Tag: M.W=150-200

Recently I am researching about STEP ECONOMY PASE; ONE-POT; CORROSION-INHIBITORS; MULTICOMPONENT REACTIONS; ORGANIC-SYNTHESIS; MILD-STEEL; PARTITION-COEFFICIENTS; ATOM ECONOMY; EFFICIENT; DERIVATIVES, Saw an article supported by the Russian Foundation for Basic ResearchRussian Foundation for Basic Research (RFBR) [18-03-00212]. COA of Formula: C9H7NO2. Published in MDPI in BASEL ,Authors: Ryzhkov, FV; Ryzhkova, YE; Elinson, MN; Vorobyev, SV; Fakhrutdinov, AN; Vereshchagin, AN; Egorov, MP. The CAS is 86-95-3. Through research, I have a further understanding and discovery of 4-Hydroxyquinolin-2(1H)-one

The Pot, Atom, and Step Economy (PASE) approach is based on the Pot economy principle and unites it with the Atom and Step Economy strategies; it ensures high efficiency, simplicity and low waste formation. The PASE approach is widely used in multicomponent chemistry. This approach was adopted for the synthesis of previously unknown hydroxyquinolinone substituted chromeno[2,3-b]pyridines via reaction of salicylaldehydes, malononitrile dimer and hydroxyquinolinone. It was shown that an ethanol-pyridine combination is more beneficial than other inorganic or organic catalysts. Quantum chemical studies showed that chromeno[2,3-b]pyridines has potential for corrosion inhibition. Real time H-1 NMR monitoring was used for the investigation of reaction mechanism and 2-((2H-chromen-3-yl)methylene)malononitrile was defined as a key intermediate in the reaction.

About 4-Hydroxyquinolin-2(1H)-one, If you have any questions, you can contact Ryzhkov, FV; Ryzhkova, YE; Elinson, MN; Vorobyev, SV; Fakhrutdinov, AN; Vereshchagin, AN; Egorov, MP or concate me.. COA of Formula: C9H7NO2

Reference:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
,Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

An article Design, synthesis and biological evaluation of fused naphthofuro[3,2-c]quinoline-6,7,12-triones and pyrano[3,2-c]quinoline-6,7,8,13-tetraones derivatives as ERK inhibitors with efficacy in BRAF-mutant melanoma WOS:000455479600032 published article about ACQUIRED-RESISTANCE; IN-VITRO; PROTEIN; DISCOVERY; DOCKING; PHOSPHORYLATION; ACTIVATION; PRODUCTS; QUINONES; BVD-523 in [Aly, Ashraf A.; El-Sheref, Essmat M.; Bakheet, Momtaz E. M.; Ibrahim, Mahmoud A. A.] Menia Univ, Fac Sci, Chem Dept, El Minia 61519, Egypt; [Mourad, Mai A. E.] Port Said Univ, Med Chem Dept, Fac Pharm, Port Said 42526, Egypt; [Kaoud, Tamer S.] Menia Univ, Fac Pharm, Dept Med Chem, El Minia 61519, Egypt; [Brase, Stefan] Karlsruhe Inst Technol, Inst Toxikol & Genet, Hermann von Helmholts Pl 1,Campus Nord, D-76344 Eggenstein Leopoldsha, Germany; [Brase, Stefan] Inst Toxikol & Genet, Hermann von Helmholts Pl 1,Campus Nord, D-76344 Eggenstein Leopoldsha, Germany; [Nieger, Martin] Univ Helsinki, Dept Chem, POB 55, Helsinki 00014, Finland; [Garvalov, Boyan K.] Mannhe Univ Heidelberg, Ctr Biomed & Med Technol Mannheim, Med Fac, D-68167 Mannheim, Germany; [Dalby, Kevin N.; Kaoud, Tamer S.] Univ Texas Austin, Div Chem Biol & Med Chem, Austin, TX 78712 USA in 2019, Cited 57. Formula: C9H7NO2. The Name is 4-Hydroxyquinolin-2(1H)-one. Through research, I have a further understanding and discovery of 86-95-3

