Category: amides-buliding-blocks

In 2019 BIOORG CHEM 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. 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. Safety of Benzo[d][1,2,3]triazin-4(3H)-one

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.

Safety of Benzo[d][1,2,3]triazin-4(3H)-one. Welcome to talk about 90-16-4, 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 send Email.

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

Formula: C13H13N. Chen, X; Yang, X; Mao, F; Wei, JL; Xu, YX; Li, BL; Zhu, J; Ni, SS; Jia, LJ; Li, J 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 published Development of novel benzimidazole-derived neddylation inhibitors for suppressing tumor growth in vitro and in vivo in 2021.0, Cited 41.0. 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.

Formula: C13H13N. Welcome to talk about 91-00-9, 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 send Email.

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

Product Details of 91-00-9. In 2020.0 GREEN CHEM 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. 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.

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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Authors Raimbault, A; Ma, CMA; Ferri, M; Baurer, S; Bonnet, P; Bourg, S; Lammerhofer, M; West, C in ELSEVIER 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. Recommanded Product: Diphenylmethanamine. 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.

Recommanded Product: Diphenylmethanamine. 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.

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

An article Synthesis and nematicidal evaluation of 1,2,3-benzotriazin-4-one derivatives containing piperazine as linker against Meloidogyne incognita WOS:000474501100016 published article about BIOLOGICAL-ACTIVITIES; MANNICH-BASES; DESIGN; ANTIFUNGAL; FLUORINE; PRODUCT; ANALOGS in [Chen, Xiulei; Jia, Haowu; 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 200237, Peoples R China in 2019, Cited 24. Product Details of 90-16-4. 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

To explore new skeleton with nematicidal activity, a series of novel 1,2,3-benzotriazin-4-one derivatives containing piperazine as linker were synthesized and varied fragments were also introduced to increase structure diversity of the new skeleton. Their inhibitory activities in vivo were evaluated against Meloidogyne incognita. The newly prepared compounds A6, A8, A21, A28 and A38 exhibited more than 50% inhibition at the concentration of 20 mg/L. Especially compound A6 displayed 71.4% inhibition against Meloidogyne incognita at the concentration of 20 mg/L. The nematicidal activities varied significantly depending on the types and positions of the substituents, which provided guidance for further structure modification. (C) 2019 Chinese Chemical Society and Institute of Materia Medica, Chinese Academy of Medical Sciences. Published by Elsevier B.V. All rights reserved.

Product Details of 90-16-4. Welcome to talk about 90-16-4, If you have any questions, you can contact Chen, XL; Jia, HW; Li, Z; Xu, XY or send Email.

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 Position of lipidation influences anticancer activity of Smac analogs WOS:000468145300016 published article about APOPTOSIS PROTEINS IAPS; HUMAN SERUM-ALBUMIN; X-LINKED INHIBITOR; STRUCTURAL BASIS; CELL-DEATH; REVERSIBLE LIPIDIZATION; CASPASE INHIBITION; POTENT ANTAGONISTS; TUMOR-REGRESSION; BIR DOMAINS 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 in 2019.0, Cited 79.0. COA of 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.

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.. COA of Formula: C13H13N

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

Computed Properties of C7H5N3O. In 2019 CHINESE CHEM LETT published article about BIOLOGICAL-ACTIVITIES; MANNICH-BASES; DESIGN; ANTIFUNGAL; FLUORINE; PRODUCT; ANALOGS in [Chen, Xiulei; Jia, Haowu; 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 200237, Peoples R China in 2019, 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.

To explore new skeleton with nematicidal activity, a series of novel 1,2,3-benzotriazin-4-one derivatives containing piperazine as linker were synthesized and varied fragments were also introduced to increase structure diversity of the new skeleton. Their inhibitory activities in vivo were evaluated against Meloidogyne incognita. The newly prepared compounds A6, A8, A21, A28 and A38 exhibited more than 50% inhibition at the concentration of 20 mg/L. Especially compound A6 displayed 71.4% inhibition against Meloidogyne incognita at the concentration of 20 mg/L. The nematicidal activities varied significantly depending on the types and positions of the substituents, which provided guidance for further structure modification. (C) 2019 Chinese Chemical Society and Institute of Materia Medica, Chinese Academy of Medical Sciences. Published by Elsevier B.V. All rights reserved.

Computed Properties of C7H5N3O. Bye, fridends, I hope you can learn more about C7H5N3O, If you have any questions, you can browse other blog as well. See you lster.

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

Product Details of 91-00-9. Authors Karteek, SD; Reddy, AG; Tej, MB; Rao, MVB in MAIK NAUKA/INTERPERIODICA/SPRINGER published article about in [Karteek, S. Durga] Koneru Lakshmaiah Educ Fdn, Dept Chem, Vaddeswaram 522502, India; [Reddy, A. Gopi] SANA Coll Pharm, Dept Pharm, Kodad 508206, India; [Tej, M. Bhuvan] Sri Ramachandra Med Coll & Res Inst, Dept Pharm, Chennai 600116, Tamil Nadu, India; [Rao, M. V. Basaveswara] Krishna Univ, Dept Chem, Machilipatnam 521001, India in 2021.0, Cited 38.0. The Name is Diphenylmethanamine. Through research, I have a further understanding and discovery of 91-00-9

A new series of fused tricyclic coumarin derivatives were designed, synthesized by a simple and convenient method, starting from 4-hydroxycoumarin and virtually screened by molecular docking on the target protein 3FRZ (PDB ID: 3FRZ), a HCV RNA-dependent RNA polymerase, for potency against hepatitis C virus (HCV). Efficient binding to the target protein was found for most of the synthesized compounds.

Product Details of 91-00-9. Welcome to talk about 91-00-9, If you have any questions, you can contact Karteek, SD; Reddy, AG; Tej, MB; Rao, MVB or send Email.

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

Formula: C7H5N3O. In 2019 CHINESE CHEM LETT published article about BIOLOGICAL-ACTIVITIES; MANNICH-BASES; DESIGN; ANTIFUNGAL; FLUORINE; PRODUCT; ANALOGS in [Chen, Xiulei; Jia, Haowu; 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 200237, Peoples R China in 2019, 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.

To explore new skeleton with nematicidal activity, a series of novel 1,2,3-benzotriazin-4-one derivatives containing piperazine as linker were synthesized and varied fragments were also introduced to increase structure diversity of the new skeleton. Their inhibitory activities in vivo were evaluated against Meloidogyne incognita. The newly prepared compounds A6, A8, A21, A28 and A38 exhibited more than 50% inhibition at the concentration of 20 mg/L. Especially compound A6 displayed 71.4% inhibition against Meloidogyne incognita at the concentration of 20 mg/L. The nematicidal activities varied significantly depending on the types and positions of the substituents, which provided guidance for further structure modification. (C) 2019 Chinese Chemical Society and Institute of Materia Medica, Chinese Academy of Medical Sciences. Published by Elsevier B.V. All rights reserved.

Bye, fridends, I hope you can learn more about C7H5N3O, If you have any questions, you can browse other blog as well. See you lster.. 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

Recommanded Product: 90-16-4. 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. 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.

Recommanded Product: 90-16-4. Welcome to talk about 90-16-4, If you have any questions, you can contact Chen, XL; Zhou, Z; Li, Z; Xu, XY or send Email.

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