Category: amides-buliding-blocks

I found the field of Pharmacology & Pharmacy very interesting. Saw the article 6-Amino[1,2,5]oxadiazolo[3,4-b]pyrazin-5-ol Derivatives as Efficacious Mitochondrial Uncouplers in STAM Mouse Model of Nonalcoholic Steatohepatitis published in 2020.0. HPLC of Formula: C13H13N, Reprint Addresses Hoehn, KL (corresponding author), Univ Virginia, Dept Pharmacol, Charlottesville, VA 22908 USA.; Hoehn, KL (corresponding author), Univ Virginia, Dept Med, Charlottesville, VA 22908 USA.; Hoehn, KL (corresponding author), Univ New South Wales, Sch Biotechnol & Biomol Sci, Kensington, NSW 2033, Australia.; Santos, WL (corresponding author), Virginia Tech, Dept Chem, Blacksburg, VA 24061 USA.; Santos, WL (corresponding author), Virginia Tech, Virginia Tech Ctr Drug Discovery, Blacksburg, VA 24061 USA.. The CAS is 91-00-9. Through research, I have a further understanding and discovery of Diphenylmethanamine

Small molecule mitochondrial uncouplers have recently garnered great interest for their potential in treating nonalcoholic steatohepatitis (NASH). In this study, we report the structure-activity relationship profiling of a 6-amino[1,2,5]oxadiazolo[3,4-b]pyrazin-5-ol core, which utilizes the hydroxy moiety as the proton transporter across the mitochondrial inner membrane. We demonstrate that a wide array of substituents is tolerated with this novel scaffold that increased cellular metabolic rates in vitro using changes in oxygen consumption rate as a readout. In particular, compound SHS4121705 (12i) displayed an EC50 of 4.3 mu M in L6 myoblast cells and excellent oral bioavailability and liver exposure in mice. In the STAM mouse model of NASH, administration of 12i at 25 mg kg(-1) day(-1) lowered liver triglyceride levels and improved liver markers such as alanine aminotransferase, NAFLD activity score, and fibrosis. Importantly, no changes in body temperature or food intake were observed. As potential treatment of NASH, mitochondrial uncouplers show promise for future development.

About Diphenylmethanamine, If you have any questions, you can contact Salamoun, JM; Garcia, CJ; Hargett, SR; Murray, JH; Chen, SY; Beretta, M; Alexopoulos, SJ; Shah, DP; Olzomer, EM; Tucker, SP; Hoehn, KL; Santos, WL or concate me.. HPLC of Formula: C13H13N

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

Chen, XL; Zhou, Z; Li, Z; Xu, XY 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 published Synthesis and nematicidal activities of 1,2,3-benzotriazin-4-one containing 4,5-dihydrothiazole-2-thiol derivatives against Meloidogyne incognita in 2020, Cited 29. 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.

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.

HPLC of Formula: C7H5N3O. 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

Authors Liu, B; Liu, CY; De Luca, HG; Pillai, SKR; Anthony, DB; Li, JH; Bismarck, A; Shaffer, MSP; Chan-Park, MB in ROYAL SOC CHEMISTRY published article about POLYIMIDE; NANOCOMPOSITES; STRENGTH; EPOXY in [Liu, Bo; Liu, Chengyin; Pillai, Suresh Kumar Raman; Li, Jianghua; Chan-Park, Mary B.] Nanyang Technol Univ, Sch Chem & Biomed Engn, 62 Nanyang Dr, Singapore 637459, Singapore; [De Luca, Hugo G.; Shaffer, Milo S. P.] Imperial Coll London, Dept Mat, London, England; [Anthony, David B.] Imperial Coll London, Dept Chem Engn, London, England; [Bismarck, Alexander] Univ Vienna, Facil Chem, Vienna, Austria; [Shaffer, Milo S. P.] Imperial Coll London, Dept Chem, London, England in 2019.0, Cited 27.0. Recommanded Product: 2-(4-Aminophenyl)ethanol. The Name is 2-(4-Aminophenyl)ethanol. Through research, I have a further understanding and discovery of 104-10-9

