Month: October 2021

Zhang, XM; Peng, AH; Xie, WD; Wang, M; Zheng, D; Feng, MK 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 published Hexokinase II Inhibitory Effect of Secondary Metabolites Derived from a Streptomyces sp. Associated with Mud Dauber Wasp in 2020, Cited 43. 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.

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.

Formula: C7H5N3O. 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

I found the field of Biochemistry & Molecular Biology; Chemistry very interesting. Saw the article C-N Coupling of DNA-Conjugated (Hetero)aryl Bromides and Chlorides for DNA-Encoded Chemical Library Synthesis published in 2020. Product Details of 104-10-9, Reprint Addresses Chen, YC; Simmons, N (corresponding author), Baylor Coll Med, Ctr Drug Discovery, Dept Pathol & Immunol, Houston, TX 77030 USA.. The CAS is 104-10-9. Through research, I have a further understanding and discovery of 2-(4-Aminophenyl)ethanol

DNA-encoded chemical library (DECL) screens are a rapid and economical tool to identify chemical starting points for drug discovery. As a robust transformation for drug discovery, palladium-catalyzed C-N coupling is a valuable synthetic method for the construction of DECL chemical matter; however, currently disclosed methods have only been demonstrated on DNA-attached (hetero)aromatic iodide and bromide electrophiles. We developed conditions utilizing an N-heterocyclic carbene-palladium catalyst that extends this reaction to the coupling of DNA-conjugated (hetero)aromatic chlorides with (hetero)aromatic and select aliphatic amine nucleophiles. In addition, we evaluated steric and electronic effects within this catalyst series, carried out a large substrate scope study on two representative (hetero)aryl bromides, and applied this newly developed method within the construction of a 63 million-membered DECL.

Product Details of 104-10-9. About 2-(4-Aminophenyl)ethanol, If you have any questions, you can contact Chen, YC; Faver, JC; Ku, AF; Miklossy, G; Riehle, K; Bohren, KM; Ucisik, MN; Matzuk, MM; Yu, ZF; Simmons, N or concate me.

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

Recently I am researching about NUCLEOTIDE-BINDING-SITES; MULTIDRUG-RESISTANCE; AUTOMATED DOCKING; DRUG-RESISTANCE; FLEXIBLE LIGANDS; TRANSPORT; OPTIMIZATION; PURIFICATION; MTT; CHEMORESISTANCE, Saw an article supported by the National Institute of General Medical Sciences (NIH/NIGMS)United States Department of Health & Human ServicesNational Institutes of Health (NIH) – USANIH National Institute of General Medical Sciences (NIGMS) [R15 GM094771-02]. Published in AMER CHEMICAL SOC in WASHINGTON ,Authors: Wise, JG; Nanayakkara, AK; Aljowni, M; Chen, G; De Oliveira, MC; Ammerman, L; Olengue, K; Lippert, AR; Vogel, PD. The CAS is 91-00-9. Through research, I have a further understanding and discovery of Diphenylmethanamine. Application In Synthesis of Diphenylmethanamine

Overexpression of ABC transporters like P-glycoprotein (P-gp) has been correlated with resistances in cancer chemotherapy. Intensive efforts to identify P-gp inhibitors for use in combination therapy have not led to clinically approved inhibitors to date. Here, we describe computational approaches combined with structure-based design to improve the characteristics of a P-gp inhibitor previously identified by us. This hit compound represents a novel class of P-gp inhibitors that specifically targets and inhibits P-gp ATP hydrolysis while not being transported by the pump. We describe here a new program for virtual chemical synthesis and computational assessment, ChemGen, to produce hit compound variants with improved binding characteristics. The chemical syntheses of several variants, efficacy in reversing multidrug resistance in cell culture, and biochemical assessment of the inhibition mechanism are described. The usefulness of the computational predictions of binding characteristics of the inhibitor variants is discussed and compared to more traditional structure-based approaches.

About Diphenylmethanamine, If you have any questions, you can contact Wise, JG; Nanayakkara, AK; Aljowni, M; Chen, G; De Oliveira, MC; Ammerman, L; Olengue, K; Lippert, AR; Vogel, PD or concate me.. Application In Synthesis of Diphenylmethanamine

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

COA of Formula: C13H13N. Recently I am researching about SIMILARITY/DIVERSITY ANALYSIS; MOLECULAR DESCRIPTORS; GETAWAY DESCRIPTORS; PREDICTION; DOCKING; INDEXES; ASSAY; RICE, Saw an article supported by the Tarbiat Modares University. Published in SPRINGER in NEW YORK ,Authors: Gholivand, K; Abbod, M; Valmoozi, AAE; Barzegar, O; Tabar, HN; Yaghoubi, R; Hosseini, M; Safaie, N; Dashtaki, MR; Dusek, M; Mani-Varnosfaderani, A. The CAS is 91-00-9. Through research, I have a further understanding and discovery of Diphenylmethanamine

A series of phosphonic acid and bisphosphoramidate derivatives were synthesized and characterized. The bioactivities against the fungal pathogen Macrophomina phaseolina and human acetylcholinesterase AChE enzyme were studied using QSAR based on multiple linear regression. L17, with (p-Cl-C6H4-NH) (p-Cl-C6H4)C(H)P(O)(OC2H5)(2) skeleton, demonstrated a great mortality on the M. phaseolina mycelial growth by 83% inhibition at 150 mg/L; the other tested derivative showed moderate to weak antifungal activity against the fungus. QSAR model based on the GA-MLR method revealed the importance of 3D descriptors (De, Mor18e, H8m, and Mor30p) on the antifungal activity. It showed good capability in predicting the fungicidal activity of the studied molecules. Another derivative, L5, with (m-CH3-NC5H4-NH)(m-CH3-C6H4)C(H)P(O)(OCH3)(2) skeleton displays the most potent anti-AChE activity. The electronic parameters, Delta EL-H, and E-LUMO, have the highest contribution of human AChE. The authors suggest that these models could be usefully employed in designing more effective crop protection compounds without side effects on non-target organisms.

About Diphenylmethanamine, If you have any questions, you can contact Gholivand, K; Abbod, M; Valmoozi, AAE; Barzegar, O; Tabar, HN; Yaghoubi, R; Hosseini, M; Safaie, N; Dashtaki, MR; Dusek, M; Mani-Varnosfaderani, A or concate me.. COA of Formula: C13H13N

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

Recently I am researching about NECROSIS-FACTOR-ALPHA; PHARMACOLOGICAL EVALUATION; HYBRID COMPOUNDS; PLATELETS; DESIGN; ASSAY, Saw an article supported by the Fundacao de Amparo a Pesquisa do Estado de Sao Paulo (FAPESP)Fundacao de Amparo a Pesquisa do Estado de Sao Paulo (FAPESP) [2013/23461-3, 2015/19531-1]; Conselho Nacional de Desenvolvimento Cientifico e Tecnologico (CNPq)Conselho Nacional de Desenvolvimento Cientifico e Tecnologico (CNPQ) [135821/2011-8]. Published in SPRINGER BIRKHAUSER in NEW YORK ,Authors: Chelucci, RC; de Oliveira, IJ; Barbieri, KP; Lopes-Pires, ME; Polesi, MC; Chiba, DE; Carlos, IZ; Marcondes, S; Dos Santos, JL; Chung, MC. The CAS is 104-10-9. Through research, I have a further understanding and discovery of 2-(4-Aminophenyl)ethanol. Recommanded Product: 2-(4-Aminophenyl)ethanol

Sickle Cell Anemia (SCA) is one of the most prevalent hereditary hematological diseases worldwide. The disease is characterized by chronic inflammation, hypercoagulable state, and pro-thrombotic profile, which lead the vaso-occlusive process. In this work, we described the antiplatelet activity and the ability to reduce tumor necrosis factor-alpha (TNF-) levels of phthalimide derivatives. All compounds inhibited platelet aggregation induced by collagen and adenosine diphosphate, at levels ranging from 26.0 to 74.2% and 30.7 to 79.6%, respectively. The compounds exhibited reduced bleeding time compared to acetylsalicylic acid (ASA). Moreover, compounds 4c and 10c inhibited TNF- levels at 73.5% and 65.0%, respectively. These findings suggest that phthalimide derivatives 4c and 10c are promising lead compounds useful to prevent vaso-occlusion and inflammation associated with the sickle cell anemia. [GRAPHICS] .

Recommanded Product: 2-(4-Aminophenyl)ethanol. About 2-(4-Aminophenyl)ethanol, If you have any questions, you can contact Chelucci, RC; de Oliveira, IJ; Barbieri, KP; Lopes-Pires, ME; Polesi, MC; Chiba, DE; Carlos, IZ; Marcondes, S; Dos Santos, JL; Chung, MC or concate me.

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

Name: Diphenylmethanamine. I found the field of Chemistry very interesting. Saw the article Diboronic Acid Anhydrides as Effective Catalysts for the Hydroxy-Directed Dehydrative Amidation of Carboxylic Acids published in 2019.0, Reprint Addresses Shimada, N (corresponding author), Kitasato Univ, Dept Pharmaceut Sci, Lab Organ Chem Drug Dev, Tokyo 1088641, Japan.. The CAS is 91-00-9. Through research, I have a further understanding and discovery of Diphenylmethanamine.

The direct catalytic dehydrative amidation of beta-hydroxycarboxylic acids with amines is described. A biphenyl-based diboronic acid anhydride with a B-O-B skeleton is shown to be an exceptionally effective catalyst for the reaction, providing beta-hydroxycarboxylic amides in high to excellent yields with a low catalyst loading (minimum of 0.01 mol %, TON up to 7,500). This hydroxy-directed amidation shows excellent chemoselectivity and is applicable to gram-scale drug synthesis.

About Diphenylmethanamine, If you have any questions, you can contact Shimada, N; Hirata, M; Koshizuka, M; Ohse, N; Kaito, R; Makino, K or concate me.. Name: Diphenylmethanamine

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

An article Chiral Phosphoric Acid Catalyzed Enantioselective Synthesis of alpha-Tertiary Amino Ketones from Sulfonium Ylides WOS:000563079000043 published article about N-H BONDS; BRONSTED ACID; METAL CATALYSIS; AMINATION; INSERTION; DERIVATIVES; COMPLEXES; CARBENE; MODE in [Luo, Yuzheng; Li, Pingfan] Beijing Univ Chem Technol, Coll Chem, Dept Organ Chem, State Key Lab Chem Resource Engn, Beijing 100029, Peoples R China; [Guo, Wengang; Sung, Herman H-Y; Williams, Ian D.; Sun, Jianwei] Hong Kong Univ Sci & Technol, Dept Chem, Kowloon, Hong Kong, Peoples R China in 2020.0, Cited 50.0. Name: Diphenylmethanamine. The Name is Diphenylmethanamine. Through research, I have a further understanding and discovery of 91-00-9

Herein we disclose a new catalytic asymmetric approach for the synthesis of chiral alpha-amino ketones, which is particularly useful for the less accessible acyclic alpha-tertiary cases. By a protonation-amination sequence, our approach represents a rare asymmetric H-heteroatom bond insertion by alpha-carbonyl sulfonium ylides, an attractive surrogate of diazocarbonyls. The mild intermolecular C-N bond formation was catalyzed by chiral phosphoric acids with excellent efficiency and enantioselectivity. The products are precursors to other important chiral amine derivatives, including drug molecules and chiral ligands. The enantioselectivity was controlled by dynamic kinetic resolution in the amination step, rather than the initial protonation. This process opens up a new platform for the development of other related insertion reactions.

Name: Diphenylmethanamine. About Diphenylmethanamine, If you have any questions, you can contact Guo, WG; Luo, YZ; Sung, HHY; Williams, ID; Li, PF; Sun, JW or concate me.

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

An article Visible-light-induced denitrogenative phosphorylation of benzotriazinones: a metal- and additive-free method for accessing ortho-phosphorylated benzamide derivatives WOS:000608623000013 published article about ALKYNE INSERTION; LIGANDS; ACIDS; ANNULATION; 1,2,3-BENZOTRIAZIN-4(3H)-ONES in [Tang, Guo] Xiamen Univ, Dept Chem, Coll Chem & Chem Engn, Xiamen 361005, Fujian, Peoples R China; Xiamen Univ, Key Lab Chem Biol Fujian Prov, Xiamen 361005, Fujian, Peoples R China in 2021, Cited 54. Quality Control of 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

Metal-free, visible-light-induced denitrogenative phosphorylation of 1,2,3-benzotriazinones was achieved. With the use of eosin Y as a photoredox catalyst, N,N-diisopropylethylamine as a base, CH3CN-H2O as a solvent and sunlight or a blue LED as a light source, a variety of aryl-phosphonates, aryl-phosphinates, and aryl-phosphine oxides were efficiently prepared. In addition, B(2)pin(2) instead of P-nucleophiles as a radical acceptor was also demonstrated. The key advantages of this newly developed method are the clean reaction profile, use of a low-cost organic-dye catalyst, energy efficiency, broad substrate scope, good to excellent yields and large-scale synthetic applicability. The gram-scale synthesised compounds could be isolated in pure form just upon extraction, followed by re-crystallisation; no tedious chromatographic purification was required.

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 Chen, FS; Hu, SS; Li, SP; Tang, G; Zhao, YF 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

An article Pd-catalyzed stereoselective tandem ring-opening amination/cyclization of vinyl gamma-lactones: access to caprolactam diversity WOS:000562597500014 published article about ENANTIOSELECTIVE SYNTHESIS; HIGHLY EFFICIENT; LACTAM SYNTHESIS; AMIDES; ACIDS; POLYMERIZATION; HYDROGENATION; HETEROCYCLES; SUBSTITUTION; CAPURAMYCIN in [Xie, Jianing; Li, Xuetong; Kleij, Arjan W.] Barcelona Inst Sci & Technol, Inst Chem Res Catalonia ICIQ, Av Paisos Catalans 16, Tarragona 43007, Spain; [Kleij, Arjan W.] Catalan Inst Res & Adv Studies ICREA, Pg Lluis Co 23, Barcelona 08010, Spain in 2020.0, Cited 68.0. The Name is 2-(4-Aminophenyl)ethanol. Through research, I have a further understanding and discovery of 104-10-9. COA of Formula: C8H11NO

A stereoselective amination/cyclization cascade process has been developed that allows for the preparation of a series of unsaturated and substituted caprolactam derivatives in good yields. This conceptually novel protocol takes advantage of the easy access and modular character of vinyl gamma-lactones that can be prepared from simple precursors. Activation of the lactone substrate in the presence of a suitable Pd precursor and newly developed phosphoramidite ligand offers a stereocontrolled ring-opening/allylic amination manifold under ambient conditions. The intermediate (E)-configured epsilon-amino acid can be cyclized using a suitable dehydrating agent in an efficient one-pot, two-step sequence. This overall highly chemo-, stereo- and regio-selective transformation streamlines the production of a wide variety of modifiable and valuable caprolactam building blocks in an operationally attractive way.

About 2-(4-Aminophenyl)ethanol, If you have any questions, you can contact Xie, JN; Li, XT; Kleij, AW or concate me.. COA of Formula: C8H11NO

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

I found the field of Science & Technology – Other Topics very interesting. Saw the article Modular click chemistry libraries for functional screens using a diazotizing reagent published in 2019. Product Details of 91-00-9, Reprint Addresses Sharpless, KB; Dong, JJ (corresponding author), Univ Chinese Acad Sci, Ctr Excellence Mol Synth, Shanghai Inst Organ Chem, Key Lab Organofluorine Chem,Chinese Acad Sci, Shanghai, Peoples R China.. The CAS is 91-00-9. Through research, I have a further understanding and discovery of Diphenylmethanamine

Click chemistry is a concept in which modular synthesis is used to rapidly find new molecules with desirable properties(1). Copper(I)-catalysed azide-alkyne cycloaddition (CuAAC) triazole annulation and sulfur(VI) fluoride exchange (SuFEx) catalysis are widely regarded as click reactions(2-4), providing rapid access to their products in yields approaching 100% while being largely orthogonal to other reactions. However, in the case of CuAAC reactions, the availability of azide reagents is limited owing to their potential toxicity and the risk of explosion involved in their preparation. Here we report another reaction to add to the click reaction family: the formation of azides from primary amines, one of the most abundant functional groups(5). The reaction uses just one equivalent of a simple diazotizing species, fluorosulfuryl azide(6-11) (FSO2N3), and enables the preparation of over 1,200 azides on 96-well plates in a safe and practical manner. This reliable transformation is a powerful tool for the CuAAC triazole annulation, the most widely used click reaction at present. This method greatly expands the number of accessible azides and 1,2,3-triazoles and, given the ubiquity of the CuAAC reaction, it should find application in organic synthesis, medicinal chemistry, chemical biology and materials science.

Product Details of 91-00-9. About Diphenylmethanamine, If you have any questions, you can contact Meng, GY; Guo, TJ; Ma, TC; Zhang, J; Shen, YC; Sharpless, KB; Dong, JJ or concate me.

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