Approximately 60% of human cancers exhibit enhanced activity of ERK1 and ERK2, reflecting their multiple roles in tumor initiation and progression. Acquired drug resistance, especially mechanisms associated with the reactivation of the MAPK (RAF/MEK/ERK) pathway represent a major challenge to current treatments of melanoma and several other cancers. Recently, targeting ERK has evolved as a potentially attractive strategy to overcome this resistance. Herein, we report the design and synthesis of novel series of fused naphthofuro[3,2-c] quinoline-6,7,12-triones 3a-f and pyrano[3,2-c]quinoline-6,7,8,13-tetraones 5a,b and 6, as potential ERK inhibitors. New inhibitors were synthesized and identified by different spectroscopic techniques and X-ray crystallography. They were evaluated for their ability to inhibit ERK1/2 in an in vitro radioactive kinase assay. 3b and 6 inhibited ERK1 with IC50s of 0.5 and 0.19 mu M, and inhibited ERK2 with IC50s of 0.6 and 0.16 mu M respectively. Kinetic mechanism studies revealed that the inhibitors are ATP-competitive inhibitors where 6 inhibited ERK2 with a K-i of 0.09 mu M. Six of the new inhibitors were tested for their in vitro anticancer activity against the NCI-60 panel of tumor cell lines. Compound 3b and 6 were the most potent against most of the human tumor cell lines tested. Moreover, 3b and 6 inhibited the proliferation of the BRAF mutant A375 melanoma cells with IC50s of 3.7 and 0.13 mu M, respectively. In addition, they suppressed anchorage-dependent colony formation. Treatment of the A375 cell line with 3b and 6 inhibited the phosphorylation of ERK substrates p-90RSK and ELK-1 and induced apoptosis in a dose dependent manner. Finally, a molecular docking study showed the potential binding mode of 3b and 6 within the ATP catalytic binding site of ERK2.

Formula: C9H7NO2. About 4-Hydroxyquinolin-2(1H)-one, If you have any questions, you can contact Aly, AA; El-Sheref, EM; Bakheet, MEM; Mourad, MAE; Brase, S; Ibrahim, MAA; Nieger, M; Garvalov, BK; Dalby, KN; Kaoud, TS or concate me.

Reference:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
,Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

An article Discovery of a novel series of hDHODH inhibitors with anti-pulmonary fibrotic activities WOS:000464108100006 published article about HUMAN DIHYDROOROTATE DEHYDROGENASE; DRUG in [Lu, Kuan; Zhao, Yanfang; Wu, Guodong; Hu, Hao; Jiang, Yuyang] Shenyang Pharmaceut Univ, Dept Pharmaceut Engn, Shenyang 110016, Liaoning, Peoples R China; [Lu, Kuan; Wang, Mingzhong] Sherushen Kivita Innovat Drug Discovery Inst, Sherushen 518057, Peoples R China; [Jiang, Yuyang] Tsinghua Univ, Natl & Local United Engn Lab Personalised Antitum, Grad Sch Shenshen, Shenzhen 518055, Peoples R China; [Jiang, Yuyang] Tsinghua Univ, Dept Pharmacol & Pharmaceut Sci, Sch Med, Beijing 100084, Peoples R China; [Gong, Guowei] Zunyi Med Univ, Dept Bioengn, Zhuhai Campus, Zhuhai 519041, Guangdong, Peoples R China in 2019, Cited 17. The Name is 3-(Trifluoromethyl)phenol. Through research, I have a further understanding and discovery of 98-17-9. Application In Synthesis of 3-(Trifluoromethyl)phenol

Human dihydroorotate dehydrogenase (hDHODH) is a flavin-dependent enzyme essential to pyrimidine de novo biosynthesis, which serves as an attractive therapeutic target for the treatment of autoimmune disorders. A novel series of hDHODH inhibitors was developed based on a lead which was obtained by a medicinal chemistry exploration. Most compounds showed moderate to significant potency against hDHODH, compounds 5d, 5e, and 6a effectively inhibited the activities of hDHODH with IC50 values from 0.9 to 2.8 mu M. Further studies showed that compound 5e also effectively suppressed proliferation of the activated PBMCs (IC50 = 20.35 mu M). Surprisingly, compound 5e also showed anti-pulmonary fibrotic activity similar to that of pirfenidone in vitro assay. Therefore, compound 5e might have potential to be developed as a novel hDHODH inhibitors for auto-immune diseases therapy.

Application In Synthesis of 3-(Trifluoromethyl)phenol. About 3-(Trifluoromethyl)phenol, If you have any questions, you can contact Lu, K; Zhao, YF; Wu, GD; Hu, H; Wang, MZ; Gong, GW; Jiang, YY or concate me.

Reference:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
,Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

Aly, AA; Ishak, E; Shwaky, AM; Mohamed, AH in [Aly, Ashraf A.; Mohamed, Asmaa H.] Menia Univ, Fac Sci, Chem Dept, El Minia 61519, Egypt; [Ishak, Esam] Al Azhar Univ, Fac Sci, Dept Chem, Assiut, Egypt; [Ishak, Esam] Jouf Univ, Coll Sci & Arts, Dept Chem, Alquurrayate, Saudi Arabia; [Shwaky, Ahmed M.] Umm Al Qura Univ, STU, Mecca, Saudi Arabia published Formation of furo[3,2-c]quinolone-2-carbonitriles and 4-oxo-4,5-dihydrofuro[3,2-c]quinolone-2-carboxamides from reaction of quinoline-2,4-diones with 2-[bis(methylthio)methylene]malononitrile in 2020, Cited 31. COA of Formula: C9H7NO2. The Name is 4-Hydroxyquinolin-2(1H)-one. Through research, I have a further understanding and discovery of 86-95-3.

Quinoline-2,4-diones reacted with 2-[bis(methylthio)methylene]malononitrile in DMF/Et3N to produce 3-(methylthio)-4-oxo-4,5-dihydrofuro[3,2-c]quinolone-2-carbonitriles and 3-(methylthio)-4-oxo-4,5-dihydrofuro[3,2-c]quinolone-2-carboxamides in state of 2-imino-substituted 4-(methylthio)-5,6-dihydro-2H-pyrano[3,2-c]quinolone-3-carbonitriles. The structures of all new products were proved using NMR, IR, and mass spectral data. The possible mechanism for the reaction is also discussed. Graphic abstract

About 4-Hydroxyquinolin-2(1H)-one, If you have any questions, you can contact Aly, AA; Ishak, E; Shwaky, AM; Mohamed, AH or concate me.. COA of Formula: C9H7NO2

Reference:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
,Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

An article Regioselectivity of Hydroxyl Radical Reactions with Arenes in Nonaqueous Solutions WOS:000461844000022 published article about HOMOLYTIC AROMATIC-SUBSTITUTION; GAS-PHASE REACTIONS; LASER FLASH-PHOTOLYSIS; SET MODEL CHEMISTRY; ORGANIC-COMPOUNDS; RATE CONSTANTS; INORGANIC RADICALS; CENTERED RADICALS; OH RADICALS; KINETICS in [Moores, Lee C.; Kaur, Devinder; Smith, Mathew D.; Poole, James S.] Ball State Univ, Dept Chem, Muncie, IN 47306 USA; [Poole, James S.] St Cloud State Univ, Dept Chem & Biochem, St Cloud, MN 56301 USA in 2019, Cited 77. Formula: C7H5F3O. The Name is 3-(Trifluoromethyl)phenol. Through research, I have a further understanding and discovery of 98-17-9

The regioselectivity of hydroxyl radical addition to arenes was studied using a novel analytical method capable of trapping radicals formed after the first elementary step of reaction, without alteration of the product distributions by secondary oxidation processes. Product analyses of these reactions indicate a preference for o- over p-substitution for electron donating groups, with both favored over m-addition. The observed distributions are qualitatively similar to those observed for the addition of other carbon-centered radicals, although the magnitude of the regioselectivity observed is greater for hydroxyl. The data, reproduced by high accuracy CBS-QB3 computational methods, indicate that both polar and radical stabilization effects play a role in the observed regioselectivities. The application and potential limitations of the analytical method used are discussed.

About 3-(Trifluoromethyl)phenol, If you have any questions, you can contact Moores, LC; Kaur, D; Smith, MD; Poole, JS or concate me.. Formula: C7H5F3O

Reference:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
,Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

Safety of 4-Hydroxyquinolin-2(1H)-one. In 2020 MONATSH CHEM published article about DERIVATIVES; INHIBITORS; FUROQUINOLINE; ALKALOIDS; MODEL in [Aly, Ashraf A.; Mohamed, Asmaa H.] Menia Univ, Fac Sci, Chem Dept, El Minia 61519, Egypt; [Ishak, Esam] Al Azhar Univ, Fac Sci, Dept Chem, Assiut, Egypt; [Ishak, Esam] Jouf Univ, Coll Sci & Arts, Dept Chem, Alquurrayate, Saudi Arabia; [Shwaky, Ahmed M.] Umm Al Qura Univ, STU, Mecca, Saudi Arabia in 2020, Cited 31. The Name is 4-Hydroxyquinolin-2(1H)-one. Through research, I have a further understanding and discovery of 86-95-3.

Quinoline-2,4-diones reacted with 2-[bis(methylthio)methylene]malononitrile in DMF/Et3N to produce 3-(methylthio)-4-oxo-4,5-dihydrofuro[3,2-c]quinolone-2-carbonitriles and 3-(methylthio)-4-oxo-4,5-dihydrofuro[3,2-c]quinolone-2-carboxamides in state of 2-imino-substituted 4-(methylthio)-5,6-dihydro-2H-pyrano[3,2-c]quinolone-3-carbonitriles. The structures of all new products were proved using NMR, IR, and mass spectral data. The possible mechanism for the reaction is also discussed. Graphic abstract

About 4-Hydroxyquinolin-2(1H)-one, If you have any questions, you can contact Aly, AA; Ishak, E; Shwaky, AM; Mohamed, AH or concate me.. Safety of 4-Hydroxyquinolin-2(1H)-one

Reference:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
,Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

Safety of 3,4-Dimethoxybenzaldehyde. Authors Menezes, AP; Jayarama, A; Ravindra, HJ in ELSEVIER published article about in [Menezes, Anthoni Praveen] Mangalore Inst Technol & Engn MITE, Dept Phys, Moodabidri 574225, India; [Jayarama, A.] Alvas Inst Engn & Technol, Dept Phys, Shobhavana Campus, Mijar 574225, Moodabidri, India; [Ravindra, H. J.] Shri Madhwa Vadiraja Inst Technol & Management, Dept Phys, Bantakal 574115, Udupi, India in 2021.0, Cited 18.0. The Name is 3,4-Dimethoxybenzaldehyde. Through research, I have a further understanding and discovery of 120-14-9

In this article we present the growth and structural details of a pyridine based chalcone single crystal grown using the method, slow evaporation of solvent. The crystal structure was studied by X-ray diffraction method. The solid belongs to orthorhombic crystal system with a non-centrosymmetric space group Pna2(1). Weak C-H-O intermolecular hydrogen bond interactions stabilize the crystal structure, which is further confirmed by surface analysis by Hirshfeld. As the material crystalizes in enantiomorphic crystal structure, it may be a potential candidate for various photonic applications. (C) 2019 Elsevier Ltd. All rights reserved.

Safety of 3,4-Dimethoxybenzaldehyde. About 3,4-Dimethoxybenzaldehyde, If you have any questions, you can contact Menezes, AP; Jayarama, A; Ravindra, HJ or concate me.

Reference:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
,Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

Authors Peshkov, AA; Bakulina, O; Dar’in, D; Kantin, G; Bannykh, A; Peshkov, VA; Krasavin, M in WILEY-V C H VERLAG GMBH published article about in [Peshkov, Anatoly A.; Bakulina, Olga; Dar’in, Dmitry; Kantin, Grigory; Bannykh, Anton; Krasavin, Mikhail] St Petersburg State Univ, Dept Nat Prod Chem, Inst Chem, 26 Univ Skyi Prospekt, Peterhof 198504, Russia; [Peshkov, Vsevolod A.] Nazarbayev Univ, Dept Chem, Sch Sci & Humanities, Nur Sultan 010000, Kazakhstan; [Krasavin, Mikhail] Immanuel Kant Baltic Fed Univ, Kaliningrad 236041, Russia; [Bannykh, Anton] Univ Jyvaskyla, Dept Chem, Survontie 9B, Jyvaskyla 40014, Finland in 2021.0, Cited 27.0. Category: indole-building-block. The Name is 3,4-Dimethoxybenzaldehyde. Through research, I have a further understanding and discovery of 120-14-9

A practical straightforward synthesis of medicinally important NH-delta-lactams through the three-component Castagnoli-Cushman reaction of 3-arylglutaconic anhydrides with carbonyl compound and ammonium acetate has been developed. The scope of the protocol has been thoroughly explored paying particular attention to the carbonyl component using wide array of aliphatic and aromatic aldehydes as well as rarely involved cyclic and acyclic ketones. Synthetic potential of prepared compounds was demonstrated by a series of post-modifications, including unexpected isomerization.

Category: indole-building-block. About 3,4-Dimethoxybenzaldehyde, If you have any questions, you can contact Peshkov, AA; Bakulina, O; Dar’in, D; Kantin, G; Bannykh, A; Peshkov, VA; Krasavin, M or concate me.

Reference:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
,Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

In 2019 J HETEROCYCLIC CHEM published article about TETRAPROPYLAMMONIUM BROMIDE; BIOLOGICAL EVALUATION; DERIVATIVES; CATALYST; WATER in [Marjani, Ahmad Poursattar; Khalafy, Jabbar; Farajollahi, Ayda] Urmia Univ, Dept Organ Chem, Fac Chem, Orumiyeh, Iran in 2019, Cited 41. The Name is 4-Hydroxyquinolin-2(1H)-one. Through research, I have a further understanding and discovery of 86-95-3. Name: 4-Hydroxyquinolin-2(1H)-one

In this research, in order to synthesize a series of ethyl 2-amino-4-benzoyl-5-oxo-5,6-dihydro-4H-pyrano[3,2-c]quinoline-3-carboxylates, a green and an efficient method is proposed through one-pot three-component reaction of substituted arylglyoxals, ethyl cyanoacetate, and 4-hydroxyquinolin-2(1H)-one in the presence of terapropylammonium bromide as a catalyst in good yields. All synthesized new substances were characterized by FTIR, H-1-NMR, and C-13-NMR spectral data and elemental analysis.

About 4-Hydroxyquinolin-2(1H)-one, If you have any questions, you can contact Marjani, AP; Khalafy, J; Farajollahi, A or concate me.. Name: 4-Hydroxyquinolin-2(1H)-one

Reference:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
,Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

An article Synthesis, structural elucidation and larvicidal activity of novel arylhydrazones WOS:000646276700011 published article about HYDRAZONE DERIVATIVES; ANTIINFLAMMATORY ACTIVITIES; N-ACYLHYDRAZONES; DESIGN; POTENT; DOCKING in [Nefisath, P.; Shashiprabha; Poojary, Vishwanatha] Sri Dharmasthala Manjunatheshwara Coll Autonomous, Post Grad Dept Chem, Ujire 574240, India; [Nefisath, P.; Dasappa, Jagadeesh Prasad] Mangalore Univ, Dept Chem, Mangalagangothri, Karnataka, India; [Haripriya, B.; Chopra, Deepak] Indian Inst Sci Educ & Res Bhopal, Dept Chem, Bhopal By Pass Rd, Bhopal 462066, Madhya Pradesh, India; [Venugopala, Katharigatta N.] King Faisal Univ, Coll Clin Pharm, Dept Pharmaceut Sci, Al Hasa 31982, Saudi Arabia; [Venugopala, Katharigatta N.; Mohanlall, Viresh] Durban Univ Technol, Dept Biotechnol & Food Technol, ZA-4001 Durban, South Africa; [Deb, Pran Kishore] Philadelphia Univ, Fac Pharm, Dept Pharmaceut Sci, POB 1, Amman 19392, Jordan; [Gleiser, Raquel M.] UNC, CONICET, IMBIV, CREAN, Av Valparaiso S-N, Cordoba, Argentina; [Gleiser, Raquel M.] Univ Nacl Cordoba, FCEFyN, Av Velez Sarsfield 299, RA-5000 Cordoba, Argentina; [Maharaj, Rajendra] South African Med Res Council, Off Malaria Res Unit, ZA-4091 Durban, South Africa in 2021.0, Cited 63.0. The Name is 3,4-Dimethoxybenzaldehyde. Through research, I have a further understanding and discovery of 120-14-9. Safety of 3,4-Dimethoxybenzaldehyde

The present study focuses on a series of novel hydrazones of 2-[3-cyano-4-(2-methylpropoxy)phenyl]-4-methyl-1,3-thiazole-5-carbohydrazide (5a-l) for their larvicidal activity against Anopheles arabiensis. The synthesis of the title compounds was achieved by the conventional reflux method, and structures of the novel compounds were ascertained by FT-IR, NMR (H-1&C-13), LC-MS, and elemental analysis. Compound (5l) was studied by single crystal X-ray diffraction for intra and intermolecular interactions. Title compounds (E)-2-(3-cyano-4-isobutoxyphenyl)-N’-(4-fluoro-3-phenoxybenzylidene)-4-methylthiazole-5-carbohydrazide (5a) and (E)-N’-(4-Chlorobenzylidene)-2-(3-cyano-4-isobutoxyphenyl)-4-methylthiazole-5-carbohydrazide (5g) emerged as promising larvicidal agents against Anopheles arabiensis. (C) 2021 Elsevier B.V. All rights reserved.

Safety of 3,4-Dimethoxybenzaldehyde. About 3,4-Dimethoxybenzaldehyde, If you have any questions, you can contact Nefisath, P; Dasappa, JP; Haripriya, B; Chopra, D; Venugopala, KN; Deb, PK; Gleiser, RM; Mohanlall, V; Maharaj, R; Shashiprabha; Poojary, V or concate me.

Reference:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
,Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles