Category: 93-02-7

An article Exploring isoxazoles and pyrrolidinones decorated with the 4,6-dimethoxy-1,3,5-triazine unit as human farnesyltransferase inhibitors WOS:000471346200001 published article about ONE-POT SYNTHESIS; BIOLOGICAL EVALUATION; AEROBIC OXIDATION; PRIMARY AMINES; DERIVATIVES; TRIAZINE; DISCOVERY; ANALOGS; AGENTS; SERIES in [Lucescu, Liliana; Ghinet, Alina; Belei, Dalila; Bicu, Elena] AI I Cuza Univ Iasi, Fac Chem, Bd Carol I 11, Iasi 700506, Romania; [Ghinet, Alina; Farce, Amaury; Rigo, Benoit] Univ Lille, CHRU Lille, Fac Med Pole Rech, LIRIC,INSERM,U995, Lille, France; [Ghinet, Alina; Rigo, Benoit] UC Lille, Yncrea Hauts De France, Lab Chim Durable & Sante Hautes Etud Ingn HEI, Lille, France; [Shova, Sergiu] Petru Poni Inst Macromol Chem, Iasi, Romania; [Magnez, Romain; Thuru, Xavier] Univ Lille, UMR S 1172, JPARC, Ctr Rech Jean Pierre AUBERT Neurosci & Canc, Lille, France; [Farce, Amaury] Fac Sci Pharmaceut & Biol Lille, Lille, France; [Dubois, Joelle] CNRS, UPR2301, Inst Chim Subst Nat, Ctr Rech Gif, Gif Sur Yvette, France in 2019.0, Cited 70.0. Recommanded Product: 93-02-7. The Name is 2,5-Dimethoxybenzaldehyde. Through research, I have a further understanding and discovery of 93-02-7

Unprecedented triazinyl-isoxazoles were afforded via an effective cycloaddition reaction between nitrile oxides and the scarcely described 2-ethynyl-4,6-dimethoxy-1,3,5-triazine as dipolarophile. The biological evaluation of the newly synthesized compounds showed that the inhibition of human farnesyltransferase by zinc complexation could be improved with triazine-isoxazole moieties. The replacement of the isoxazole unit by a pyrrolidin-2-one was detrimental to the inhibitory activity while the pyrrolidin-2-thione derivatives conserved the biological potential. The potential of selected compounds to disrupt protein farnesylation in Chinese hamster ovary (CHO) cells transfected with pEGFP-CAAX was also evaluated.

Welcome to talk about 93-02-7, If you have any questions, you can contact Lucescu, L; Ghinet, A; Shova, S; Magnez, R; Thuru, X; Farce, A; Rigo, B; Belei, D; Dubois, J; Bicu, E or send Email.. Recommanded Product: 93-02-7

Reference:
Isothiazole – Wikipedia,
,Isothiazole – ScienceDirect.com

An article Design, Synthesis and Antibacterial Evaluation of Hybrid Curcumin Based Pyrazole Derivatives WOS:000549899700014 published article about ANALOGS; RESISTANCE; SPICE in [Jha, Anand Mohan] BN Mandal Univ, MLT Coll Saharsa, Dept Chem, Madhepura 852201, Bihar, India; [Alam, Md. Mansoor] Lalit Narayan Mithila Univ, Dept Zool, Darbhanga 846004, Bihar, India in 2020.0, Cited 28.0. COA of Formula: C9H10O3. The Name is 2,5-Dimethoxybenzaldehyde. Through research, I have a further understanding and discovery of 93-02-7

Present work demonstrates synthesis and antibacterial property of new pyrazole derivatives. A series of new Curcumin based dihydropyrazoles has been synthesized with an objective to evaluate their antibacterial property. Dihydropyrazoles analogues were synthesized using Curcumin based chalcones and differently substituted phenylhydrazine derivatives. We used the previously designed Curcumin based chalconesto react with phenylhydrazine derivatives in ethanol in a catalyst free medium to afford new dihydropyrazole derivatives. Effect of substituent on reactivity was also studied. All the synthesized pyrazole analogues were characterized using proton and carbon NMR, Mass spectroscopy and IR techniques. Effect of substituent on reactivity was explained on the basis of electronic effect generated due to groups on phenyl ring. Presence of dd (double doublet) in proton NMR spectrum of Dihydropyrazoles was also explained due to presence of optically active carbon of pyrazole ring. The synthesized library was screened for their inhibitory activity against 4 different bacterial strains 1. E. Coli (ATCC 9637), 2. Pseudomonas aeruginosa (ATCC BAA-427), 3. Staphylococcus aureus (ATCC 25923) and 4. Klebsiella pneumonia (ATCC 27736). Out of all the compounds evaluated, the compounds that exhibited IC50 value greater than 50 mu M, were considered to be inactive. We established an important SAR based on the structure dependent inhibitory potential of screened dihydropyrazoles. Two compounds 4e and 4t having nitro and benzyl substitution respectively were showing the best inhibitory potential against Gram Positive bacterial strain Staphylococcus aureus with MIC value of 1.56 mu g/ml. Compounds having Chloro and Methoxy substitution were found to be less effective against screened bacterial strains. Compounds 4a and 4b were selective towards Staphylococcus aureus species with the MIC value of 1.56 mu g/ml for each. These pyrazole analogues were not showing inhibitory potential against other screened bacterial strains.

COA of Formula: C9H10O3. Bye, fridends, I hope you can learn more about C9H10O3, If you have any questions, you can browse other blog as well. See you lster.

Reference:
Isothiazole – Wikipedia,
,Isothiazole – ScienceDirect.com

In 2019.0 J AM CHEM SOC published article about H REDUCTIVE ELIMINATION; C-H; OXIDATION LEVEL; ARYL BROMIDES; CARBONYL ALLYLATION; AROMATIC-ALDEHYDES; O-H; ENANTIOSELECTIVE ADDITION; DIRECT ACYLATION; ORGANIC HALIDES in [Swyka, Robert A.; Zhang, Wandi; Krische, Michael J.] Univ Texas Austin, Dept Chem, Austin, TX 78712 USA; [Richardson, Jeffery] Eli Lilly & Co Ltd, Discovery Chem Res & Technol, Windlesham GU20 6PH, Surrey, England; [Ruble, J. Craig] Eli Lilly & Co, Discovery Chem Res & Technol, Indianapolis, IN 46285 USA in 2019.0, Cited 82.0. The Name is 2,5-Dimethoxybenzaldehyde. Through research, I have a further understanding and discovery of 93-02-7. Product Details of 93-02-7

The first intermolecular carbonyl arylations via transfer hydrogenative reductive coupling are described. Using rhodium catalysts modified by (Bu2PMe)-Bu-t, sodium formate-mediated reductive coupling of aryl iodides with aldehydes occurs in a chemoselective fashion in the presence of protic functional groups and lower halides. This work expands the emerging paradigm of transfer hydrogenative coupling as an alternative to preformed carbanions or metallic reductants in C=X addition.

Product Details of 93-02-7. About 2,5-Dimethoxybenzaldehyde, If you have any questions, you can contact Swyka, RA; Zhang, WD; Richardson, J; Ruble, JC; Krische, MJ or concate me.

Reference:
Isothiazole – Wikipedia,
,Isothiazole – ScienceDirect.com

In 2019.0 J ENZYM INHIB MED CH published article about ALZHEIMERS-DISEASE; BUTYRYLCHOLINESTERASE INHIBITORS; POLY(ADP-RIBOSE) POLYMERASE-1; POTENT; ACETYLCHOLINESTERASE; DERIVATIVES; DISCOVERY; THERAPY; CANCER; CHALCONE in [Gao, Cheng-Zhi; Dong, Wei; Cui, Zhi-Wen; Yuan, Qiong; Wu, Qing-Ming; Min, Zhen-Li] Wuhan Univ Sci & Technol, Hubei Prov Key Lab Occupat Hazard Identificat & C, Wuhan 430081, Hubei, Peoples R China; [Hu, Xia-Min] Shanghai Univ Med & Hlth Sci, Coll Pharm, Shanghai, Peoples R China; [Han, Xianlin; Min, Zhen-Li] Univ Texas Hlth Sci Ctr San Antonio, Barshop Inst Longev & Aging Studies, San Antonio, TX 78229 USA; [Xu, Yao] Wuhan Univ Sci & Technol, Coll Life Sci & Hlth, Wuhan, Hubei, Peoples R China in 2019.0, Cited 37.0. The Name is 2,5-Dimethoxybenzaldehyde. Through research, I have a further understanding and discovery of 93-02-7. HPLC of Formula: C9H10O3

A series of new Olaparib derivatives was designed and synthesized, and their inhibitory activities against poly (ADP-ribose) polymerases-1 (PARP-1) enzyme and cancer cell line MDA-MB-436 in vitro were evaluated. The results showed that compound 5l exhibited the most potent inhibitory effects on PARP-1 enzyme (16.10 +/- 1.25 nM) and MDA-MB-436 cancer cell (11.62 +/- 2.15 mu M), which was close to that of Olaparib. As a PARP-1 inhibitor had been reported to be viable to neuroprotection, in order to search for new multitarget-directed ligands (MTDLs) for the treatment of Alzheimer’s disease (AD), the inhibitory activities of the synthesized compounds against the enzymes AChE (from electric eel) and BChE (from equine serum) were also tested. Compound 5l displayed moderate BChE inhibitory activity (9.16 +/- 0.91 mu M) which was stronger than neostigmine (12.01 +/- 0.45 mu M) and exhibited selectivity for BChE over AChE to some degree. Molecular docking studies indicated that 5l could bind simultaneously to the catalytic active of PARP-1, but it could not interact well with huBChE. For pursuit of PARP-1 and BChE dual-targeted inhibitors against AD, small and flexible non-polar groups introduced to the compound seemed to be conducive to improving its inhibitory potency on huBChE, while keeping phthalazine-1-one moiety unchanged which was mainly responsible for PARP-1 inhibitory activity. Our research gave a clue to search for new agents based on AChE and PARP-1 dual-inhibited activities to treat Alzheimer’s disease.

HPLC of Formula: C9H10O3. Welcome to talk about 93-02-7, If you have any questions, you can contact Gao, CZ; Dong, W; Cui, ZW; Yuan, Q; Hu, XM; Wu, QM; Han, XL; Xu, Y; Min, ZL or send Email.

Reference:
Isothiazole – Wikipedia,
,Isothiazole – ScienceDirect.com

Safety of 2,5-Dimethoxybenzaldehyde. Authors Chauhan, D; George, G; Sridhar, SNC; Bhatia, R; Paul, AT; Monga, V in WILEY-V C H VERLAG GMBH published article about in [Chauhan, Divya; Bhatia, Rohit; Monga, Vikramdeep] ISF Coll Pharm, Dept Pharmaceut Chem, Moga 142001, Punjab, India; [George, Ginson; Sridhar, S. N. C.; Paul, Atish T.] Birla Inst Technol & Sci, Dept Pharm, Lab Nat Prod Chem, Pilani Campus, Pilani 333031, Rajasthan, India in 2019.0, Cited 27.0. The Name is 2,5-Dimethoxybenzaldehyde. Through research, I have a further understanding and discovery of 93-02-7

A series of rhodanine-3-acetic acid derivatives were synthesized via Knoevenagel condensation of rhodanine-3-acetic acid with various substituted aromatic aldehydes. The synthesized derivatives were screened in vitro for understanding the inhibitory potential towards pancreatic lipase (PL), a key enzyme responsible for the digestion of dietary fats. Derivative 8f exhibited a potential inhibitory activity towards PL (IC50 =( )5.16 mu M), comparable to that of the standard drug, orlistat (0.99 mu M). An increase in the density of the aromatic ring resulted in potential PL inhibition. The enzyme kinetics of 8f exhibited a reversible competitive-type inhibition, similar to that of orlistat. Derivative 8f exhibited a MolDock score of -125.19 kcal/mol in docking studies, and the results were in accordance with their PL inhibitory potential. Furthermore, the reactive carbonyl group of 8f existed at a distance adjacent to Ser152 (approximate to 3 angstrom) similar to that of orlistat. Molecular dynamics simulation (10 ns) of the 8f-PL complex revealed a stable binding conformation of 8f in the active site of PL (maximum root mean square displacement of approximate to 2.25 angstrom). The present study identified novel rhodanine-3-acetic acid derivatives with promising PL inhibitory potential, and further lead optimization might result in potent PL inhibitors.

Safety of 2,5-Dimethoxybenzaldehyde. About 2,5-Dimethoxybenzaldehyde, If you have any questions, you can contact Chauhan, D; George, G; Sridhar, SNC; Bhatia, R; Paul, AT; Monga, V or concate me.

Reference:
Isothiazole – Wikipedia,
,Isothiazole – ScienceDirect.com

Product Details of 93-02-7. Authors Ximenis, M; Mulet, J; Sala, S; Sala, F; Criado, M; Gonzalez-Muniz, R; de Vega, MJP in MDPI published article about in [Ximenis, Marta; Gonzalez-Muniz, Rosario; Perez de Vega, Maria Jesus] CSIC, IQM, Inst Quim Med, Juan Cierva 3, Madrid 28006, Spain; [Mulet, Jose; Sala, Salvador; Sala, Francisco; Criado, Manuel] Univ Miguel Hernandez, CSIC, Inst Neurociencias, Sant Joan dAlacant 03050, Spain in 2021.0, Cited 65.0. The Name is 2,5-Dimethoxybenzaldehyde. Through research, I have a further understanding and discovery of 93-02-7

The alpha 7 nicotinic acetylcholine receptor (alpha 7 nAChR) is a ligand-gated ion channel that is involved in cognition disorders, schizophrenia, pain, and inflammation. Allosteric modulation of this receptor might be advantageous to reduce the toxicity in comparison with full agonists. Our previous results obtained with some hydroxy-chalcones, which were identified as positive allosteric modulators (PAMs) of alpha 7 nAChR, prompted us to evaluate the potential of some structurally related naturally occurring flavonoids and curcuminoids and some synthetic curcumin analogues, with the aim of identifying new allosteric modulators of the alpha 7 nAChR. Biological evaluation showed that phloretin, demethoxycurcumin, and bis-demethoxicurcuming behave as PAMs of alpha 7 nAChR. In addition, some new curcumin derivatives were able to enhance the signal evoked by ACh; the activity values found for the tetrahydrocurcuminoid analog 23 were especially promising.

Product Details of 93-02-7. Welcome to talk about 93-02-7, If you have any questions, you can contact Ximenis, M; Mulet, J; Sala, S; Sala, F; Criado, M; Gonzalez-Muniz, R; de Vega, MJP or send Email.

Reference:
Isothiazole – Wikipedia,
,Isothiazole – ScienceDirect.com

Recently I am researching about CHALCONE DERIVATIVES; BIOLOGICAL-ACTIVITIES; MOLECULAR-PROPERTIES; LICOCHALCONE; PREDICTION; DISCOVERY; GROWTH; SERIES; AGENTS, Saw an article supported by the Coordination for the Improvement of Higher Education Personnel (CAPES)Coordenacao de Aperfeicoamento de Pessoal de Nivel Superior (CAPES) [001]; National Council for Scientific and Technological Development (CNPq)Conselho Nacional de Desenvolvimento Cientifico e Tecnologico (CNPQ) [471129/2013-5, 309957/2019-2, 306251/2016-7, 429322/2018-6]; State of Sao Paulo Research Foundation (FAPESP)Fundacao de Amparo a Pesquisa do Estado de Sao Paulo (FAPESP) [2014/18330-0, 2018/15083-2]; Fundacao de Apoio a Pesquisa e Extensa de Sao Jose do Rio Preto (FAPERP); Multiuser Centre for Biomolecular Innovation (FAPESP) [2009/53989-4]; National Institute of Science and Technology – INCT BioNat Biodiversity and Natural Products [CNPq 465637/2014-0, FAPESP 2014/50926-0]; FAPESPFundacao de Amparo a Pesquisa do Estado de Sao Paulo (FAPESP) [2014/18577-5, 2016/08084-7, 2017/09245-7]. Published in BENTHAM SCIENCE PUBL LTD in SHARJAH ,Authors: Marques, BC; Santos, MB; Anselmo, DB; Monteiro, DA; Gomes, E; Saiki, MFC; Rahal, P; Rosalen, PL; Sardi, JCO; Regasini, LO. The CAS is 93-02-7. Through research, I have a further understanding and discovery of 2,5-Dimethoxybenzaldehyde. HPLC of Formula: C9H10O3

Background: Chalcones substituted by methoxyl groups have presented a broad spectrum of bioactivities, including antifungal, antibacterial and antiproliferative effects. However, a clear and unambiguous investigation about the relevance of this substituent on the chalcone framework has not been described. Objective: The purpose of this work is to assess the antibacterial, antifungal and antiproliferative activities of the two series of seventeen synthesized regioisomeric methoxychalcones. Series I and II were constituted by cbalcones substituted by methoxyl groups on rings A (5-12) and B (13-21), respectively. In addition, the library of methoxychalcones was submitted to in silico drug-likeness and pharmacokinetics properties predictions. Methods: Methoxychalcones were synthesized and their structures were confirmed by NMR spectral data analyses. Evaluations of antimicrobial activity were performed against five species of Candida, two Gram-negative and five Gram-positive species. For antiproliferative activity, methoxychalcones were evaluated against four human tumorigenic cell lines, as well as human non-tumorigenic keratinocytes. Drug-likeness and pharmacokinetics properties were predicted using Molinspiration and PreADMET toolkits. Results: In general, chalcones of series I are the most potent antifungal, antibacterial and antiproliferative agents. 3′, 4′, 5′-Trimethoxychalcone (12) demonstrated potent antifungal activity against Candida krusei (MIC = 3.9 mu g/mL), eight times more potent than fluconazole (reference antifungal drug). 3′-Methoxychalcone (6) displayed anti-Pseudomonas activity (MIC = 7.8 mu g/mL). 2′,5′-Dimethoxychalcone (9) displayed potent antiproliferative effect against C-33A (cervix), A-431 (skin) and MCF-7 (breast), with IC50 values ranging from 7.7 to 9.2 mu M. Its potency was superior to curcumin (reference antiproliferative compound), which exhibited IC50 values ranging from 10.4 to 19.0 mu M. Conclusion: Our studies corroborated the relevance of methoxychalcones as antifungal, antibacterial and antiproliferative agents. In addition, we elucidated influence of the position and number of methoxyl groups toward bioactivity. In silico predictions indicated good drug-likeness and pharmacokinetics properties to the library of methoxychalcones.

Welcome to talk about 93-02-7, If you have any questions, you can contact Marques, BC; Santos, MB; Anselmo, DB; Monteiro, DA; Gomes, E; Saiki, MFC; Rahal, P; Rosalen, PL; Sardi, JCO; Regasini, LO or send Email.. HPLC of Formula: C9H10O3

Reference:
Isothiazole – Wikipedia,
,Isothiazole – ScienceDirect.com

Authors Dyachenko, IV; Dyachenko, VD; Dorovatovskii, PV; Khrustalev, VN; Nenajdenko, VG in SPRINGER published article about in [Dyachenko, Ivan, V; Dyachenko, Vladimir D.] Luhansk T Shevchenko Natl Univ, 2 Oboronnaya St, UA-91011 Lugansk, Ukraine; [Dorovatovskii, Pavel, V; Khrustalev, Victor N.] Kurchatov Inst, Natl Res Ctr, 1 Akad Kurchatova Sq, Moscow 123182, Russia; [Khrustalev, Victor N.] RUDN Univ, 6 Miklukho Maklaya St, Moscow 117198, Russia; [Nenajdenko, Valentine G.] Moscow MV Lomonosov State Univ, 1 Build 3 Leninskie Gory, Moscow 119991, Russia in 2019.0, Cited 24.0. Safety of 2,5-Dimethoxybenzaldehyde. The Name is 2,5-Dimethoxybenzaldehyde. Through research, I have a further understanding and discovery of 93-02-7

The multicomponent reaction of aromatic and heteroaromatic aldehydes, malonodithioamide, 1-(cyclohex-1-en-1-yl)piperidine, and alkylating reagents was studied. A wide range of new 2-(alkylsulfanyl)-4-aryl(hetaryl)-5,6,7,8-tetrahydroquinoline-3-carbonitriles were synthesized, and their molecular and crystalline structures were studied by X-ray structural analysis.

Welcome to talk about 93-02-7, If you have any questions, you can contact Dyachenko, IV; Dyachenko, VD; Dorovatovskii, PV; Khrustalev, VN; Nenajdenko, VG or send Email.. Safety of 2,5-Dimethoxybenzaldehyde

Reference:
Isothiazole – Wikipedia,
,Isothiazole – ScienceDirect.com

Recently I am researching about HYDROGEN-SULFIDE; FLUORESCENT CHEMOSENSOR; SELECTIVE DETECTION; GOLD NANOPARTICLES; CU2+; SENSOR; CHEMISTRY; GAS; H2S; CHEMODOSIMETER, Saw an article supported by the Deanship of Scientific Research, Najran University [NU/MID/16/091]. Product Details of 93-02-7. Published in PERGAMON-ELSEVIER SCIENCE LTD in OXFORD ,Authors: Mahnashi, MH; Mahmoud, AM; Alkahtani, SA; Ali, R; El-Wekil, MM. The CAS is 93-02-7. Through research, I have a further understanding and discovery of 2,5-Dimethoxybenzaldehyde

Herein, a novel ON-OFF colorimetric and fluorometric chemosensor; 1N-allyl-2-(2, 5-dimethoxyphenyl)-4, 5-diphenyl-1H-imidazole (ADPPI), was constructed for sequential determination of Cu2+ and S2- ions in aqueous media. The interaction between chemosensor ADPPI and different metal cations was investigated using UV-VIS and fluorimetric spectroscopy. ADPPI showed a favorable and good interaction with Cu2+ ions producing blue colored solution peaked at 610 nm with blue fluorescence at lambda(em) = 447 nm. The produced complex between Cu2+ ions and ADPPI can be used as a cascade probe for detection of S2- ions. The detection limits (LODs) were 1.01 nM and 1.25 mu M for Cu2+ and S2- ions, respectively (the lowest between the family of colorimetric and fluorometric chemosensors). To further increase the applicability of the proposed method, Cu2+ and S2- ions concentrations were measured in environmental water samples. (c) 2019 Elsevier B.V. All rights reserved.

Product Details of 93-02-7. Welcome to talk about 93-02-7, If you have any questions, you can contact Mahnashi, MH; Mahmoud, AM; Alkahtani, SA; Ali, R; El-Wekil, MM or send Email.

Reference:
Isothiazole – Wikipedia,
,Isothiazole – ScienceDirect.com

In 2020.0 EUR J MED CHEM published article about OXIDOREDUCTASE 1 NQO1; DT-DIAPHORASE; OXIDATIVE STRESS; CANCER; CYTOTOXICITY; EXPRESSION; SENSITIVITY; METABOLISM; APOPTOSIS; REDUCTASE in [Wu, Li-Qiang; Liu, Zhao-Peng] Shandong Univ, Sch Pharmaceut Sci, Dept Med Chem, Key Lab Chem Biol,Minist Educ, Jinan 250012, Peoples R China; [Wu, Li-Qiang; Ma, Xin; Zhang, Chong] Xinxiang Med Univ, Sch Pharm, Xinxiang 453003, Henan, Peoples R China in 2020.0, Cited 44.0. The Name is 2,5-Dimethoxybenzaldehyde. Through research, I have a further understanding and discovery of 93-02-7. Safety of 2,5-Dimethoxybenzaldehyde

A novel series of 4-substituted-3,4-dihydrobenzo[h]quinoline-2,5,6(1H)-triones as NQO1-directed anti-tumor agents were designed, synthesized, biologically evaluated. Compounds 3n, 3o and 3j proved to be good NQO1 substrates that showed increased metabolic rates relative to that of beta-lapachone. In addition, 3n, 3o and 3j potently inhibited the growth of NQO1-rich breast cancer MCF-7 cell, liver hepatocellular HepG2 cell, and lung cancer A549 cell. In cellular mechanistic studies, the representative compound 3o triggered ROS generation depending on the NQO1 dose, and induce HepG2 cell apoptosis by the generated oxidative stress. In HepG2 xenografts mouse model, at the dose of 20 mg/kg, 3o remarkably suppressed the tumor growth without affecting the animal weights. (C) 2020 Elsevier Masson SAS. All rights reserved.

Safety of 2,5-Dimethoxybenzaldehyde. Welcome to talk about 93-02-7, If you have any questions, you can contact Wu, LQ; Ma, X; Zhang, C; Liu, ZP or send Email.

Reference:
Isothiazole – Wikipedia,
,Isothiazole – ScienceDirect.com