Tag: M.W=150-200

Application In Synthesis of Diphenylmethanamine. Wei, MJ; Liang, DC; Cao, XH; Luo, WJ; Ma, GJ; Liu, ZY; Li, L in [Wei, Mingjie; Liang, Dacheng; Luo, Wenjun; Ma, Guojian; Liu, Zeyuan; Li, Le] Sun Yat Sen Univ, Sch Chem, PCFM Lab, Guangzhou 510275, Peoples R China; [Wei, Mingjie; Liang, Dacheng; Luo, Wenjun; Ma, Guojian; Liu, Zeyuan; Li, Le] Sun Yat Sen Univ, Sch Chem, GDHPRC Lab, Guangzhou 510275, Peoples R China; [Cao, Xiaohui] Guangdong Pharmaceut Univ, Sch Pharm, Guangzhou 510006, Peoples R China published A Broad-Spectrum Catalytic Amidation of Sulfonyl Fluorides and Fluorosulfates** in 2021, Cited 144. The Name is Diphenylmethanamine. Through research, I have a further understanding and discovery of 91-00-9.

A broad-spectrum, catalytic method has been developed for the synthesis of sulfonamides and sulfamates. With the activation by the combination of a catalytic amount of 1-hydroxybenzotriazole (HOBt) and silicon additives, amidations of sulfonyl fluorides and fluorosulfates proceeded smoothly and excellent yields were generally obtained (87-99 %). Noticeably, this protocol is particularly efficient for sterically hindered substrates. Catalyst loading is generally low and only 0.02 mol % of catalyst is required for the multidecagram-scale synthesis of an amantadine derivative. In addition, the potential of this method in medicinal chemistry has been demonstrated by the synthesis of the marketed drug Fedratinib via a key intermediate sulfonyl fluoride 13. Since a large number of amines are commercially available, this route provides a facile entry to access Fedratinib analogues for biological screening.

Application In Synthesis of Diphenylmethanamine. Welcome to talk about 91-00-9, If you have any questions, you can contact Wei, MJ; Liang, DC; Cao, XH; Luo, WJ; Ma, GJ; Liu, ZY; Li, L or send Email.

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Amide – Wikipedia,
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Micewicz, ED; Nguyen, C; Micewicz, A; Waring, AJ; McBrid, WH; Ruchala, P in [Micewicz, Ewa D.; Nguyen, Christine; McBrid, William H.] Univ Calif Los Angeles, Dept Radiat Oncol, 10833 Le Conte Ave, Los Angeles, CA 90095 USA; [Micewicz, Alina] Univ Calif Los Angeles, David Geffen Sch Med, Volunteering Program, 10833 Le Conte Ave, Los Angeles, CA 90095 USA; [Waring, Alan J.] Harbor UCLA Med Ctr, Dept Med, Los Angeles Biomed Res Inst, 1000 West Carson St, Torrance, CA 90502 USA; [Ruchala, Piotr] Univ Calif Los Angeles, Dept Psychiat & Biobehav Sci, 760 Westwood Plaza, Los Angeles, CA 90024 USA; [Ruchala, Piotr] Jane & Terry Semel Inst Neurosci & Human Behav, Pasarow Mass Spectrometry Lab, 760 Westwood Plaza, Los Angeles, CA 90024 USA published Position of lipidation influences anticancer activity of Smac analogs in 2019.0, Cited 79.0. Formula: C13H13N. The Name is Diphenylmethanamine. Through research, I have a further understanding and discovery of 91-00-9.

A small group of lipid-conjugated Smac mimetics was synthesized to probe the influence of the position of lipidation on overall anti-cancer activity. Specifically, new compounds were modified with lipid(s) in position 3 and C-terminus. Previously described position 2 lipidated analog M11 was also synthesized. The resulting mini library of Smacs lipidated in positions 2, 3 and C-terminus was screened extensively in vitro against a total number of 50 diverse cancer cell lines revealing that both the position of lipidation as well as the type of lipid, influence their anti-cancer activity and cancer type specificity. Moreover, when used in combination therapy with inhibitor of menin-MLL1 protein interactions, position 2 modified analog SM2 showed strong synergistic anti-cancer properties. The most promising lipid-conjugated analogs SM2 and SM6, showed favorable pharmacokinetics and in vivo activity while administered subcutaneously in the preclinical mouse model. Collectively, our findings suggest that lipid modification of Smacs may be a viable approach in the development of anti-cancer therapeutic leads.

