Tag: M.W=100-150

I found the field of Pharmacology & Pharmacy very interesting. Saw the article Novel Phenyldiazenyl Fibrate Analogues as PPAR alpha/gamma/delta Pan-Agonists for the Amelioration of Metabolic Syndrome published in 2019.0. Application In Synthesis of 2-(4-Aminophenyl)ethanol, Reprint Addresses Giampietro, L (corresponding author), Univ G dAnnunzio, Dept Pharm, Via Vestini 31, I-66100 Chieti, Italy.; Loiodice, F (corresponding author), Univ Bari Aldo Moro, Dept Pharm Drug Sci, Via E Orabona 4, I-70126 Bari, Italy.; Lavecchia, A (corresponding author), Univ Napoli Federico II, Drug Discovery Lab, Dept Pharm, Via D Montesano 49, I-80131 Naples, Italy.. The CAS is 104-10-9. Through research, I have a further understanding and discovery of 2-(4-Aminophenyl)ethanol

The development of PPAR alpha/gamma dual or PPAR alpha/gamma/S pan-agonists could represent an efficacious approach for a simultaneous pharmacological intervention on carbohydrate and lipid metabolism. Two series of new phenyldiazenyl fibrate derivatives of GL479, a previously reported PPAR alpha/gamma dual agonist, were synthesized and tested. Compound 12a was identified as a PPAR pan-agonist with moderate and balanced activity on the three PPAR isoforms (alpha, gamma, delta). Moreover, docking experiments showed that 12a adopts a different binding mode in PPARy compared to PPARa or PPARS, providing a structural basis for further structure-guided design of PPAR pan-agonists. The beneficial effects of 12a were evaluated both in vitro, on the expression of PPAR target key metabolic genes, and ex vivo in two rat tissue inflammatory models. The obtained results allow considering this compound as an interesting lead for the development of a new class of PPAR pan-agonists endowed with an activation profile exploitable for therapy of metabolic syndrome.

Application In Synthesis of 2-(4-Aminophenyl)ethanol. About 2-(4-Aminophenyl)ethanol, If you have any questions, you can contact Giampietro, L; Laghezza, A; Cerchia, C; Florio, R; Recinella, L; Capone, F; Ammazzalorso, A; Bruno, I; De Filippis, B; Fantacuzzi, M; Ferrante, C; Maccallini, C; Tortorella, P; Verginelli, F; Brunetti, L; Cama, A; Amoroso, R; Loiodice, F; Lavecchia, A or concate me.

Reference:
Amide – Wikipedia,
,Amide – an overview | ScienceDirect Topics

An article Scandium-catalyzed Michael addition of quinazolinones and vinylazaarenes WOS:000535721300001 published article about ALLYLIC SUBSTITUTION; FUNCTIONALIZATION; HYDROAMINATION; HETEROCYCLES; 2-PYRIDONES; ALKYLATION; DISCOVERY in [Zhang, Zhiguang; Dai, Siwei; Li, Ling; Jia, Chenyu; Zhang, Yong] Hebei Univ Sci & Technol, Coll Chem & Pharmaceut Engn, 26 Yuxiang Rd, Shijiazhuang 050018, Hebei, Peoples R China; [Li, Hao] East China Univ Sci & Technol, State Key Lab Bioengn Reactor, Shanghai Key Lab New Drug Design, 130 Meilong Rd, Shanghai 200237, Peoples R China; [Li, Hao] East China Univ Sci & Technol, Sch Pharm, 130 Meilong Rd, Shanghai 200237, Peoples R China in 2020, Cited 35. The Name is Benzo[d][1,2,3]triazin-4(3H)-one. Through research, I have a further understanding and discovery of 90-16-4. Quality Control of Benzo[d][1,2,3]triazin-4(3H)-one

We described a novel scandium-catalyzed selective Michael addition of quinazolinones and vinylazaarenes. The protocol proceeds smoothly to give diverse quinazolinone derivatives in moderate to excellent yields. The high practicality of this protocol was proved by excellent chemo selectivity and broad substrate and functional group compatibility. (C) 2020 Elsevier Ltd. All rights reserved.

