Month: December 2022

Simler, Thomas published the artcileDirect synthesis of doubly deprotonated, dearomatised lutidine PNP Cr and Zr pincer complexes based on isolated K and Li ligand transfer reagents, Category: pyridine-derivatives, the publication is Dalton Transactions (2016), 45(7), 2800-2804, database is CAplus and MEDLINE.

Chromium and zirconium complexes with dearomatized double deprotonated 2,6-bis[(di-tert-butylphosphino)methyl]pyridine were prepared by transmetalation of potassium and lithium salts. Double deprotonation of 2,6-bis-(di-tert-butylphosphinomethyl)-pyridine (^tBuPN^tBuP), with KCH₂C₆H₅ afforded K₂(^tBuP*N_a^tBuP*), N_a = anionic amido N, ^tBuP* = di-tert-Bu vinylic P donor. The analogous [Li₂(^tBuP*N_a^tBuP*)]₂ (1) was reacted with [CrCl₂(THF)₂] and [ZrCl₄(THT)₂] to give the helical [Cr{Cr(^tBuP*N_a^tBuP*)Cl}₂] (2) and [Zr(^tBuP*N_a^tBuP*)Cl₂] (3), resp. DFT calculations support dearomatization of P*N_aP* and its high donor ability.

Dalton Transactions published new progress about 338800-13-8. 338800-13-8 belongs to pyridine-derivatives, auxiliary class Bis-phosphine Ligands, name is 2,6-Bis((di-tert-butylphosphino)methyl)pyridine, and the molecular formula is C10H16Br3N, Category: pyridine-derivatives.

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

Yart, Lucile published the artcileDual effect of nifedipine on pregnant human myometrium contractility: Implication of TRPC1, HPLC of Formula: 21829-25-4, the publication is Journal of Cellular Physiology (2022), 237(3), 1980-1991, database is CAplus and MEDLINE.

Nifedipine, an L-type voltage-gated Ca²⁺ channel (L-VGCC) blocker, is one of the most used tocolytics to treat preterm labor. In clin. practice, nifedipine efficiently decreases uterine contractions, but its efficacy is limited over time, and repeated or maintained nifedipine-based tocolysis appears to be ineffective in preventing preterm birth. We aimed to understand why nifedipine has short-lasting efficiency for the inhibition of uterine contractions. We used ex vivo term pregnant human myometrial strips treated with cumulative doses of nifedipine. We observed that nifedipine inhibited spontaneous myometrial contractions in tissues with high and regular spontaneous contractions. By contrast, nifedipine appeared to increase contractions in tissues with low and/or irregular spontaneous contractions. To investigate the mol. mechanisms activated by nifedipine in myometrial cells, we used the pregnant human myometrial cell line PHM1-41 that does not express L-VGCC. The in vitro measurement of intracellular Ca²⁺ showed that high doses of nifedipine induced an important intracellular Ca²⁺ entry in myometrial cells. The inhibition or downregulation of the genes encoding for store-operated Ca²⁺ entry channels from the Orai and transient receptor potential-canonical (TRPC) families in PHM1-41 cells highlighted the implication of TRPC1 in nifedipine-induced Ca²⁺ entry. In addition, the use of 2-APB in combination with nifedipine on human myometrial strips tends to confirm that the pro-contractile effect induced by nifedipine on myometrial tissues may involve the activation of TRPC channels.

Journal of Cellular Physiology published new progress about 21829-25-4. 21829-25-4 belongs to pyridine-derivatives, auxiliary class Membrane Transporter/Ion Channel,Calcium Channel, name is Dimethyl 2,6-dimethyl-4-(2-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate, and the molecular formula is C28H29NO4, HPLC of Formula: 21829-25-4.

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

Raydan, Daniel published the artcileManganese-Catalyzed Synthesis of Imines from Primary Alcohols and (Hetero)Aromatic Amines, COA of Formula: C5H5BrN2, the publication is Synlett (2022), 33(13), 1290-1294, database is CAplus.

Herein, the synthesis of a wide variety of imines through oxidative coupling of alcs. and aromatic amines catalyzed by Mn complexes bearing NN triazole ligands was described. A wide variety of imines in excellent yields (up to 99%) was prepared Mn-based catalysts proved to be highly efficient and versatile, allowing for the first time the preparation of several imines containing N-based heterocycles.

Synlett published new progress about 39856-58-1. 39856-58-1 belongs to pyridine-derivatives, auxiliary class Pyridine,Bromide,Amine, name is 2-Bromopyridin-3-amine, and the molecular formula is C5H5BrN2, COA of Formula: C5H5BrN2.

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

Robinett, R. Graham published the artcileThe discovery of substituted 4-(3-hydroxyanilino)-quinolines as potent RET kinase inhibitors, Computed Properties of 197958-29-5, the publication is Bioorganic & Medicinal Chemistry Letters (2007), 17(21), 5886-5893, database is CAplus and MEDLINE.

Substituted 4-(3-hydroxyanilino)-quinoline compounds, initially identified as small-mol. inhibitors of src family kinases, have been evaluated as potential inhibitors of RET kinase. Three compounds, 38, 31, and 40, had K_i‘s of 3, 25, and 50 nM in an in vitro kinase assay; while a cell based kinase assay showed K_i‘s of 300, 100, and 45 nM, resp. These compounds represent potential new leads for the treatment of medullary and papillary thyroid cancer.

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 C5H6BNO2, Computed Properties of 197958-29-5.

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

Surman, Matthew D. published the artcile5-(Pyridinon-1-yl)indazoles and 5-(furopyridinon-5-yl)indazoles as MCH-1 antagonists, Safety of 2-Pyridinylboronic acid, the publication is Bioorganic & Medicinal Chemistry Letters (2010), 20(23), 7015-7019, database is CAplus and MEDLINE.

A new series of 5-(pyridinon-1-yl)indazoles with MCH-1 antagonist activity were synthesized. Potential cardiovascular risk for these compounds was assessed based upon their interaction with the hERG potassium channel in a mini-patch clamp assay. Selected compounds were studied in a 5-day diet-induced obese mouse model to evaluate their potential use as weight loss agents. Structural modification of the 5-(pyridinon-1-yl)indazoles to give 5-(furopyridinon-5-yl)indazoles provided compounds with enhanced pharmacokinetic properties and improved efficacy.

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 C5H10Cl3O3P, Safety of 2-Pyridinylboronic acid.

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

Nicolaus, Norman published the artcileModular Synthesis of Naphthothiophenes by Pd-Catalyzed Tandem Direct Arylation/Suzuki Coupling, Synthetic Route of 612845-44-0, the publication is Organic Letters (2011), 13(16), 4236-4239, database is CAplus and MEDLINE.

A short and highly modular three-step synthesis of a new class of substituted naphthothiophenes has been developed exploiting a Pd-catalyzed tandem direct arylation/Suzuki coupling transformation of 3-[2-(2,2-dibromovinyl)phenyl]thiophenes as the key step.

Organic Letters published new progress about 612845-44-0. 612845-44-0 belongs to pyridine-derivatives, auxiliary class Pyridine,Boronic acid and ester,Ether,Boronic Acids,Boronic acid and ester, name is (6-Ethoxypyridin-3-yl)boronic acid, and the molecular formula is C7H10BNO3, Synthetic Route of 612845-44-0.

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

Gellibert, F. published the artcileDesign of novel quinazoline derivatives and related analogues as potent and selective ALK5 inhibitors, Quality Control of 18437-58-6, the publication is Bioorganic & Medicinal Chemistry Letters (2009), 19(8), 2277-2281, database is CAplus and MEDLINE.

Starting from quinazoline 3a, we designed potent and selective ALK5 inhibitors over p38MAP kinase from a rational drug design approach based on co-crystal structures in the human ALK5 kinase domain. The quinazoline 3d exhibited also in vivo activity in an acute rat model of DMN-induced liver fibrosis when administered orally at 5 mg/kg (bid).

Bioorganic & Medicinal Chemistry Letters 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, Quality Control of 18437-58-6.

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

Sadig, Jessie E. R. published the artcilePalladium-Catalyzed Synthesis of Benzimidazoles and Quinazolinones from Common Precursors, Category: pyridine-derivatives, the publication is Journal of Organic Chemistry (2012), 77(21), 9473-9486, database is CAplus and MEDLINE.

N-(o-Halophenyl)imidoyl chlorides and the corresponding imidates are easily prepared and can be utilized as complementary precursors for the synthesis of important heterocycles. The synthesis of N-substituted benzimidazoles was possible from the palladium-catalyzed reaction of both classes of substrate with a variety of N-nucleophiles. The use of the imidate precursor for the synthesis of N-substituted quinazolinones by incorporation of a palladium-catalyzed aminocarbonylation reaction has also been demonstrated. Both processes tolerate a wide range of functional groups.

Journal of Organic Chemistry published new progress about 39856-58-1. 39856-58-1 belongs to pyridine-derivatives, auxiliary class Pyridine,Bromide,Amine, name is 2-Bromopyridin-3-amine, and the molecular formula is C5H5BrN2, Category: pyridine-derivatives.

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

Grases, F. published the artcileA simple monitored thermometric determination of copper(II) by reaction-rate measurement based on the catalysis of the aerial oxidation of 2,2′-dipyridylketone hydrazone, SDS of cas: 2215-33-0, the publication is Analytica Chimica Acta (1984), 158(2), 389-93, database is CAplus.

The initial rate of oxidation of 2,2′-dipyridylketone hydrazone was measured by monitoring the rate of increase of temperature of the solution with a thermistor. Cu 0.2-2 mg/L was determined in the final solution with very few interferences.

Analytica Chimica Acta published new progress about 2215-33-0. 2215-33-0 belongs to pyridine-derivatives, auxiliary class Pyridine,Amine, name is 2-((2-(Pyridin-2-yl)hydrazono)methyl)pyridine, and the molecular formula is C11H10N4, SDS of cas: 2215-33-0.

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

Wu, Jiang-Ping published the artcileThe discovery of thienopyridine analogues as potent IκB kinase β inhibitors. Part II, Related Products of pyridine-derivatives, the publication is Bioorganic & Medicinal Chemistry Letters (2009), 19(19), 5547-5551, database is CAplus and MEDLINE.

An SAR study that identified a series of thienopyridine-based potent IκB Kinase β (IKKβ) inhibitors is described. With focuses on the structural optimization at C-4 and C-6 of 3-aminothieno[2,3-b]pyridine-2-carboxamide, the study reveals that small alkyl and certain aromatic groups are preferred at C-4, whereas polar groups with proper orientation at C-6 efficiently enhance compound potency. The most potent analogs inhibit IKKβ with IC₅₀s as low as 40 nM, suppress LPS-induced TNF-α production in vitro and in vivo, display good kinase selectivity profiles, and are active in a HeLa cell NF-κB reporter gene assay, demonstrating that they directly interfere with the NF-κB signaling pathway.

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 C2H4ClNO, Related Products of pyridine-derivatives.

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