula: 71255-09-9.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Sidhu, Preetpal S. published the artcileDevelopment of Novel Vitamin D Receptor-Coactivator Inhibitors, Safety of 2-Methoxynicotinaldehyde, the main research area is novel vitamin D receptor coactivator inhibitor; 3-indolylmethanamines; CAMP; CYP24A1; HL60; VDR; Vitamin D receptor; apoptosis; fluorescence polarization; high throughput screening; steroid receptor coactivator.

Nuclear receptor coregulators are master regulators of transcription and selectively interact with the vitamin D receptor (VDR) to modulate cell differentiation, cell proliferation, and calcium homeostasis. Herein, we report the syntheses and evaluation of highly potent and selective VDR-coactivator inhibitors based on a recently identified 3-indolylmethanamine scaffold. The most active compound, PS121912, selectively inhibited VDR-mediated transcription among eight other nuclear receptors tested. PS121912 is also selectively disrupting the binding between VDR and the third nuclear receptor interaction domain of the coactivator SRC2. Genetic studies revealed that PS121912 behaves like a VDR antagonist by repressing 1,25-(OH)2D3 activated gene transcription. In addition, PS121912 induced apoptosis in HL-60.

ACS Medicinal Chemistry Letters published new progress about Homo sapiens. 71255-09-9 belongs to class pyridine-derivatives, name is 2-Methoxynicotinaldehyde, and the molecular formula is C7H7NO2, Safety of 2-Methoxynicotinaldehyde.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Jin, Cheng Hua published the artcileSynthesis and biological evaluation of 1-substituted-3-(6-methylpyridin-2-yl)-4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)pyrazoles as transforming growth factor-β type 1 receptor kinase inhibitors, Related Products of pyridine-derivatives, the main research area is ALK5 inhibition triazolopyridinylpyrazole pyridinyl preparation.

A series of 1-substituted-3-(6-methylpyridin-2-yl)-4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)pyrazoles has been prepared and evaluated for their ALK5 inhibitory activity in an enzyme assay and in a cell-based luciferase reporter assay. 4-([1,2,4]Triazolo[1,5-a]pyridin-6-yl)-N-(4-methoxyphenyl)-3-(6-methylpyridin-2-yl)-1H-pyrazole-1-carbothioamide (I) inhibited ALK5 phosphorylation with IC50 value of 0.57 nM and showed 94% inhibition at 100 nM in a luciferase reporter assay using HaCaT cells permanently transfected with p3TP-luc reporter construct.

Bioorganic & Medicinal Chemistry Letters published new progress about Homo sapiens. 614750-81-1 belongs to class pyridine-derivatives, name is [1,2,4]Triazolo[1,5-a]pyridine-6-carbaldehyde, and the molecular formula is C7H5N3O, Related Products of pyridine-derivatives.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Trecourt, Francois published the artcileSynthesis of diazaxanthones: 5H-pyrano[2,3b:6,5-b’]dipyridin-5-one and 5H-thiopyrano[2,3-b:6,5-b’]dipyridin-5-one, Computed Properties of 71255-09-9, the main research area is pyranodipyridinone; thiopyranodipyridinone; formylation bromopyridine; pyridinecarboxaldehyde conformation.

The title compds (I; X = O, S, resp.) were prepared in 5 and 6 steps, resp., from 3-bromo-2-chloropyridine; yields were excellent. The CO bridge of the diazaxanthones was formed by coupling the aldehydes II (X = O) with 3-lithio-2-methoxypyridine and II (X = S) with 3-lithio-2-(methylthio)pyridine followed by oxidation of the resulting benzylic alc. The other bridge was formed by coupling the 2 ether or sulfide functions with pyridinium-HCl at ∼220°. The conformations of II (X = O, S) are discussed. II (X = O, S) were prepared by treatment of the 3-bromo analogs with BuLi and HCO2Et. I are the 1st reported xanthone-like heterocycles with 2 pyridine rings condensed to the 4-pyrone or -thiopyrone ring.

Journal of Chemical Research, Synopses published new progress about Cyclization. 71255-09-9 belongs to class pyridine-derivatives, name is 2-Methoxynicotinaldehyde, and the molecular formula is C7H7NO2, Computed Properties of 71255-09-9.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem