Day: January 7, 2022

An article Novel [1,2,3] triazolo[1,5-a]pyridine derivatives are trypanocidal by sterol biosynthesis pathway alteration WOS:000478848800005 published article about CELL-PROLIFERATION; STRUCTURAL-BASIS; DRUG CANDIDATES; CHOLESTEROL; 14-ALPHA-DEMETHYLASE; INHIBITION; INSIGHTS; BINDING; CYP51; CHAIN in [Lapier, Michel; Guzman-Rivera, Daniela; Gonzalez-Herrera, Fabiola; Pesce, Barbara; Maya, Juan D.] Univ Chile, Fac Med, Inst Ciencias Biomed ICBM, Clin & Mol Pharmacol Program, Independencia 1027, Santiago 1027, Chile; [Ballesteros-Garrido, Rafael; Ballesteros, Rafael; Abarca, Belen] Univ Valencia, Fac Pharm, Dept Organ Chem, Avda Vicent Andres Estelles S-N, E-46100 Valencia, Spain; [Aguilera-Venegas, Benjamin; Moncada-Basualto, Mauricio; Olea-Azar, Claudio] Univ Chile, Fac Chem & Pharmaceut Sci, Free Rad & Antioxidants Lab, Inorgan & Analyt Dept, Santos Dumt 964, Santiago, Chile; [Moncada-Basualto, Mauricio] Univ Santiago Chile, Fac Chem & Biol, Dept Environm Sci, Santiago, Chile; [Kemmerling, Ulrike] Univ Chile, Fac Med, Inst Ciencias Biomed ICBM, Anat & Dev Biol Program, Independencia 1027, Santiago, Chile in 2019, Cited 38. The Name is Ethyl nicotinate. Through research, I have a further understanding and discovery of 614-18-6. Recommanded Product: Ethyl nicotinate

Aim: To study a new series of [1,2,3] triazolo[1,5-alpha] pyridine derivatives as trypanocidal agents because current antichagasic pharmacologic therapy is only partially effective. Materials & methods: The effect of the series upon Trypanosoma cruzi epimastigotes and murine macrophages viability, cell cycle, cell death and on the metabolites of the sterol biosynthesis pathway was measured; also, docking in 14 alpha-demethylase was analyzed. Results: Compound 16 inhibits 14 alpha-demethylase producing an imbalance in the cholesterol/ergosterol synthesis pathway, as suggested by a metabolic control and theoretical docking analysis. Consequently, it prevented cell proliferation, stopping the cellular cycle at the G2/M phase, inducing cell death. Conclusion: Although the exact cell death mechanism remained elusive, this series can be used for the further rational design of novel antiparasitic molecules.

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Reference:
Pyridine – Wikipedia,
,Pyridine | C5H5N – PubChem

Recommanded Product: 3-Hydroxy-5-(hydroxymethyl)-2-methylisonicotinaldehyde hydrochloride. Authors Pishchugin, FV; Tuleberdiev, IT in MAIK NAUKA/INTERPERIODICA/SPRINGER published article about in [Pishchugin, F. V.; Tuleberdiev, I. T.] Kyrgyz Natl Acad Sci, Inst Chem & Phytotechnol, Bishkek 720071, Kyrgyzstan in 2021.0, Cited 13.0. The Name is 3-Hydroxy-5-(hydroxymethyl)-2-methylisonicotinaldehyde hydrochloride. Through research, I have a further understanding and discovery of 65-22-5

The kinetics and mechanism of condensation of pyridoxal hydrochloride with L-alpha-asparagine, L-alpha- and D-alpha-aspartic acids are analyzed via UV spectroscopy and polarimetry. It is found that L-alpha-asparagine containing alpha-NH2 and gamma-NH2 groups interacts with pyridoxal via the gamma-NH2 group, forming Schiff bases that are resistant to chemical transformations. Rearrangement produces Schiff bases that form the cyclic structure from the amino acid moiety. L-alpha- and D-alpha-aspartic acids interacting with pyridoxal via alpha-NH2 groups create Schiff bases that form quinoid structures after elimination of alpha-hydrogen or CO2. Their subsequent hydrolysis results in pyridoxamine, alpha-ketoacids, and aldehyde acids, respectively. Schemes of the condensation mechanisms of L-alpha-asparagine, L-alpha-, D-alpha-aspartic acids with pyridoxal hydrochloride are proposed.

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Reference:
Pyridine – Wikipedia,
,Pyridine | C5H5N – PubChem

In 2019.0 BIOORGAN MED CHEM published article about ALZHEIMERS-DISEASE; GSK-3 INHIBITORS; DESIGN; CANCER; GENE; COMBINATION; INDIRUBINS; METABOLISM; SIMULATION; EFFICIENT in [Lozinskaya, Natalia A.; Zaryanova, Ekaterina V.; Bezsonova, Elena N.; Borisov, Alexander V.; Tsymlyakov, Michael D.; Proskurnina, Marina V.] Lomonosov Moscow State Univ, Dept Chem, Leninskie Gory St 1, Moscow 119234, Russia; [Lozinskaya, Natalia A.; Anikina, Lada V.; Proskurnina, Marina V.] Russian Acad Sci, Inst Physiol Act Cpds, 1 Severnyi Proezd, Chernogolovka 142432, Russia; [Babkov, Denis A.; Zakharyascheva, Olga Yu.; Borisov, Alexander V.; Perfilova, Valentina N.; Tyurenkov, Ivan N.; Spasov, Alexander A.] Volgograd State Med Univ, Novorossiyskaya St 39, Volgograd 400087, Russia in 2019.0, Cited 49.0. The Name is 3-Pyridinecarboxaldehyde. Through research, I have a further understanding and discovery of 500-22-1. SDS of cas: 500-22-1

Glycogen synthase kinase 3 beta (GSK-3 beta) is a widely investigated molecular target for numerous diseases including Alzheimer’s disease, cancer, and diabetes mellitus. Inhibition of GSK-3 beta activity has become an attractive approach for treatment of diabetes and cancer. We report the discovery of novel GSK-3 beta inhibitors of 3-arylidene-2-oxindole scaffold with promising activity. The most potent compound 3a inhibits GSK-3 beta with IC(50 )4.19 nM. In a cell-based assay 3a shows no significant leucocyte toxicity at 10 mu M and is moderately cytotoxic against A549 cells. Compound 3a demonstrated high antidiabetic efficacy in obese streptozotocin-treated rats improving glucose tolerance at a dose of 50 mg/kg body weight thus representing an interesting lead for further optimization.

SDS of cas: 500-22-1. Welcome to talk about 500-22-1, If you have any questions, you can contact Lozinskaya, NA; Babkov, DA; Zaryanova, EV; Bezsonova, EN; Borisov, AV; Tsymlyakov, MD; Anikina, LV; Zakharyascheva, OY; Borisov, AV; Perfilova, VN; Tyurenkov, IN; Proskurnina, MV; Spasov, AA or send Email.

Reference:
Pyridine – Wikipedia,
,Pyridine | C5H5N – PubChem

In 2020.0 ADV MED SCI-POLAND published article about EPITHELIAL OVARIAN CARCINOMAS; NITRIC-OXIDE SYNTHASE; HYDROXY-L-ARGININE; PROGNOSTIC VALUE; CANCER; EXPRESSION; RECEPTOR; MICROENVIRONMENT; THERAPIES; SURVIVAL in [Mohan, Srinidi; Patel, Seema; Barlow, David; Rojas, Augusto Cardenas] Univ New England, Coll Pharm, Dept Pharmaceut Sci, Portland, ME USA in 2020.0, Cited 28.0. The Name is 3-Hydroxy-5-(hydroxymethyl)-2-methylisonicotinaldehyde hydrochloride. Through research, I have a further understanding and discovery of 65-22-5. Safety of 3-Hydroxy-5-(hydroxymethyl)-2-methylisonicotinaldehyde hydrochloride

Purpose: We investigated Nw-hydroxy L-Arginine (NOHA) predictive response in serous ovarian carcinoma based on estrogen-hormone receptor expression status; and assessed the distinctive NOHA response between estrogen-receptor-negative (ER-) tumor subtypes of ovarian and breast cancer. Materials/methods: Three-dimensional (3D) spheroids models of ER- and estrogen-receptor-positive (ER+) from breast and ovarian tumor, cultured for 9 weeks, were assayed for cellular levels of inducible nitric oxide synthase (NOS2), nitric oxide (as total nitrite) and L-Arginine, and compared to NOHA in culture medium. Statistical difference was set at p < 0.01. Results: Nine-week in vitro studies showed a progressive NOHA reduction in culture medium by at least 0.4-0.8 fold, and 0.65-0.92 fold only in the ER-breast tumor and ER-ovarian tumor 3D spheroids, respectively; with increases in cellular NOS2 and nitric-oxide levels, by at least 1.0-2.45 fold in both ER-tumor subtype 3D spheroids (p < 0.01; n = 6). Within ER-subtypes, medium NOHA decreased by >= 38.9% in ovarian cancer over breast cancer 3D-spheroids, with cellular increases in NOS2 (by >= 17.4%), and nitric oxide (by >= 18.8%). Cellular L-Arginine to medium NOHA ratio was higher, and by at least 6.5-22.5 fold in ER-breast tumor 3D-spheroids, and at least 10-70 fold in ER-ovarian tumor 3D spheroids, than in ER+ and control conditions; and was >= 48% higher in ER-ovarian cancer than in ER-breast cancer 3D-spheroids. Conclusions: The present study shows NOHA as a sensitive and selective indicator differentiating and distinguishing ER-subtypes based on the tumor grade.

Safety of 3-Hydroxy-5-(hydroxymethyl)-2-methylisonicotinaldehyde hydrochloride. Welcome to talk about 65-22-5, If you have any questions, you can contact Mohan, S; Patel, S; Barlow, D; Rojas, AC or send Email.

Reference:
Pyridine – Wikipedia,
,Pyridine | C5H5N – PubChem

I found the field of Pharmacology & Pharmacy very interesting. Saw the article Visnagin and benzofuran scaffold-based molecules as selective cyclooxygenase-2 inhibitors with anti-inflammatory and analgesic properties: design, synthesis and molecular docking published in 2019.0. COA of Formula: C6H5NO, Reprint Addresses Arafa, RK (corresponding author), Zewail City Sci & Technol, Program Biomed Sci, Cairo 12578, Egypt.. The CAS is 500-22-1. Through research, I have a further understanding and discovery of 3-Pyridinecarboxaldehyde

A series of new visnagin and benzofuran scaffold-based molecules was designed and synthesized as anti-inflammatory and analgesic agents. Biological screening of these compounds showed that they exhibit potent anti-inflammatory/analgesic activity with a safer side effect profile in in vivo mouse models. In vitro cyclooxygenase (COX)inhibition assay showed that the compounds elicit their function through selective COX-2 inhibition. Molecular docking study also revealed the ability of the compounds to correctly recognize the active site and achieve noncovalent binding interactions with key residues therein. The best combined profile of anti-inflammatory, analgesic and COX-2 selective inhibition properties in association with low gastrotoxicity was displayed by the analogs 8, 11b and 19d, which can be considered as promising leads for further future optimization. [GRAPHICS] .

COA of Formula: C6H5NO. Bye, fridends, I hope you can learn more about C6H5NO, If you have any questions, you can browse other blog as well. See you lster.