About Benzo[d][1,2,3]triazin-4(3H)-one, If you have any questions, you can contact Zhang, ZG; Dai, SW; Li, L; Jia, CY; Zhang, Y; Li, H or concate me.. Quality Control of Benzo[d][1,2,3]triazin-4(3H)-one

Reference:
Patent; Guizhou University; Xue Wei; Zhang Juping; Zhang Cheng; Chen Lijuan; Wang Yihui; Li Pu; Li Qin; Ruan Xianghui; Wang Xiaobin; Wu Xiaoqiong; Wang Jun; (24 pag.)CN107602493; (2019); B;,
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

An article Hexokinase II Inhibitory Effect of Secondary Metabolites Derived from a Streptomyces sp. Associated with Mud Dauber Wasp WOS:000538917100001 published article about BACTERIAL SYMBIONTS; GLYCOLYSIS; CANCER; GERMINATION; ANSAMYCIN; PROVIDE in [Zhang, Xiu-Mei; Wang, Mei; Zheng, Dan; Feng, Ming-Kuan] Shandong Drug & Food Vocat Coll, Dept Pharm, Weihai 264210, Peoples R China; [Peng, Ai-Hong; Xie, Wei-Dong] Shandong Univ, Coll Marine Sci, Dept Pharm, Weihai 264209, Peoples R China in 2020, Cited 43. The Name is Benzo[d][1,2,3]triazin-4(3H)-one. Through research, I have a further understanding and discovery of 90-16-4. Recommanded Product: 90-16-4

Insect-microbial symbioses have vast biochemical diversity, which is beneficial to produce bioactive secondary metabolites. In this study, chemical examination of a Streptomyces sp. associated with a mud dauber wasp led to the isolation of fourteen compounds. Their structures were determined by spectroscopic methods and comparison with literature data. Among the isolates, compounds 1,2,3-benzotriazin-4(1H)-one and 4-(2-aminoethyl)phenyl acetate were first reported from this species. Bioactivities of the isolated compounds were assayed for the first time against hexokinase II. 4-(2-Aminoethyl)phenyl acetate, germicidin B, phenylacetic acid, isogermicidin A and germicidin C displayed significant inhibitory activity against hexokinase II, with the IC50 values of 5.11, 7.11, 7.15, 8.45 and 8.78 mu M, respectively.

Recommanded Product: 90-16-4. About Benzo[d][1,2,3]triazin-4(3H)-one, If you have any questions, you can contact Zhang, XM; Peng, AH; Xie, WD; Wang, M; Zheng, D; Feng, MK or concate me.

Reference:
Patent; Guizhou University; Xue Wei; Zhang Juping; Zhang Cheng; Chen Lijuan; Wang Yihui; Li Pu; Li Qin; Ruan Xianghui; Wang Xiaobin; Wu Xiaoqiong; Wang Jun; (24 pag.)CN107602493; (2019); B;,
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

In 2020 PHOSPHORUS SULFUR published article about ANTICANCER; DISCOVERY; LARGAZOLE in [Chen, Xiulei; Zhou, Zhen; Li, Zhong; Xu, Xiaoyong] East China Univ Sci & Technol, Sch Pharm, Shanghai Key Lab Chem Biol, Shanghai 200237, Peoples R China; [Li, Zhong; Xu, Xiaoyong] Shanghai Collaborat Innovat Ctr Biomfg Technol, Shanghai, Peoples R China in 2020, Cited 29. The Name is Benzo[d][1,2,3]triazin-4(3H)-one. Through research, I have a further understanding and discovery of 90-16-4. SDS of cas: 90-16-4

A series of novel 1,2,3-benzotriazin-4-one derivatives containing 4,5-dihydrothiazole-2-thiol were synthesized and characterized by H-1 NMR, C-13 NMR, F-19 NMR and HRMS. The bioassay results showed that compounds 3-(3-((4,5-dihydrothiazol-2-yl)thio)propyl)-7-methoxybenzo[d][1-3]triazin-4(3H)-one, 3-(3-((4,5-dihydrothiazol-2-yl)thio)propyl)-6-nitrobenzo[d][1-3]triazin-4(3H)-one, 7-chloro-3-(3-((4,5-dihydrothiazol-2-yl)thio)propyl)benzo[d][1-3]triazin-4(3H)-one exhibited good control efficacy against the cucumber root-knot nematode disease caused by Meloidogyne incognita at the concentration of 10.0 mg L-1 in vivo. Compound 7-chloro-3-(3-((4,5-dihydrothiazol-2-yl)thio)propyl)benzo[d][1-3]triazin-4(3H)-one showed excellent nematicidal activity with inhibition 68.3% at a concentration of 1.0 mg L-1. It suggested that the structure of 1,2,3-benzotriazin-4-one containing 4,5-dihydro-thiazole-2-thiol could be optimized further.

SDS of cas: 90-16-4. About Benzo[d][1,2,3]triazin-4(3H)-one, If you have any questions, you can contact Chen, XL; Zhou, Z; Li, Z; Xu, XY or concate me.

Reference:
Patent; Guizhou University; Xue Wei; Zhang Juping; Zhang Cheng; Chen Lijuan; Wang Yihui; Li Pu; Li Qin; Ruan Xianghui; Wang Xiaobin; Wu Xiaoqiong; Wang Jun; (24 pag.)CN107602493; (2019); B;,
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

Recommanded Product: Benzo[d][1,2,3]triazin-4(3H)-one. Recently I am researching about ANTICANCER; DISCOVERY; LARGAZOLE, Saw an article supported by the National Natural Science Foundation of ChinaNational Natural Science Foundation of China (NSFC) [21672061]; National Key Research Program of China [2018YFD0200105, 2017YFD0200505]; Fundamental Research Funds for the Central UniversitiesFundamental Research Funds for the Central Universities. Published in TAYLOR & FRANCIS LTD in ABINGDON ,Authors: Chen, XL; Zhou, Z; Li, Z; Xu, XY. The CAS is 90-16-4. Through research, I have a further understanding and discovery of Benzo[d][1,2,3]triazin-4(3H)-one

A series of novel 1,2,3-benzotriazin-4-one derivatives containing 4,5-dihydrothiazole-2-thiol were synthesized and characterized by H-1 NMR, C-13 NMR, F-19 NMR and HRMS. The bioassay results showed that compounds 3-(3-((4,5-dihydrothiazol-2-yl)thio)propyl)-7-methoxybenzo[d][1-3]triazin-4(3H)-one, 3-(3-((4,5-dihydrothiazol-2-yl)thio)propyl)-6-nitrobenzo[d][1-3]triazin-4(3H)-one, 7-chloro-3-(3-((4,5-dihydrothiazol-2-yl)thio)propyl)benzo[d][1-3]triazin-4(3H)-one exhibited good control efficacy against the cucumber root-knot nematode disease caused by Meloidogyne incognita at the concentration of 10.0 mg L-1 in vivo. Compound 7-chloro-3-(3-((4,5-dihydrothiazol-2-yl)thio)propyl)benzo[d][1-3]triazin-4(3H)-one showed excellent nematicidal activity with inhibition 68.3% at a concentration of 1.0 mg L-1. It suggested that the structure of 1,2,3-benzotriazin-4-one containing 4,5-dihydro-thiazole-2-thiol could be optimized further.

About Benzo[d][1,2,3]triazin-4(3H)-one, If you have any questions, you can contact Chen, XL; Zhou, Z; Li, Z; Xu, XY or concate me.. Recommanded Product: Benzo[d][1,2,3]triazin-4(3H)-one

Reference:
Patent; Guizhou University; Xue Wei; Zhang Juping; Zhang Cheng; Chen Lijuan; Wang Yihui; Li Pu; Li Qin; Ruan Xianghui; Wang Xiaobin; Wu Xiaoqiong; Wang Jun; (24 pag.)CN107602493; (2019); B;,
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

Recently I am researching about BINDING-SITES; P2X RECEPTORS; PURINERGIC RECEPTORS; DRUG-METABOLISM; P2Y1 RECEPTOR; IN-VIVO; ANTAGONISTS; DISCOVERY; LIGAND; RAT, Saw an article supported by the Life Science Stiftung [1011170009]; HZDR-Innovationsfonds; Sino-German Center for Research Promotion [GZ1236]; Fonds der Chemischen IndustrieFonds der Chemischen IndustrieEuropean Commission. Quality Control of 2-(4-Aminophenyl)ethanol. Published in ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER in ISSY-LES-MOULINEAUX ,Authors: Moldovan, RP; Wenzel, B; Teodoro, R; Neumann, W; Dukic-Stefanovic, S; Kraus, W; Rong, PJ; Deuther-Conrad, W; Hey-Hawkins, E; Krugel, U; Brust, P. The CAS is 104-10-9. Through research, I have a further understanding and discovery of 2-(4-Aminophenyl)ethanol

Purine nucleotides such as ATP and ADP are important extracellular signaling molecules in almost all tissues activating various subtypes of purinoreceptors. In the brain, the P2Y(1) receptor (P2Y(1)R) subtype mediates trophic functions like differentiation and proliferation, and modulates fast synaptic transmission, both suggested to be affected in diseases of the central nervous system. Research on P2Y(1)R is limited because suitable brain-penetrating P2Y(1)R-selective tracers are not yet available. Here, we describe the first efforts to develop an F-18-labeled PET tracer based on the structure of the highly affine and selective, non-nucleotidic P2Y(1)R allosteric modulator 1-(2-[2-(tert-butyl)phenoxy]pyridin-3-yl)-3-[4- (trifluoromethoxy)phenyl]urea (7). A small series of fluorinated compounds was developed by systematic modification of the p-(trifluoromethoxy)phenyl, the urea and the 2-pyridyl subunits of the lead compound 7. Additionally, the p-(trifluoromethoxy)phenyl subunit was substituted by carborane, a boron-rich cluster with potential applicability in boron neutron capture therapy (BNCT). By functional assays, the new fluorinated derivative 1-{2-[2-(tert-butyl)phenoxy]pyridin-3-yl}-3-[4-(2-fluoroethyl) phenyl]urea (18) was identified with a high P2Y(1)R antagonistic potency (IC50 = 10 nM). Compound [F-18] 18 was radiosynthesized by using tetra-n-butyl ammonium [F-18]fluoride with high radiochemical purity, radiochemical yield and molar activities. Investigation of brain homogenates using hydrophilic interaction chromatography (HILIC) revealed [F-18]fluoride as major radiometabolite. Although [F-18]18 showed fast in vivo metabolization, the high potency and unique allosteric binding mode makes this class of compounds interesting for further optimizations and investigation of the theranostic potential as PET tracer and BNCT agent. (C) 2019 Elsevier Masson SAS. All rights reserved.

Quality Control of 2-(4-Aminophenyl)ethanol. About 2-(4-Aminophenyl)ethanol, If you have any questions, you can contact Moldovan, RP; Wenzel, B; Teodoro, R; Neumann, W; Dukic-Stefanovic, S; Kraus, W; Rong, PJ; Deuther-Conrad, W; Hey-Hawkins, E; Krugel, U; Brust, P or concate me.

Reference:
Amide – Wikipedia,
,Amide – an overview | ScienceDirect Topics

Recommanded Product: 104-10-9. Authors Wu, JL; Liu, SH; Huang, JL; Cui, Y; Ma, PW; Wu, DC; Matyjaszewski, K in AMER CHEMICAL SOC published article about in [Wu, Jinlun; Liu, Shaohong; Huang, Junlong; Cui, Yin; Ma, Pengwei; Wu, Dingcai] Sun Yat Sen Univ, Sch Chem, Key Lab Polymer Composite & Funct Mat, Minist Educ, Guangzhou 510275, Peoples R China; [Matyjaszewski, Krzysztof] Carnegie Mellon Univ, Dept Chem, Pittsburgh, PA 15213 USA in 2021.0, Cited 57.0. The Name is 2-(4-Aminophenyl)ethanol. Through research, I have a further understanding and discovery of 104-10-9

Porous polymers have attracted tremendous interest in lithium-sulfur batteries due to the combination of good physical confinement and chemical immobilization to suppress the polysulfide shuttle. Currently, the development of facile and effective methods for fabrication of porous polymers with hierarchical porous structures, strong polar species, and efficient charge-transfer pathways is significant yet challenging, which is crucial for high-performance sulfur cathodes. Herein, for the first time, we present the successful development of a novel class of advanced hierarchical porous polymer nanosheets (AHPPNs) based on a union of surface-initiated atom transfer radical polymerization and a cross-linking-induced coassembly strategy. Due to their well-defined nanoarchitectures, AHPPNs are capable of providing a commendable shuttle-suppressing shield for polysulfides via strong chemisorption, hierarchical porous structures for immobilizing sulfur and relieving volume change, and shortened pathways for ions and electrons. Benefiting from these synergistic effects, the lithium-sulfur batteries assembled with S@AHPPNs cathodes exhibit greatly enhanced rate performance and long stable cycle capability.

Recommanded Product: 104-10-9. About 2-(4-Aminophenyl)ethanol, If you have any questions, you can contact Wu, JL; Liu, SH; Huang, JL; Cui, Y; Ma, PW; Wu, DC; Matyjaszewski, K or concate me.

Reference:
Amide – Wikipedia,
,Amide – an overview | ScienceDirect Topics

In 2019.0 ACS CATAL published article about ONE-POT SYNTHESIS; N-ALKYLATION; ALPHA-METHYLATION; METHANOL; COMPLEXES; KETONES; AMINES; EFFICIENT; FUNCTIONALIZATION; ISOBUTANOL in [Polidano, Kurt; Morrill, Louis C.] Cardiff Univ, Sch Chem, Cardiff Catalysis Inst, Main Bldg,Pk Pl, Cardiff CF10 3AT, S Glam, Wales; [Williams, Jonathan M. J.] Univ Bath, Dept Chem, Bath BA2 7AY, Avon, England in 2019.0, Cited 79.0. The Name is 2-(4-Aminophenyl)ethanol. Through research, I have a further understanding and discovery of 104-10-9. Computed Properties of C8H11NO

Herein we report the iron-catalyzed beta-C(sp(3))-methylation of primary alcohols using methanol as a Cl building block. This borrowing hydrogen approach employs a well-defined bench-stable (cyclopentadienone)iron(0) carbonyl complex as precatalyst (5 mol %) and enables a diverse selection of substituted 2-arylethanols to undergo beta-C(sp(3))-methylation in good isolated yields (24 examples, 65% average yield).

About 2-(4-Aminophenyl)ethanol, If you have any questions, you can contact Polidano, K; Williams, JMJ; Morrill, LC or concate me.. Computed Properties of C8H11NO

Reference:
Amide – Wikipedia,
,Amide – an overview | ScienceDirect Topics

An article Synthesis of 3-indolylmethyl substituted (pyrazolo/benzo)triazinone derivatives under Pd/Cu-catalysis: Identification of potent inhibitors of chorismate mutase (CM) WOS:000487812000051 published article about 1,2,3-BENZOTRIAZIN-4-ONE DERIVATIVES; NEMATOCIDAL ACTIVITIES; INDOLES; 1-ALKYNES; RV1885C; 2-HETEROARYL; DOCKING; PROTEIN; 2-ARYL in [Reddy, Gangireddy Sujeevan; Snehalatha, Ampalam Venkata; Edwin, Rebecca Kristina; Hossain, Kazi Amirul; Misra, Parimal; Pal, Manojit] Dr Reddys Inst Life Sci, Univ Hyderabad Campus, Hyderabad 500046, India; [Reddy, Gangireddy Sujeevan; Giliyaru, Varadaraj Bhat; Hariharapura, Raghu Chandrashekhar; Shenoy, G. Gautham] Manipal Acad Higher Educ, Manipal Coll Pharmaceut Sci, Manipal 576104, Karnataka, India in 2019, Cited 38. Recommanded Product: Benzo[d][1,2,3]triazin-4(3H)-one. The Name is Benzo[d][1,2,3]triazin-4(3H)-one. Through research, I have a further understanding and discovery of 90-16-4

The chorismate mutase (CM) is considered as an attractive target for the identification of potential antitubercular agents due to its absence in animals but not in bacteria. A series of 3-indolylmethyl substituted pyrazolo-triazinone derivatives were designed and docked into CM in silico as potential inhibitors. These compounds were efficiently synthesized using the Pd/Cu-catalyzed coupling-cyclization in a single pot involving the construction of indole ring. The methodology was later extended to the preparation of corresponding benzo analogs of pyrazolotriazinones i.e. 3-indolylmethyl substituted benzotriazinone derivatives. Several of these novel compounds showed significant inhibition of CM when tested in vitro at 30 mu M. The SAR (Structure-Activity-Relationship) studies suggested that benzotriazinone moiety was more favorable over the pyrazolotriazinone ring. The two best active compounds showed IC50 similar to 0.4-0.9 mu M (better than the reference/known compounds used) and no toxicity till 30 mu M in vitro.

Recommanded Product: Benzo[d][1,2,3]triazin-4(3H)-one. About Benzo[d][1,2,3]triazin-4(3H)-one, If you have any questions, you can contact Reddy, GS; Snehalatha, AV; Edwin, RK; Hossain, KA; Giliyaru, VB; Hariharapura, RC; Shenoy, GG; Misra, P; Pal, M or concate me.

Reference:
Patent; Guizhou University; Xue Wei; Zhang Juping; Zhang Cheng; Chen Lijuan; Wang Yihui; Li Pu; Li Qin; Ruan Xianghui; Wang Xiaobin; Wu Xiaoqiong; Wang Jun; (24 pag.)CN107602493; (2019); B;,
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

Authors Reddy, GS; Snehalatha, AV; Edwin, RK; Hossain, KA; Giliyaru, VB; Hariharapura, RC; Shenoy, GG; Misra, P; Pal, M in ACADEMIC PRESS INC ELSEVIER SCIENCE published article about 1,2,3-BENZOTRIAZIN-4-ONE DERIVATIVES; NEMATOCIDAL ACTIVITIES; INDOLES; 1-ALKYNES; RV1885C; 2-HETEROARYL; DOCKING; PROTEIN; 2-ARYL in [Reddy, Gangireddy Sujeevan; Snehalatha, Ampalam Venkata; Edwin, Rebecca Kristina; Hossain, Kazi Amirul; Misra, Parimal; Pal, Manojit] Dr Reddys Inst Life Sci, Univ Hyderabad Campus, Hyderabad 500046, India; [Reddy, Gangireddy Sujeevan; Giliyaru, Varadaraj Bhat; Hariharapura, Raghu Chandrashekhar; Shenoy, G. Gautham] Manipal Acad Higher Educ, Manipal Coll Pharmaceut Sci, Manipal 576104, Karnataka, India in 2019, Cited 38. HPLC of Formula: C7H5N3O. The Name is Benzo[d][1,2,3]triazin-4(3H)-one. Through research, I have a further understanding and discovery of 90-16-4

The chorismate mutase (CM) is considered as an attractive target for the identification of potential antitubercular agents due to its absence in animals but not in bacteria. A series of 3-indolylmethyl substituted pyrazolo-triazinone derivatives were designed and docked into CM in silico as potential inhibitors. These compounds were efficiently synthesized using the Pd/Cu-catalyzed coupling-cyclization in a single pot involving the construction of indole ring. The methodology was later extended to the preparation of corresponding benzo analogs of pyrazolotriazinones i.e. 3-indolylmethyl substituted benzotriazinone derivatives. Several of these novel compounds showed significant inhibition of CM when tested in vitro at 30 mu M. The SAR (Structure-Activity-Relationship) studies suggested that benzotriazinone moiety was more favorable over the pyrazolotriazinone ring. The two best active compounds showed IC50 similar to 0.4-0.9 mu M (better than the reference/known compounds used) and no toxicity till 30 mu M in vitro.

About Benzo[d][1,2,3]triazin-4(3H)-one, If you have any questions, you can contact Reddy, GS; Snehalatha, AV; Edwin, RK; Hossain, KA; Giliyaru, VB; Hariharapura, RC; Shenoy, GG; Misra, P; Pal, M or concate me.. HPLC of Formula: C7H5N3O

Reference:
Patent; Guizhou University; Xue Wei; Zhang Juping; Zhang Cheng; Chen Lijuan; Wang Yihui; Li Pu; Li Qin; Ruan Xianghui; Wang Xiaobin; Wu Xiaoqiong; Wang Jun; (24 pag.)CN107602493; (2019); B;,
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics