Category: 88-68-6

An article CYP enzymes, expressed within live human suspension cells, are superior to widely-used microsomal enzymes in identifying potent CYP1A1/CYP1B1 inhibitors: Identification of quinazolinones as CYP1A1/CYP1B1 inhibitors that efficiently reverse B[a] P toxicity and cisplatin resistance WOS:000460399800020 published article about HUMAN CYTOCHROME-P450 ENZYMES; IN-VITRO; CANCER-RISK; ESTROGEN METABOLISM; DRUG; HYDROXYLATION; POLYMORPHISM; DERIVATIVES; VALIDATION; INITIATION in [Sonawane, Vinay R.; Gatchie, Linda; Williams, Ibidapo S.; Chaudhuri, Bhabatosh] CYP Design Ltd, Innovat Ctr, 49 Oxford St, Leicester LE1 5XY, Leics, England; [Siddique, Mohd Usman Mohd; Jayaprakash, Venkatesan; Sinha, Barij N.] Birla Inst Technol, Dept Pharmaceut Sci & Technol, Ranchi 835215, Bihar, India; [Bharate, Sandip B.] CSIR Indian Inst Integrat Med, Med Chem Div, Cana Rd, Jammu 180001, Jammu & Kashmir, India in 2019, Cited 69. The Name is 2-Aminobenzamide. Through research, I have a further understanding and discovery of 88-68-6. SDS of cas: 88-68-6

Microsomal cytochrome P450 (CYP) enzymes, isolated from recombinant bacterial/insect/yeast cells, are extensively used for drug metabolism studies. However, they may not always portray how a developmental drug would behave in human cells with intact intracellular transport mechanisms. This study emphasizes the usefulness of human HEK293 kidney cells, grown in ‘suspension’ for expression of CYPs, in finding potent CYP1A1/CYP1B1 inhibitors, as possible anticancer agents. With live cell-based assays, quinazolinones 9i/9b were found to be selective CYP1A1/CYP1B1 inhibitors with IC50 values of 30/21 nM, and > 150-fold selectivity over CYP2/3 enzymes, whereas they were far less active using commercially-available CYP1A1/CYP1B1 microsomal enzymes (IC50, > 10/1.3-1.7 mu M). Compound 9i prevented CYP1A1-mediated benzo [a]pyrene-toxicity in normal fibroblasts whereas 9b completely reversed cisplatin resistance in PC-3/prostate, COR-L23/1ung, MIAPaCa-2/pancreatic and LS174T/colon cancer cells, underlining the human-cell-assays’ potential. Our results indicate that the most potent CYP1A1/CYP1B1 inhibitors would not have been identified if one had relied merely on microsomal enzymes.

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Thiomorpholine – Wikipedia,
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In 2020 SPECTROCHIM ACTA A published article about SOLUBLE FLUORESCENT-PROBE; ON CHEMOSENSOR; SENSOR; WATER; IONS; HOCL; PH in [Li, Yuanyuan; Liu, Lei] Jiangsu Univ, Jingjiang Coll, Zhenjiang 212013, Jiangsu, Peoples R China; [Tang, Yong] Jiangnan Univ, Sch Chem & Mat Engn, Wuxi 214122, Jiangsu, Peoples R China; [Wang, Yun; Ni, Liang] Jiangsu Univ, Sch Chem & Chem Engn, Zhenjiang 212013, Jiangsu, Peoples R China; [Han, Juan] Jiangsu Univ, Sch Food & Biol Engn, Zhenjiang 212013, Jiangsu, Peoples R China in 2020, Cited 31. The Name is 2-Aminobenzamide. Through research, I have a further understanding and discovery of 88-68-6. Quality Control of 2-Aminobenzamide

In this study, a new fluorescence probe HMAQ based on quinazoline and diaminomaleonitrile was constructed for sensing ClO- and Al3+. A fluorescence blue-shift with 102 nm together with a color change from golden-yellow to colorless was found by hypochlorite-induced hydrolysis of -CH = N- group to release the initial fluorophore. Besides, Al3+ could cause a 72-nm blue-shifted emission spectra and a color change from golden-yellow to brown. As expected, HMAQ exhibited a satisfactory selectivity and sensitivity to ClO-/Al3+ with a quick response. Most notably, the reversibility of the [HMAQ+Al3+] complex could be used to detect ClO- and Al3+ simultaneously without mutual interferences. The detection limits of HMAQ for ClO- and Al3+ were turned out to be 102 nM and 1.56 nM, respectively. The high-performance results of real-time detections demonstrated the enormous potential of HMAQ in real-water samples and living cells. (C) 2020 Published by Elsevier B.V.

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Thiomorpholine – Wikipedia,
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Product Details of 88-68-6. In 2020 J ORG CHEM published article about DERIVATIVES; COMPLEXES; IMINES; ENTRY in [Asskar, Ghada; Rivard, Michael; Martens, Thierry] Univ Paris Est, UPEC, CNRS, ICMPE,UMR 7182, F-94320 Thiais, France in 2020, Cited 40. The Name is 2-Aminobenzamide. Through research, I have a further understanding and discovery of 88-68-6.

In the presence of amines, the degradation of glutaconaldehyde in acidic medium can be prevented. By exploitation of this behavior, primary amines are transformed into their corresponding pyridinium salts, including those substrates that remain unreactive toward the Zincke salt, which is the reagent typically used to perform this transformation. The use of glutaconaldehyde also allows control of the nature of the counterion of the pyridinium with no need for additional salt metathesis reaction.

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Thiomorpholine – Wikipedia,
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Computed Properties of C7H8N2O. I found the field of Pharmacology & Pharmacy; Chemistry very interesting. Saw the article Styryl quinazolinones and its ethynyl derivatives induce myeloid differentiation published in 2019, Reprint Addresses Radhakrishnan, S; Tenen, DG; Kobayashi, SS (corresponding author), Natl Univ Singapore, Canc Sci Inst Singapore, Singapore 117599, Singapore.. The CAS is 88-68-6. Through research, I have a further understanding and discovery of 2-Aminobenzamide.

The tumor suppressor transcription factor CCAAT enhancer-binding protein alpha (C/EBP alpha) expression is down-regulated in myeloid leukemias and enhancement of C/EBP alpha expression induces granulocytic differentiation in leukemic cells. Previously we reported that Styryl quinazolinones induce myeloid differentiation in HL-60 cells by upregulating C/EBP alpha expression. To identify more potent molecule that can induce leukemic cell differentiation we synthesized and evaluated new series of styryl quinazolinones, ethynyl styryl quinazolinones, styryl quinolinones and thienopyrimidinones. Thienopyrimidinones were found toxic and styryl quinolinones were found inactive. Ethynyl styryl quinazolinone 39 and styryl quinazolinone 5 were found active on par with the earlier reported analogues 1 and 2 suggesting that the 5-nitro furan-2-yl styryl quinazolinones find a real promise in leukemic cell differentiation. The improved potency of 5 suggested that further modifications in the 5-nitro furan-2-yl styryl quinazolinones can be at the phenyl substitution at the 3-position of the quinazolinone ring apart from the 5-position of the heteroaryl ring.

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Thiomorpholine – Wikipedia,
,Thiomorpholine | C4H9NS – PubChem

Shamanth, S; Nagarakere, SC; Sagar, KS; Narayana, Y; Mamatha, M; Rangappa, KS; Kempegowda, M in [Shamanth, Sadashivamurthy; Sagar, Kunigal S.; Narayana, Yatheesh; Rangappa, Kanchugarakoppal S.; Kempegowda, Mantelingu] Univ Mysore, DOS Chem, Manasagangotri, Mysuru 570006, Karnataka, India; [Nagarakere, Sandhya C.] St Philomenas Coll, PG Dept Studies Chem, Mysuru, India; [Nagarakere, Sandhya C.] St Philomenas Coll, Res Ctr, Mysuru, India; [Mamatha, Mahesha] SRSMN Govt First Grade Coll, Barkur, India published T3P mediated intramolecular rearrangement of o-aminobenzamide to o-ureidobenzonitrile using isothiocyanates in 2021, Cited 38. Category: thiomorpholine. The Name is 2-Aminobenzamide. Through research, I have a further understanding and discovery of 88-68-6.

Current work describes the environmentally benign approach for the synthesis of o-ureidobenzonitriles, from o-aminobenzamides and isothiocyanates using T3P. Here, the conversion of thiourea to urea and amide to nitrile take place simultaneously via unprecedented intramolecular rearrangement. This protocol is operationally facile and offers wide variety of o-ureidobenzonitriles at room temperature in good to excellent yields.

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Thiomorpholine – Wikipedia,
,Thiomorpholine | C4H9NS – PubChem

An article A mechanistic insight into the acid catalyzed, one-pot synthesis of isoindole-fused quinazolin 4-ones WOS:000528568400001 published article about EFFICIENT in [Mondal, Mohabul A.; Mondal, Sudipta; Khan, Abdul A.] Jadavpur Univ, Dept Chem, Kolkata 700032, W Bengal, India in 2020, Cited 11. The Name is 2-Aminobenzamide. Through research, I have a further understanding and discovery of 88-68-6. Safety of 2-Aminobenzamide

One-pot synthesis of isoindole fused quinazolin 4-ones via intramolecular 1,3 hydride transfer in the presence of acid catalyst has been described. Substrate scope and mechanistic insights were investigated. Substituents on the amide side have a negligible influence on the key step and therefore the method have wide scope for accessing various bicyclic core structure.

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Thiomorpholine – Wikipedia,
,Thiomorpholine | C4H9NS – PubChem

Quality Control of 2-Aminobenzamide. Keivanloo, A; Bakherad, M; Mokhtarei, L in [Keivanloo, Ali; Bakherad, Mohammad; Mokhtarei, Lotfollah] Shahrood Univ Technol, Fac Chem, Shahrood 3619995161, Iran published Sodium 4-amino-5-hydroxy-7-sulfonaphthalene-2-sulfonate an efficient ligand for click reaction in water: Synthesis of 1,2,3-triazole pharmacophore linked-quinazolinone scaffold in 2020, Cited 42. The Name is 2-Aminobenzamide. Through research, I have a further understanding and discovery of 88-68-6.

Water soluble sodium 4-amino-5-hydroxy-7-sulfonaphthalene-2-sulfonate ligand was used successfully for the preparation of 1,2,3-triazoles pharmacophore linked-quinazolinone scaffold. The reaction of ethyl 4-oxo-3,4-dihydroquinazoline-2-carboxylate and related amide compounds with propargyl bromide afforded ethyl 4-oxo-3-(prop-2-yn-1-yl)-3,4-dihydroquinazoline-2-carboxylate and its amide derivatives. The reaction of propargylated compounds with azides catalyzed by copper (II) salt, in the presence of Sodium 4-amino-5-hydroxy-7-sulfonaphthalene-2-sulfonate as a ligand in water produced novel 1,2,3-triazole pharmacophore linked-quinazolinone-4-one scaffold with high-to-excellent yields. The ligand assisted in the click reaction and reduced loading of copper salt to 2 mol%. Simplicity, short reaction times, use of water as green solvent, and low catalyst loading are the main advantages of this procedure.

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Thiomorpholine – Wikipedia,
,Thiomorpholine | C4H9NS – PubChem

I found the field of Chemistry very interesting. Saw the article Synthesis of Quinazoline and Quinazolinone Derivatives via Ligand-Promoted Ruthenium-Catalyzed Dehydrogenative and Deaminative Coupling Reaction of 2-Aminophenyl Ketones and 2-Aminobenzamides with Amines published in 2019. Safety of 2-Aminobenzamide, Reprint Addresses Yi, CS (corresponding author), Marquette Univ, Dept Chem, Milwaukee, WI 53201 USA.. The CAS is 88-68-6. Through research, I have a further understanding and discovery of 2-Aminobenzamide

The in situ formed ruthenium catalytic system ([Ru]/L) was found to be highly selective for the dehydrogenative coupling reaction of 2-aminophenyl ketones with amines to form quinazoline products. The deaminative coupling reaction of 2-aminobenzamides with amines led to the efficient formation of quinazolinone products. The catalytic coupling method provides an efficient synthesis of quinazoline and quinazolinone derivatives without using any reactive reagents or forming any toxic byproducts.

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Thiomorpholine – Wikipedia,
,Thiomorpholine | C4H9NS – PubChem

Pismataro, MC; Felicetti, T; Bertagnin, C; Nizi, MG; Bonomini, A; Barreca, ML; Cecchetti, V; Jochmans, D; De Jonghe, S; Neyts, J; Loregian, A; Tabarrini, O; Massari, S in [Pismataro, Maria Chiara; Felicetti, Tommaso; Nizi, Maria Giulia; Barreca, Maria Letizia; Cecchetti, Violetta; Tabarrini, Oriana; Massari, Serena] Univ Perugia, Dept Pharmaceut Sci, Via Del Liceo 1, I-06123 Perugia, Italy; [Bertagnin, Chiara; Bonomini, Anna; Loregian, Arianna] Univ Padua, Dept Mol Med, Via Gabelli 63, I-35121 Padua, Italy; [Jochmans, Dirk; De Jonghe, Steven; Neyts, Johan] Katholieke Univ Leuven, Dept Microbiol Immunol & Transplantat, Rega Inst Med Res, Lab Virol & Chemotherapy, Herestr 49,Box 1043, B-3000 Leuven, Belgium published 1,2,4-Triazolo[1,5-a]pyrimidines: Efficient one-step synthesis and functionalization as influenza polymerase PA-PB1 interaction disruptors in 2021, Cited 46. Category: thiomorpholine. The Name is 2-Aminobenzamide. Through research, I have a further understanding and discovery of 88-68-6.

In the search for new anti-influenza virus (IV) compounds, we have identified the 1,2,4-triazolo[1,5-a] pyrimidine (TZP) as a very suitable scaffold to obtain compounds able to disrupt IV RNA-dependent RNA polymerase (RdRP) PA-PB1 subunits heterodimerization. In this work, in order to acquire further SAR insights for this class of compounds and identify more potent derivatives, we designed and synthesized additional series of analogues to investigate the role of the substituents around the TZP core. To this aim, we developed four facile and efficient one-step procedures for the synthesis of 5-phenyl-, 6- phenyl- and 7-phenyl-2-amino-[1,2,4]triazolo[1,5-a]pyrimidines, and 2-amino-5-phenyl-[1,2,4]triazolo[1,5-a]pyrimidin-7-ol. Two analogues having the ethyl carboxylate moiety at the C-2 position of the TZP were also prepared in good yields. Then, the scaffolds herein synthesized and two previous scaffolds were functionalized and evaluated for their anti-IAV activity, leading to the identification of compound 22 that showed both anti-PA-PB1 (IC50 = 19.5 mM) and anti-IAV activity (EC50 = 16 mM) at non-toxic concentrations, thus resulting among the most active TZP derivatives reported to date by us. A selection of the synthesized compounds, along with a set of in-house available analogues, was also tested against SARS-CoV-2. The most promising compound 49 from this series displayed an EC50 value of 34.47 mM, high-lighting the potential of the TPZ scaffold in the search for anti-CoV agents. (C) 2021 Elsevier Masson SAS. All rights reserved.

Welcome to talk about 88-68-6, If you have any questions, you can contact Pismataro, MC; Felicetti, T; Bertagnin, C; Nizi, MG; Bonomini, A; Barreca, ML; Cecchetti, V; Jochmans, D; De Jonghe, S; Neyts, J; Loregian, A; Tabarrini, O; Massari, S or send Email.. Category: thiomorpholine

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Thiomorpholine – Wikipedia,
,Thiomorpholine | C4H9NS – PubChem

HPLC of Formula: C7H8N2O. I found the field of Chemistry very interesting. Saw the article DMAP-Catalyzed One-Pot Synthesis of Quinazoline-2,4-diones from 2-Aminobenzamides and Di-tert-butyl Dicarbonate published in 2020, Reprint Addresses Li, G; Huang, HH (corresponding author), Peking Union Med Coll & Chinese Acad Med Sci, Beijing Key Lab Act Subst Discovery & Druggabil E, Inst Mat Med, Beijing 100050, Peoples R China.; Li, G; Huang, HH (corresponding author), Peking Union Med Coll & Chinese Acad Med Sci, Chinese Acad Med Sci, Key Lab AntiDR TB Innovat Drug Res, Inst Mat Med, Beijing 100050, Peoples R China.. The CAS is 88-68-6. Through research, I have a further understanding and discovery of 2-Aminobenzamide.

The one-pot synthesis of quinazoline-2,4-diones was developed in the presence of 4-dimethylaminopyridine (DMAP) by metal-free catalysis. The commercially available (Boc)(2)O acted as a key precursor in the construction of the 2-position carbonyl of quinazolinediones. The p-methoxybenzyl (PMB)-activated hetero- cyclization could smoothly proceed at room temperature instead of the microwave condition. This strategy is compatible with a variety of substrates with different functional groups. Furthermore, this protocol was utilized to smoothly prepare Zenarestat with a total yield of 70%.

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Reference:
Thiomorpholine – Wikipedia,
,Thiomorpholine | C4H9NS – PubChem