Reference:
Pyridine – Wikipedia,
,Pyridine | C5H5N – PubChem

Recommanded Product: 65-22-5. Authors Zubenko, AA; Divaeva, LN; Morkovnik, AS; Fetisov, LN; Sochnev, VS; Kononenko, KN; Bodryakov, AN; Klimenko, AI in MAIK NAUKA/INTERPERIODICA/SPRINGER published article about in [Zubenko, A. A.; Fetisov, L. N.; Kononenko, K. N.; Bodryakov, A. N.; Klimenko, A. I.] Fed Rostov Agr Sci Ctr, North Caucasian Zonal Vet Res Inst, Novocherkassk 346406, Russia; [Divaeva, L. N.; Morkovnik, A. S.; Sochnev, V. S.] Southern Fed Univ, Inst Phys & Organ Chem, Rostov Na Donu 344090, Russia in 2020.0, Cited 29.0. The Name is 3-Hydroxy-5-(hydroxymethyl)-2-methylisonicotinaldehyde hydrochloride. Through research, I have a further understanding and discovery of 65-22-5

4-Hydroxymethyl-2-hetaryl(hetaroyl)furo[2,3-c]pyridines, the products of furan cyclization of pyridoxal with acylmethyl- and heteroarylmethyl halides, easily react with thionyl chloride in DMF to form new series of 4-chloromethyl-2-heteroaryl[2,3-c]pyridines. Further action of primary or secondary amines on these chloromethyl derivatives leads to the nucleophilic substitution of chlorine atoms with the formation of 4-aminomethyl-2-heteroaryl[2,3-c]pyridines. The study of anti-infective activity of the 4-RCH2-furo[2,3-c]pyridines (R = OH, Cl, (NRR2)-R-1) showed significant protistocidal and moderate antibacterial activity of some of representatives of these compounds.

Welcome to talk about 65-22-5, If you have any questions, you can contact Zubenko, AA; Divaeva, LN; Morkovnik, AS; Fetisov, LN; Sochnev, VS; Kononenko, KN; Bodryakov, AN; Klimenko, AI or send Email.. Recommanded Product: 65-22-5

Reference:
Pyridine – Wikipedia,
,Pyridine | C5H5N – PubChem

In 2021.0 J INORG BIOCHEM published article about X-RAY-STRUCTURE; METAL-COMPLEXES; BIOLOGICAL EVALUATION; CRYSTAL-STRUCTURE; DNA-BINDING; METHYLDITHIOCARBAZATE SMDTC; ANTIBACTERIAL ACTIVITY; ANTIFUNGAL ACTIVITY; CIRCULAR-DICHROISM; ZN(II) COMPLEXES in [Ramilo-Gomes, Filipa; Addis, Yemataw; Tekamo, Israel; Cavaco, Isabel; Matilde Marques, M.; Pessoa, Joao Costa; Correia, Isabel] Univ Lisbon, Inst Super Tecn, Ctr Quim Estrutural, Av Rovisco Pais, P-1049001 Lisbon, Portugal; [Ramilo-Gomes, Filipa; Addis, Yemataw; Tekamo, Israel; Cavaco, Isabel; Matilde Marques, M.; Pessoa, Joao Costa; Correia, Isabel] Univ Lisbon, Inst Super Tecn, Dept Engn Quim, Av Rovisco Pais, P-1049001 Lisbon, Portugal; [Ramilo-Gomes, Filipa] Univ Lisbon, Inst Invest Medicamento IMed ULisboa, Fac Farm, Av Prof Gama Pinto, P-1649003 Lisbon, Portugal; [Addis, Yemataw; Tekamo, Israel; Cavaco, Isabel] Univ Algarve, Dept Quim & Farm, Campus Gambelas, P-8005139 Faro, Portugal; [Campos, Debora L.; Pavan, Fernando R.] UNESP, Fac Ciencias Farmaceut, CP 582, BR-14801902 Araraquara, SP, Brazil; [Gomes, Clara S. B.] Univ NOVA Lisboa, Dept Quim, LAQV REQUIMTE Lab Associado Quim Verde, Fac Ciencias & Tecnol, P-2829516 Monte De Caparica, Portugal; [Gomes, Clara S. B.] Univ NOVA Lisboa, Appl Mol Biosci Unit UCIBIO, Fac Ciencias & Tecnol, P-2829516 Monte De Caparica, Portugal; [Brito, Vanessa; Santos, Adriana O.; Domingues, Fernanda; Luis, Angelo; Ferreira, Susana; Silvestre, Samuel] Univ Beira Interior, CICS UBI Hlth Sci Res Ctr, Av Infante D Henrique, P-6200506 Covilha, Portugal in 2021.0, Cited 80.0. The Name is 3-Hydroxy-5-(hydroxymethyl)-2-methylisonicotinaldehyde hydrochloride. Through research, I have a further understanding and discovery of 65-22-5. Recommanded Product: 65-22-5

Schiff bases (SB) obtained from S-methyl dithiocarbazate and aromatic aldehydes: salicylaldehyde (H2L1), ovanillin (H2L2), pyridoxal (H2L3) and 2,6-diformyl-4-methylphenol (H3L4), and their corresponding Zn(II)complexes (1-4), are synthesized. All compounds are characterized by elemental analyses, infrared, UV-Vis, nuclear magnetic resonance spectroscopy and mass spectrometry. The structures of H2L2 and [Zn-2(L-1)(2)(H2O) (DMF)] (1a) (DMF = dimethylformamide) are solved by single crystal X-ray diffraction. The SB coordinates the metal center through the Ophenolate, Nimine and Sthiolate atoms. The radical scavenging activity is tested using the 2,2-diphenyl-1-picrylhydrazyl (DPPH) assay, with all ligand precursors showing IC50 values similar to 40 mu M. Cytotoxicity studies with several tumor cell lines (PC-3, MCF-7 and Caco-2) as well as a non-tumoral cell line (NHDF) are reported. Interestingly, 1 has relevant and selective antiproliferative effect against Caco-2 cells (IC50 = 9.1 mu M). Their antimicrobial activity is evaluated in five bacterial strains (Klebsiella pneumoniae, Acinetobacter baumannii, Listeria monocytogenes, Pseudomonas aeruginosa and Staphylococcus aureus) and two yeast strains (Candida albicans and Candida tropicalis) with some compounds showing bacteriostatic and fungicidal activity. The minimal inhibitory concentration (MIC90) of HnL against Mycobacterium tuberculosis is also reported, with H2L2 and H3L4 showing very high activity (MIC90 < 0.6 mu g/mL). The ability of the compounds to bind bovine serum albumin (BSA) and DNA is evaluated for H3L4 and [Zn-2(L-4)(CH3COO)] (4), both showing high binding constants to BSA (ca. 106 M 1) and ability to bind DNA. Overall, the reported compounds show relevant antitumor and antimicrobial properties, our data indicating they may be promising compounds in several fields of medicinal chemistry. Recommanded Product: 65-22-5. Bye, fridends, I hope you can learn more about C8H10ClNO3, If you have any questions, you can browse other blog as well. See you lster.

Reference:
Pyridine – Wikipedia,
,Pyridine | C5H5N – PubChem

SDS of cas: 500-22-1. Recently I am researching about FRUSTRATED LEWIS PAIRS; METAL-FREE HYDROGENATIONS; DERIVATIVES; ANTAGONISTS; REDUCTION; INSIGHTS; KETONES, Saw an article supported by the Natural Science Foundation of Zhejiang Province of ChinaNatural Science Foundation of Zhejiang Province [LY19B060011]; National Natural Science Foundation of ChinaNational Natural Science Foundation of China (NSFC) [21676253, 21706234]. Published in WILEY in HOBOKEN ,Authors: Ling, F; Chen, JC; Xie, Z; Hou, HC; Pan, ZT; Feng, C; Shen, HW; Zhong, WH. The CAS is 500-22-1. Through research, I have a further understanding and discovery of 3-Pyridinecarboxaldehyde