Formula: C13H13N. Welcome to talk about 91-00-9, If you have any questions, you can contact Micewicz, ED; Nguyen, C; Micewicz, A; Waring, AJ; McBrid, WH; Ruchala, P or send Email.

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Category: amides-buliding-blocks. Authors Sun, WN; Chen, XL; Huang, SZ; Li, WP; Tian, CY; Yang, SY; Li, LL in PERGAMON-ELSEVIER SCIENCE LTD published article about in [Sun, Weining; Tian, Chenyu; Li, Linli] Sichuan Univ, West China Sch Pharm, Key Lab Drug Targeting & Drug Delivery Syst, Minist Educ, Chengdu 610041, Sichuan, Peoples R China; [Chen, Xiuli; Huang, Shenzhen; Li, Wenpei; Yang, Shengyong] Sichuan Univ, West China Hosp, State Key Lab Biotherapy, Chengdu 610041, Sichuan, Peoples R China; [Chen, Xiuli; Huang, Shenzhen; Li, Wenpei; Yang, Shengyong] Sichuan Univ, West China Hosp, Canc Ctr, Chengdu 610041, Sichuan, Peoples R China in 2020, Cited 14. The Name is Diphenylmethanamine. Through research, I have a further understanding and discovery of 91-00-9

SIRT6 is a deacetylase of histone H3 and inhibitors of SIRT6 have been thought as potential agents for treatment of diabetes. Herein we report the discovery of a series of new SIRT6 inhibitors containing the skeleton 1-phenylpiperazine. Among them, compound 5-(4-methylpiperazin-1-yl)-2-nitroaniline (6d) is the most potent one, which showed an IC50 value of 4.93 mu M against SIRT6 in the Fluor de Lys (FDL) assay. It displayed K-D values of 9.76 mu M and 10 mu M in surface plasmon resonance (SPR) and isothermal titration calorimetry (ITC) assays, respectively. In selectivity assay, 6d showed no activity against other members of the HDAC family (SIRT1-3 and HDAC1-11) at concentrations up to 200 mu M. In a mouse model of type 2 diabetes, 6d could significantly increase the level of glucose transporter GLUT-1, thereby reducing blood glucose. Overall, this study provides a promising lead compound for subsequent drug discovery targeting SIRT6.

Category: amides-buliding-blocks. Welcome to talk about 91-00-9, If you have any questions, you can contact Sun, WN; Chen, XL; Huang, SZ; Li, WP; Tian, CY; Yang, SY; Li, LL or send Email.

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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. HPLC 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.

HPLC of Formula: C13H13N. Bye, fridends, I hope you can learn more about C13H13N, If you have any questions, you can browse other blog as well. See you lster.

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Amide – Wikipedia,
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SDS of cas: 91-00-9. In 2020.0 CHEMMEDCHEM published article about NITRIC-OXIDE SYNTHASE; SELECTIVE-INHIBITION; DERIVATIVES; AGENT; IDENTIFICATION; ACETAMIDINES; AMIDOXIME; COMPONENT; THERAPY; AMIDINE in [Maccallini, Cristina; Marinelli, Lisa; Cacciatore, Ivana; Fantacuzzi, Marialuigia; Di Stefano, Antonio; Amoroso, Rosa] Univ G dAnnunzio, Dept Pharm, Via Vestini 31, I-66100 Chieti, Italy; [Indorf, Patrick; Clement, Bernd] Univ Kiel, Inst Pharmaceut, Gutenbergstr 76, D-24118 Kiel, Germany in 2020.0, Cited 48.0. The Name is Diphenylmethanamine. Through research, I have a further understanding and discovery of 91-00-9.

Under different pathological conditions, aberrant induction of neuronal nitric oxide synthase (nNOS) generates overproduction of NO that can cause irreversible cell damage. The aim of this study was to develop an amidoxime prodrug of a potent nNOS inhibitor, the benzhydryl acetamidine. We synthesized the benzhydryl acetamidoxime, which was evaluatedin vitroto ascertain the potential NOS inhibitory activity, as well as conducting bioconversion into the parent acetamidine. The prodrug was also profiled forin vitrophysicochemical properties, by determining the lipophilicity, passive permeation through the human gastrointestinal tract and across the blood-brain barrier by PAMPA, and chemical, enzymatic, and plasma stability. The obtained data demonstrate that the amidoxime prodrug shows an improved pharmacokinetic profile with respect to the acetamidine nNOS inhibitor, thus suggesting that it could be a promising lead compound to treat all those pathological conditions in which nNOS activity is dysregulated.

Welcome to talk about 91-00-9, If you have any questions, you can contact Maccallini, C; Marinelli, L; Indorf, P; Cacciatore, I; Fantacuzzi, M; Clement, B; Di Stefano, A; Amoroso, R or send Email.. SDS of cas: 91-00-9

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

Authors Shelp, RA; Ciro, A; Pu, YG; Merchant, RR; Hughes, JME; Walsh, PJ in ROYAL SOC CHEMISTRY published article about in [Shelp, Russell A.; Ciro, Anthony; Pu, Youge; Walsh, Patrick J.] Univ Penn, Dept Chem, Roy & Diana Vagelos Labs, 231 South 34th St, Philadelphia, PA 19104 USA; [Merchant, Rohan R.] Merck & Co Inc, Dept Discovery Chem, San Francisco, CA 94080 USA; [Hughes, Jonathan M. E.] Merck & Co Inc, Dept Proc Res & Dev, Rahway, NJ 07065 USA in 2021, Cited 41. Formula: C13H13N. The Name is Diphenylmethanamine. Through research, I have a further understanding and discovery of 91-00-9

We report a 3-component reaction between N-benzyl ketimines, [1.1.1]propellane, and pinacol boronates to generate benzylamine bicyclo[1.1.1]pentane (BCP) pinacol boronates. These structures are analogous to highly sought diarylmethanamine cores, which are common motifs in bioactive molecules. We demonstrate the versatility of the boronate ester handle via downstream functionalization through a variety of reactions, including a challenging Pd-catalyzed (hetero)arylation that exhibits a broad substrate scope. Together, these methods enable the synthesis of high-value BCP benzylamines which are inaccessible by existing methods. Furthermore, we demonstrate the successful application of these newly developed (hetero)arylation conditions to a variety of challenging tertiary pinacol boronates, including nitrogen-containing heterocycles, 1,1-disubstituted cyclopropanes, and other BCP cores.

Formula: C13H13N. Welcome to talk about 91-00-9, If you have any questions, you can contact Shelp, RA; Ciro, A; Pu, YG; Merchant, RR; Hughes, JME; Walsh, PJ or send Email.

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

Raimbault, A; Ma, CMA; Ferri, M; Baurer, S; Bonnet, P; Bourg, S; Lammerhofer, M; West, C in [Raimbault, Adrien; Cam Mai Anh Ma; Bonnet, Pascal; Bourg, Stephane; West, Caroline] Univ Orleans, Inst Organ & Analyt Chem, CNRS UMR 7311, Rue Chartres BP 6759, F-45067 Orleans, France; [Ferri, Martina; Baeurer, Stefanie; Laemmerhofer, Michael] Univ Tubingen, Inst Pharmaceut Sci, Pharmaceut Bio Anal, Morgenstelle 8, D-72076 Tubingen, Germany; [Ferri, Martina] Univ Perugia, Dept Pharmaceut Sci, Via Liceo 1, I-06123 Perugia, Italy published Cinchona-based zwitterionic stationary phases: Exploring retention and enantioseparation mechanisms in supercritical fluid chromatography with a fragmentation approach in 2020, Cited 43. Product Details of 91-00-9. The Name is Diphenylmethanamine. Through research, I have a further understanding and discovery of 91-00-9.

Chiralpak ZWIX(+) and ZWIX(-), are brush-type bonded-silica chiral stationary phases (CSPs), based on complex diastereomeric Cinchona alkaloids derivatives bearing both a positive and a negative charge. In the present study, we aimed to improve the understanding of retention and enantioseparation mechanisms of these CSPs employed in supercritical fluid chromatography (SFC). For this purpose, 9 other stationary phases were used as comparison systems: two of them are commercially available and bear only a positive charge (Chiralpak QN-AX and QD-AX) and the 7 others were designed purposely to be structurally similar to the parent ZWIX phases, but miss some portion of the complex ligand. First, cluster analysis was employed to identify similar and dissimilar behavior among the 11 stationary phases, where ionic interactions appeared to dominate the observed differences. Secondly, the stationary phases were characterized with linear solvation energy relationships (LSER) based on the SFC analysis of 161 achiral analytes and a modified version of the solvation parameter model to include ionic interactions. This served to compare the interaction capabilities for the 11 stationary phases and showed in particular the contribution of attractive and repulsive ionic interactions. Then the ZWIX phases were characterized for their enantioseparation capabilities with a set of 58 racemic probes. Discriminant analysis was applied to explore the molecular structural features that are useful to successful enantioseparation on the ZWIX phases. In particular, it appeared that the presence of positive charges in the analyte is causing increased retention but is not necessarily a favorable feature to enantiorecognition. On the opposite, the presence of negative charges in the analyte favors early elution and enantiorecognition. Finally, a smaller set of 30 pairs of enantiomers, selected by their structural diversity and different enantioseparation values on the ZWIX phases, were analyzed on all chiral phases to observe the contribution of each structural fragment of the chiral ligand on enantioselectivity. Molecular modelling of the ligands also helped in understanding the three-dimensional arrangement of each ligand, notably the intra-molecular hydrogen bonding or the possible contribution of ionic interactions. In the end, each structural element in the ZWIX phases appeared to be a significant contributor to successful enantioresolution, whether they contribute as direct interaction groups (ion-exchange functions) or as steric constraints to orientate the interacting groups towards the analytes. (C) 2019 Elsevier B.V. All rights reserved.

Product Details of 91-00-9. Bye, fridends, I hope you can learn more about C13H13N, If you have any questions, you can browse other blog as well. See you lster.

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Amide – Wikipedia,
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An article Environmentally benign decarboxylative N-, O-, and S-acetylations and acylations WOS:000598242900016 published article about EFFICIENT RECYCLABLE CATALYST; DBN TETRAPHENYLBORATE SALTS; DIRECT AMIDATION; CARBOXYLIC-ACIDS; HIGHLY EFFICIENT; SILICA-GEL; ALCOHOLS; AMINES; PHENOLS; SOLVENT in [Ghosh, Santanu; Purkait, Anisha; Jana, Chandan K.] Indian Inst Technol Guwahati, Dept Chem, Gauhati 781039, India in 2020.0, Cited 76.0. Application In Synthesis of Diphenylmethanamine. The Name is Diphenylmethanamine. Through research, I have a further understanding and discovery of 91-00-9

An operationally simple and general method for acetylation and acylation of a wide variety of substrates (amines, alcohols, phenols, thiols, and hydrazones) has been reported. Meldrum’s acid and its derivatives have been used as an air-stable, non-volatile, cost-effective, and easy to handle acetylating/acylating agent. Easily separable byproducts (CO2 and acetone) allowed the isolation of analytically pure acetylated products without the requirement of work-up and any chromatography.

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

An article A novel approach for the synthesis of functionalized hydroxylamino derivative of dihydroquinazolinones WOS:000538897200001 published article about EFFICIENT SYNTHESIS; 2,3-DIHYDROQUINAZOLIN-4(1H)-ONES; INHIBITORS; CHEMISTRY; SYNTHASE in [Jaganmohan, Chikkanti; Kumar, Vinay K. P.; Venkateshwarlu, R.; Mohanty, Sandeep; Kumar, Jaydeep; Raghunadh, Akula] Dr Reddys Labs Ltd, Hyderabad 500049, India; [Jaganmohan, Chikkanti; Rao, Venkateswara B.] Andhra Univ, Dept Organ Chem & FDW, Visakhapatnam, Andhra Pradesh, India; [Tadiparthi, Krishnaji] CHRIST Deemed Be Univ, Dept Chem, Hosur Rd, Bangalore 560029, Karnataka, India in 2020.0, Cited 41.0. The Name is Diphenylmethanamine. Through research, I have a further understanding and discovery of 91-00-9. Category: amides-buliding-blocks

A new metal-free and modular approach for the synthesis of various functionalized dihydroquinazolinones has been developed from isatoic anhydride, amines, 4-chloro-N-hydroxybenzimidoylchloride to yield up to 71%. The reaction has been screened in various bases, solvents at different temperatures. The substrate scope of the reaction has been studied with various amines and the possible reaction mechanism for this reaction has also been proposed.

Welcome to talk about 91-00-9, If you have any questions, you can contact Jaganmohan, C; Kumar, KPV; Venkateshwarlu, R; Mohanty, S; Kumar, J; Rao, BV; Raghunadh, A; Tadiparthi, K or send Email.. Category: amides-buliding-blocks

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Amide – Wikipedia,
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Recommanded Product: 91-00-9. In 2020 J CHROMATOGR A published article about CHIRAL RECOGNITION MECHANISM; BETA-AMINO ACIDS; LIQUID-CHROMATOGRAPHY; CAPILLARY ELECTROCHROMATOGRAPHY; PERFORMANCE; SEPARATIONS; INSIGHTS; POLYSACCHARIDE; ENANTIOMER; QUININE in [Raimbault, Adrien; Cam Mai Anh Ma; Bonnet, Pascal; Bourg, Stephane; West, Caroline] Univ Orleans, Inst Organ & Analyt Chem, CNRS UMR 7311, Rue Chartres BP 6759, F-45067 Orleans, France; [Ferri, Martina; Baeurer, Stefanie; Laemmerhofer, Michael] Univ Tubingen, Inst Pharmaceut Sci, Pharmaceut Bio Anal, Morgenstelle 8, D-72076 Tubingen, Germany; [Ferri, Martina] Univ Perugia, Dept Pharmaceut Sci, Via Liceo 1, I-06123 Perugia, Italy in 2020, Cited 43. The Name is Diphenylmethanamine. Through research, I have a further understanding and discovery of 91-00-9.

Chiralpak ZWIX(+) and ZWIX(-), are brush-type bonded-silica chiral stationary phases (CSPs), based on complex diastereomeric Cinchona alkaloids derivatives bearing both a positive and a negative charge. In the present study, we aimed to improve the understanding of retention and enantioseparation mechanisms of these CSPs employed in supercritical fluid chromatography (SFC). For this purpose, 9 other stationary phases were used as comparison systems: two of them are commercially available and bear only a positive charge (Chiralpak QN-AX and QD-AX) and the 7 others were designed purposely to be structurally similar to the parent ZWIX phases, but miss some portion of the complex ligand. First, cluster analysis was employed to identify similar and dissimilar behavior among the 11 stationary phases, where ionic interactions appeared to dominate the observed differences. Secondly, the stationary phases were characterized with linear solvation energy relationships (LSER) based on the SFC analysis of 161 achiral analytes and a modified version of the solvation parameter model to include ionic interactions. This served to compare the interaction capabilities for the 11 stationary phases and showed in particular the contribution of attractive and repulsive ionic interactions. Then the ZWIX phases were characterized for their enantioseparation capabilities with a set of 58 racemic probes. Discriminant analysis was applied to explore the molecular structural features that are useful to successful enantioseparation on the ZWIX phases. In particular, it appeared that the presence of positive charges in the analyte is causing increased retention but is not necessarily a favorable feature to enantiorecognition. On the opposite, the presence of negative charges in the analyte favors early elution and enantiorecognition. Finally, a smaller set of 30 pairs of enantiomers, selected by their structural diversity and different enantioseparation values on the ZWIX phases, were analyzed on all chiral phases to observe the contribution of each structural fragment of the chiral ligand on enantioselectivity. Molecular modelling of the ligands also helped in understanding the three-dimensional arrangement of each ligand, notably the intra-molecular hydrogen bonding or the possible contribution of ionic interactions. In the end, each structural element in the ZWIX phases appeared to be a significant contributor to successful enantioresolution, whether they contribute as direct interaction groups (ion-exchange functions) or as steric constraints to orientate the interacting groups towards the analytes. (C) 2019 Elsevier B.V. All rights reserved.

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