Polyimides (PI) generally have a high affinity for single-walled carbon nanotubes (SWNTs), but they suffer from poor solubility in most low boiling point organic solvents and low compatibility with common resins (such as epoxy) used in composites, limiting their suitability as dispersants. PI block copolymer systems containing reactive poly(ester carbonate) s have not yet been reported and are expected to act as effective reactive dispersing agents of SWNTs. Herein, PI-derived block copolymers are synthesized via ring-opening copolymerization of lactide (LA) (a control monomer) and allyl-bearing 2-methyl-2-(allyloxycarbonyl)-propylene carbonate (MAC) from the OH-terminal ends of the PI block to produce PLA-PI-PLA (TB1, a control) and PMAC-PI-PMAC (TB2). The allyl pendant group of TB2 allows further facile functionalization to form a third series of epoxidized (EP) derivatives, i.e. PMACEP-block-PI-block-PMACEP (TB3). TB3 copolymer when mixed with a conventional structural epoxy resin forms blends that do not show inferior tensile properties compared with the epoxy, which is unusual. Furthermore, the mixing solvent tetrahydrofuran (THF) can be readily evaporated off after forming the blends. TB3-dispersed (2 wt%) SWNTs added to epoxy increased the tensile strength, modulus, and elongation at break of the resulting nanocomposite films by 40%, 34%, and 26% respectively, compared to the baseline epoxy resin. Furthermore, when TB3b triblock-dispersed SWNTs in epoxy were combined with fuzzy carbon fibers, i.e. carbon nanotube-grafted-carbon fibers (CNT-g-CF), a synergistic interfacial strength reinforcement was observed, together with shifting of the failure mode from the matrix interphase to the carbon fiber-grafted nanotube interface. The ultimate interfacial shear strength between the TB3-dispersed SWNT-epoxy matrix and the fuzzy carbon fibers (i.e., fibers having carbon nanotubes grown on them) measured via single fiber pull-out tests was 100 MPa, which was ca. 11% improvement over the baseline unsized carbon fiber in neat epoxy. To our knowledge, this is the first evidence of a synergistic enhancement in interfacial properties when fuzzy carbon fibers are combined with a SWNT-reinforced epoxy using the new epoxidized TB3 nanotube dispersing agent that forms a strong covalent TB3-epoxy interface. The new functionalizable TB3 synthesis route introduced here is generalizable to other PI-based copolymers with diverse functionalities and solvent compatibilities.

About 2-(4-Aminophenyl)ethanol, If you have any questions, you can contact Liu, B; Liu, CY; De Luca, HG; Pillai, SKR; Anthony, DB; Li, JH; Bismarck, A; Shaffer, MSP; Chan-Park, MB or concate me.. Recommanded Product: 2-(4-Aminophenyl)ethanol

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

An article Synthesis and Biological Activities of Some New Benzotriazinone Derivatives Based on Molecular Docking; Promising HepG2 Liver Carcinoma Inhibitors WOS:000523299700057 published article about PHARMACOLOGICAL EVALUATION; LIGANDS; GROWTH in [El Rayes, Samir M.; Ali, Ibrahim A. I.; Mahmoud, Mostafa A. A.] Suez Canal Univ, Fac Sci, Dept Chem, Ismailia 41529, Egypt; [Fathalla, Walid] Port Said Univ, Fac Engn, Phys & Math Engn Dept, Port Said 42526, Egypt in 2020, Cited 24. 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. Category: amides-buliding-blocks

In one-pot strategy, diazotization of methyl anthranilate 5 followed by addition of amino acid ester hydrochloride, we have prepared methyl-2-(4-oxobenzotriazin-3(4H)-yl)-alkanoates 6a-c. Starting with hydrazides 7a,b, N-alkyl-2-(4-oxobenzotriazin-3(4H)-yl)-alkanamides 9-10(a-h) and methyl-2-(2-(4-oxobenzotriazin-3(4H)-yl)alkanamido)alkanoates 11- 12(a-e) were prepared via azide coupling. Hydrazones 13-15 were prepared via condensation of hydrazides 7a,b with 4-methoxybenzaldehyde, 4-dimethylaminobenzaldehyde, and/or arabinose. Molecular docking was done for synthesized compounds using MOE 2008-10 software. The compounds 9a, 12a, 12c, 13a, 13b, and 14b have the most pronounced strong binding affinities toward the target E. coli Fab-H receptor, whereas compounds 3, 11e, 12e, and 13a have the most pronounced strong binding affinities toward the target vitamin D receptor. The in vitro antibacterial activities of the highest binding affinity docked compounds were tested against E. coli, Staphylococcus aureus, and Salmonella spp. Majority of the tested compounds showed effective positive results against E. coli, while they were almost inactive against Staphylococcus aureus and Salmonella spp. The in vitro cytotoxic activities of the highest binding affinity-docked compounds were tested against the human liver carcinoma cell line (HepG2). Some compounds showed potent cytotoxic activity with low IC50 values, especially for 3 (6.525 mu M) and 13a (10.97 mu M) than that for standard drug doxorubicin (2.06 mu M).

About Benzo[d][1,2,3]triazin-4(3H)-one, If you have any questions, you can contact El Rayes, SM; Ali, IAI; Fathalla, W; Mahmoud, MAA or concate me.. Category: amides-buliding-blocks

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 Development of novel benzimidazole-derived neddylation inhibitors for suppressing tumor growth in vitro and in vivo WOS:000604903800017 published article about NEDD8-ACTIVATING ENZYME-INHIBITOR; PROTEIN NEDDYLATION; IDENTIFICATION; PATHWAY; DEGRADATION; DISCOVERY; APOPTOSIS; LIGASES in [Chen, Xin; Mao, Fei; Wei, Jinlian; Xu, Yixiang; Li, Baoli; Zhu, Jin; Li, Jian] East China Univ Sci & Technol, State Key Lab Bioreactor Engn, Shanghai Key Lab New Drug Design, 130 Mei Long Rd, Shanghai 200237, Peoples R China; [Yang, Xi; Ni, Shuaishuai; Jia, Lijun] Shanghai Univ Tradit Chinese Med, Longhua Hosp, Canc Inst, Shanghai 200032, Peoples R China; [Li, Jian] Dali Univ, Coll Pharm & Chem, 5 Xue Ren Rd, Dali 671000, Yunnan, Peoples R China; [Li, Jian] East China Univ Sci & Technol, Frontiers Sci Ctr Materiobiol & Dynam Chem, 130 Mei Long Rd, Shanghai 200237, Peoples R China in 2021.0, Cited 41.0. COA of Formula: C13H13N. The Name is Diphenylmethanamine. Through research, I have a further understanding and discovery of 91-00-9

Ubiquitin-like protein neddylation is overactivated in various human cancers and correlates with disease progression, and targeting this pathway represents a valuable therapeutic strategy. Our previous work disclosed an antihypertensive agent, candesartan cilexetic (CDC), serves as a novel neddylation inhibitor for suppressing tumor growth by targeting Nedd8-activating enzyme (NAE). In this study, 42 benzimidazole derivatives were designed and synthesized based on lead compound CDC to improve the neddylation inhibition and anticancer efficacy. Optimal benzimidazole-derived 35 displayed superior neddylation inhibition in enzyme assay compared to CDC (IC50 = 5.51 mu M vs 16.43 mu M), along with promising target inhibitory activity and killing selectivity in cancer cell. The results of cellular mechanism research combined with tumor growth suppression in human lung cancer cell A549 in vivo, accompanied with docking model, revealed that 35 has the potential to be developed as a promising neddylation inhibitor for anticancer therapy. (C) 2020 Elsevier Masson SAS. All rights reserved.

About Diphenylmethanamine, If you have any questions, you can contact Chen, X; Yang, X; Mao, F; Wei, JL; Xu, YX; Li, BL; Zhu, J; Ni, SS; Jia, LJ; Li, J or concate me.. COA of Formula: C13H13N

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

Computed Properties of C13H13N. He, JH; Dong, J; Su, LB; Wu, SF; Liu, LX; Yin, SF; Zhou, YB in [He, Junhui; Su, Lebin; Wu, Shaofeng; Liu, Lixin; Yin, Shuang-Feng; Zhou, Yongbo] Hunan Univ, Coll Chem & Chem Engn, State Key Lab Chemo Biosensing & Chemometr, Changsha 410082, Peoples R China; [Dong, Jianyu] Hunan First Normal Univ, Dept Educ Sci, Changsha 410205, Peoples R China published Selective Oxidative Cleavage of 3-Methylindoles with Primary Amines Affording Quinazolinones in 2020.0, Cited 77.0. The Name is Diphenylmethanamine. Through research, I have a further understanding and discovery of 91-00-9.

A selective functionalization of C-C.C bonds toward N-C=O bonds is realized by an n-Bu4NI-catalyzed reaction of 3-methylindoles with primary amines using TBHP as the unique oxidant. The systematic process involves oxygenation, nitrogenation, ring-opening, and recyclization, affording a broad range of quinazolinones in good to excellent yields.

Computed Properties of C13H13N. About Diphenylmethanamine, If you have any questions, you can contact He, JH; Dong, J; Su, LB; Wu, SF; Liu, LX; Yin, SF; Zhou, YB or concate me.

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

An article Efficient synthesis of cyclic amidine-based fluorophores via 6 pi-electrocyclic ring closure WOS:000525512500017 published article about ONE-POT SYNTHESIS; FLUORESCENT-PROBES; SULFONYL; REARRANGEMENT; TACHYKININ; ALKYNES; ACCESS; FUNCTIONALIZATION; 1,2,3-TRIAZOLES; ANNULATION in [Li, Guofeng; Zhao, Man; Yao, Ying; Xu, Jiecheng; Xue, Jianzhong; Hu, Tao; Li, Min; Hong, Liang] Sun Yat Sen Univ, Sch Pharmaceut Sci, Guangdong Key Lab Chiral Mol & Drug Discovery, Guangzhou 510006, Peoples R China; [Xie, Junqiu; Mou, Lingyun; Zhang, Xiaowei; Guo, Xiaomin; Sun, Wangsheng; Zhang, Ming] Lanzhou Univ, Sch Basic Med Sci, Key Lab Preclin Study New Drugs Gansu Prov, Lanzhou 730000, Peoples R China; [Wang, Zheng] Peking Univ, Sch Chem Biol & Biotechnol, Guangdong Key Lab Nanomicro Mat Res, Shenzhen Grad Sch, Shenzhen 518055, Peoples R China in 2020, Cited 67. The Name is 2-(4-Aminophenyl)ethanol. Through research, I have a further understanding and discovery of 104-10-9. Recommanded Product: 104-10-9

Novel 10 pi-electron cyclic amidines with excellent fluorescence properties were synthesized by a general and efficient 6 pi-electrocyclic ring closure of ketenimine and imine starting from N-sulfonyl triazoles and arylamines. The photophysical properties of cyclic amidine fluorophores have been studied in detail and have shown good properties of a large Stokes shift, pH insensitivity, low cytotoxicity and higher photostability, which have great potential for biological imaging. Furthermore, this novel fluorophore was successfully applied to the localization of the NK-1 receptor in living systems.

Recommanded Product: 104-10-9. About 2-(4-Aminophenyl)ethanol, If you have any questions, you can contact Li, GF; Zhao, M; Xie, JQ; Yao, Y; Mou, LY; Zhang, XW; Guo, XM; Sun, WS; Wang, Z; Xu, JC; Xue, JZ; Hu, T; Zhang, M; Li, M; Hong, L or concate me.

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

Authors Shimazaki, Y; Wata, C; Hashimoto, T; Maruoka, K in WILEY-V C H VERLAG GMBH published article about HYPERVALENT IODINE REAGENTS; OXIDATIVE SPIROLACTONIZATION; SPIROCYCLIZATION; DIARYLAMINES; FLUORINATION; ANILINES; PHENOLS in [Shimazaki, Yuto; Maruoka, Keiji] Kyoto Univ, Grad Sch Sci, Dept Chem, Sakyo Ku, Kyoto 6068502, Japan; [Wata, Chisato; Hashimoto, Takuya] Chiba Univ, Chiba Iodine Resource Innovat Ctr, Inage Ku, 1-33 Yayoi, Chiba 2638522, Japan; [Wata, Chisato; Hashimoto, Takuya] Chiba Univ, Dept Chem, Grad Sch Sci, Inage Ku, 1-33 Yayoi, Chiba 2638522, Japan; [Maruoka, Keiji] Guangdong Univ Technol, Sch Chem Engn & Light Ind, Guangzhou 510006, Panyu District, Peoples R China; [Maruoka, Keiji] Kyoto Univ, Grad Sch Pharmaceut Sci, Sakyo Ku, Kyoto 6068501, Japan in 2021.0, Cited 89.0. HPLC of Formula: C8H11NO. The Name is 2-(4-Aminophenyl)ethanol. Through research, I have a further understanding and discovery of 104-10-9

We report herein the development of an enantioselective oxidative para-dearomatization of sulfonanilides with water by use of an indanol-based chiral organoiodine catalyst, originally developed in our group. This reaction proceeds efficiently by the use of N-mesyl-protected anilines as substrates, giving functionalized p-quinol imines in good yields and moderate to high enantioselectivities.

HPLC of Formula: C8H11NO. About 2-(4-Aminophenyl)ethanol, If you have any questions, you can contact Shimazaki, Y; Wata, C; Hashimoto, T; Maruoka, K or concate me.

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

In 2020 BIOORG MED CHEM LETT published article about SYSTEMIC ACQUIRED-RESISTANCE; ROTYLENCHULUS-RENIFORMIS; ELICITORS; NEMATICIDES; EFFICACY; TOMATO; PLANTS; SPP. in [Zhang, Ruifeng; Wang, Gaolei; Chen, Xiulei; Li, Zhong; Xu, Xiaoyong] East China Univ Sci & Technol, Shanghai Key Lab Chem Biol, Sch Pharm, Shanghai 200237, Peoples R China; [Guo, Wei] China Crop Protect Ind Assoc, Beijing 100723, Peoples R China in 2020, Cited 28. 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

Based on the characteristic of benzo[d][1,2,3]thiadiazole to induce the systemic acquired resistance and improve the immunity of plants, benzo[d][1,2,3]thiadiazole was introduced into 1,2,3-benzotriazin-4-one, thirty-one novel 1,2,3-benzotriazin-4-one derivatives containing benzo[d][1,2,3]thiadiazole were designed and synthesized. Nematicidal activity showed that most of the synthesized compounds exhibited great inhibitory activity in vivo against Meloidogyne incognita at 20 mg/L. Among 31 tested compounds, A2 and A3 showed an excellent nematicidal activity with the inhibition rate of 50.4% and 53.1% at the concentration of 1.0 mg/L, respectively. The influence of substituent type and position was investigated. The relationship between structure and activity was also preliminary analyzed.

Quality Control of 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 Zhang, RF; Guo, W; Wang, GL; Chen, XL; 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

Recently I am researching about CATALYZED DENITROGENATIVE ANNULATION; TERT-BUTYL NITRITE; NEMATOCIDAL ACTIVITIES; SELECTIVE SYNTHESIS; DERIVATIVES; 1,2,3-BENZOTRIAZINE-4-(3H)-ONES; ACID, Saw an article supported by the Council of Scientific and Industrial Research, New DelhiCouncil of Scientific & Industrial Research (CSIR) – India [BSC-0114]. Published in PERGAMON-ELSEVIER SCIENCE LTD in OXFORD ,Authors: Barak, DS; Mukhopadhyay, S; Dahatonde, DJ; Batra, S. 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. Recommanded Product: Benzo[d][1,2,3]triazin-4(3H)-one

An efficient transformation of 2-aminobenzamides to 1,2,3-benzotriazin-4(3H)-ones in the presence of sodium nitrite (NaNO2) and Iodine (I-2) is described. The reaction is proposed to proceed via formation of nitrosyl halide that induces nitrosylation of the amino group of 2-aminobenzamide leading to diazotization followed by intramolecular cyclization. (C) 2018 Elsevier Ltd. All rights reserved.

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 Barak, DS; Mukhopadhyay, S; Dahatonde, DJ; Batra, S 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