A metal-free method to construct quinoline derivatives via B(C6F5)(3)-catalyzed cyclization of anilines with aldehyde derivatives and pyruvates is described. This three-component cascade reaction provides an efficient approach for the easy access to various substituted quinoline-4-carboxylic esters with 71% to 92% yield. The utility of this methodology was further demonstrated by gram-scale formal synthesis of the antimalarial drug DDD107498.

SDS of cas: 500-22-1. Welcome to talk about 500-22-1, If you have any questions, you can contact Ling, F; Chen, JC; Xie, Z; Hou, HC; Pan, ZT; Feng, C; Shen, HW; Zhong, WH or send Email.

Reference:
Pyridine – Wikipedia,
,Pyridine | C5H5N – PubChem

I found the field of Spectroscopy very interesting. Saw the article Imidazo[1,5-alpha]pyridine-based fluorescent probe with a large Stokes shift for specific recognition of sulfite published in 2020.0. Computed Properties of C12H9NO, Reprint Addresses Chen, S (corresponding author), Qiqihar Med Univ, Coll Pharm, 333 Bukui St, Qiqihar 161006, Heilongjiang, Peoples R China.. The CAS is 91-02-1. Through research, I have a further understanding and discovery of Phenyl(pyridin-2-yl)methanone

By taking advantage of the intramolecular charge transfer (ICT) process, we presented a novel fluorescent probe IPY-SO2 based on imidazo[1,5-alpha]pyridine derivative for detecting SO32- with a low detection limit (70 nM). Combining its favorable turn-on fluorescence feature (75-fold), rapid response (5 min), high selectivity, large Stokes shift (174 nm) and low cytotoxicity, IPY-SO2 was successfully applied to imaging SO32 in living MCF-7 cells and zebrafish. (C) 2019 Elsevier B.V. All rights reserved.

Computed Properties of C12H9NO. About Phenyl(pyridin-2-yl)methanone, If you have any questions, you can contact Chen, S; Hou, P; Sun, JW; Wang, HJ; Liu, L or concate me.

Reference:
Pyridine – Wikipedia,
,Pyridine | C5H5N – PubChem

I found the field of Chemistry very interesting. Saw the article Fluorenone Schiff base derivative complexes of ruthenium, rhodium and iridium exhibiting efficient antibacterial activity and DNA-binding affinity published in 2020.0. Computed Properties of C12H9NO, Reprint Addresses Kollipara, MR (corresponding author), North Eastern Hill Univ, Ctr Adv Studies Chem, Shillong 793022, Meghalaya, India.. The CAS is 91-02-1. Through research, I have a further understanding and discovery of Phenyl(pyridin-2-yl)methanone

Metal precursors [(arene)MCl2](2) (arene = p-cymene, Cp*; M = Ru, Rh and Ir) on reacting with 9-fluorenone derivative ligands L1, L2 and L3 resulted in the formation of mononuclear bidentate cationic N boolean AND N bonded complexes. The biological studies of these complexes such as antibacterial activity studies (against Gram-positive and Gram-negative bacteria) revealed significant antibacterial activity with complexes 4, 7 and 9 having the highest activity potency (in-vitro). Whilst for DNA-binding studies, the results revealed that complexes 4 and 5 displayed significant changes in their spectral features upon addition of SM-DNA, thus, indicating that these complexes bind to DNA with a significant affinity. (C) 2020 Elsevier B.V. All rights reserved.

Bye, fridends, I hope you can learn more about C12H9NO, If you have any questions, you can browse other blog as well. See you lster.. Computed Properties of C12H9NO

Reference:
Pyridine – Wikipedia,
,Pyridine | C5H5N – PubChem