Month: October 2021

Recommanded Product: 90-16-4. 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.

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. 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

COA of Formula: C7H5N3O. I found the field of Chemistry very interesting. Saw the article Synthesis and nematicidal activities of 1,2,3-benzotriazin-4-one containing 4,5-dihydrothiazole-2-thiol derivatives against Meloidogyne incognita published in 2020, Reprint Addresses Xu, XY (corresponding author), East China Univ Sci & Technol, Sch Pharm, Shanghai Key Lab Chem Biol, Shanghai 200237, Peoples R China.. 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.

COA 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

HPLC of Formula: C13H13N. Recently I am researching about E3 UBIQUITIN LIGASE; 2 SH2 DOMAIN; SIGNAL TRANSDUCER; PEPTIDOMIMETIC INHIBITORS; SMALL MOLECULES; DESIGN; DEGRADATION; ACTIVATOR; OPTIMIZATION; VALIDATION, Saw an article supported by the Oncopia Therapeutics Inc.; NIHUnited States Department of Health & Human ServicesNational Institutes of Health (NIH) – USA [P30 CA046592]; (Rogel Cancer Center) Core grant from the National Cancer Institute (NCI), NIH; DOE Office of ScienceUnited States Department of Energy (DOE) [DE-AC02-06CH11357]; Michigan Technology Tri-Corridor [085P1000817]. Published in AMER CHEMICAL SOC in WASHINGTON ,Authors: Zhou, HB; Bai, LC; Xu, RQ; Zhao, YJ; Chen, JY; McEachern, D; Chinnaswamy, K; Wen, B; Dai, LP; Kumar, P; Yang, CY; Liu, ZM; Wang, M; Liu, L; Meagher, JL; Yi, H; Sun, DX; Stuckey, JA; Wang, SM. The CAS is 91-00-9. Through research, I have a further understanding and discovery of Diphenylmethanamine

Signal transducer and activator of transcription 3 (STAT3) is a transcription factor and an attractive therapeutic target for cancer and other human diseases. Despite 20 years of persistent research efforts, targeting STAT3 has been very challenging. We report herein the structure-based discovery of potent small-molecule STAT3 degraders based upon the proteolysis targeting chimera (PROTAC) concept. We first designed SI-109 as a potent, small-molecule inhibitor of the STAT3 SH2 domain. Employing ligands for cereblon/cullin 4A E3 ligase and SI-109, we obtained a series of potent PROTAC STAT3 degraders, exemplified by SD-36. SD-36 induces rapid STAT3 degradation at low nanomolar concentrations in cells and fails to degrade other STAT proteins. SD-36 achieves nanomolar cell growth inhibitory activity in leukemia and lymphoma cell lines with high levels of phosphorylated STAT3. A single dose of SD-36 results in complete STAT3 protein degradation in xenograft tumor tissue and normal mouse tissues. SD-36 achieves complete and long-lasting tumor regression in the Molm-16 xenograft tumor model at well-tolerated dose-schedules. SD-36 is a potent, selective, and efficacious STAT3 degrader.

About Diphenylmethanamine, If you have any questions, you can contact Zhou, HB; Bai, LC; Xu, RQ; Zhao, YJ; Chen, JY; McEachern, D; Chinnaswamy, K; Wen, B; Dai, LP; Kumar, P; Yang, CY; Liu, ZM; Wang, M; Liu, L; Meagher, JL; Yi, H; Sun, DX; Stuckey, JA; Wang, SM or concate me.. HPLC of Formula: C13H13N

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

Computed Properties of C13H13N. In 2020.0 BIOL PHARM BULL published article about POTENT; MICROSOMES; BENZOFURAN; DIMERS in [Yamaguchi, Yuki; Nishizono, Naozumi; Oda, Kazuaki] Hlth Sci Univ Hokkaido, Sch Pharmaceut Sci, Ishikari, Hokkaido 0610293, Japan in 2020.0, Cited 27.0. The Name is Diphenylmethanamine. Through research, I have a further understanding and discovery of 91-00-9.

Aromatase inhibitors are effective for the treatment of diseases such as breast cancer, which has led to an increase in their demand. However, only a limited number of aromatase inhibitor drugs are currently being marketed. In addition, considering the important aspect of drug resistance, the development of newer drug types is required. We have been developing inhibitors with backbone structures that differ from existing aromatase inhibitors. In this regard, we previously reported that diethylaminocoumarin dimers and thiazolyl coumarin derivatives possess strong aromatase inhibiting capabilities. In this study, we further examined the structure activity relationships of coumarin derivatives synthesized from thiazolyl coumarin derivatives and their aromatase inhibiting capabilities. Consequently, amide coumarin N-benzhydry1-7-(diethylamino)2-oxo-2H-chromene-3-carboxamide (IC50 values 4.5 mu M) is inhibitor of aromatase. This inhibitor was found to be comparable aromatase inhibitory activity to the 1st generation aromatase inhibitor aminoglutethimide (3.2 mu M). Substitution of the amide group on the amide coumarin derivative affects the aromatase inhibiting activity. Our findings suggest that the structure of each substituent changes the orientation of the compound in the active site of aromatase, thus creating a difference in their activities.

Computed Properties of C13H13N. About Diphenylmethanamine, If you have any questions, you can contact Yamaguchi, Y; Nishizono, N; Oda, K or concate me.

Reference:
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. COA 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.

COA of Formula: C7H5N3O. 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

Product Details of 91-00-9. In 2020.0 ORG LETT published article about EFFICIENT; ARYLATION; AMIDES in [Gao, Zhenhua; Li, Junchen; Shi, Enxue] State Key Lab NBC Protect Civilian, Beijing 102205, Peoples R China; [Li, Bowen; Aliyu, Muinat; Li, Tiejun; Dong, Wei; Tang, Wenjun] Shanghai Inst Organ Chem, State Key Lab Bioorgan & Nat Prod Chem, Shanghai 200032, Peoples R China; [Li, Bowen; Tang, Wenjun] Univ Chinese Acad Sci, Sch Chem & Mat Sci, Hangzhou Inst Adv Study, Hangzhou 310024, Peoples R China in 2020.0, Cited 34.0. The Name is Diphenylmethanamine. Through research, I have a further understanding and discovery of 91-00-9.

A general synthesis of chiral alpha,alpha-diaryl carboxamides is developed by enantioselective cross-coupling between 2-bromo-2-aryl carboxamides and arylboronic acids, leading to a series of chiral alpha,alpha-diaryl carboxamides with various electronic properties and functionalities in moderate to excellent enantioselectivities and yields. The employment of a sterically bulky chiral P,P=O ligand L2 is critical for the reactivity and selectivity. This protocol is applied to an efficient asymmetric synthesis of a key intermediate of dopamine receptor agonist SKF 38393.

Product Details of 91-00-9. About Diphenylmethanamine, If you have any questions, you can contact Li, BW; Aliyu, M; Gao, ZH; Li, TJ; Dong, W; Li, JC; Shi, EX; Tang, WJ or concate me.

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

COA of Formula: C13H13N. In 2019.0 ORG LETT published article about DIRECT AMIDE FORMATION; MECHANISTIC INSIGHTS; BOND FORMATION; BORONIC ACIDS; CONDENSATION; ALPHA; CYCLOADDITIONS; ACTIVATION; CHEMISTRY; AMINES in [Shimada, Naoyuki] Kitasato Univ, Dept Pharmaceut Sci, Lab Organ Chem Drug Dev, Tokyo 1088641, Japan; Kitasato Univ, Dept Pharmaceut Sci, Med Res Labs, Tokyo 1088641, Japan in 2019.0, Cited 72.0. The Name is Diphenylmethanamine. Through research, I have a further understanding and discovery of 91-00-9.

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.. COA of Formula: C13H13N

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

COA of Formula: C13H13N. I found the field of Pharmacology & Pharmacy very interesting. Saw the article Structure-activity relationships of potentiators of the antibiotic activity of clarithromycin against Escherichia coli published in 2019.0, Reprint Addresses LaVoie, EJ (corresponding author), Rutgers State Univ, Ernest Mario Sch Pharm, 160 Frelinghuysen Rd, Piscataway, NJ 08854 USA.. The CAS is 91-00-9. Through research, I have a further understanding and discovery of Diphenylmethanamine.

Several studies that have identified agents that potentiate the antimicrobial activity of antibiotics, but there are limited insights into their structure-activity relationships (SAR). The SAR associated with select N-alkylaryl amide derivatives of ornithine was performed to establish those structural features that were associated with potentiation of the antimicrobial activity of clarithromycin against E. coli ATCC 25922. The data indicate that the N-propyl derivative was slightly more active in reducing the effective MIC of clarithromycin against E. coli ATCC 25922. In addition, the S-enantiomer of compound 9 was somewhat more potent than the R-enantiomer in potentiating clarithromycin activity. No significant enhancement in potentiation activity was observed with the conversion of these secondary amides to their N-methyl tertiary amides. Formation of the N-methyl or N,N-dimethyl derivatives of the primary amine of 9 was associated with the loss of potentiation activity. Conversion of this primary amine to a guanidine was also not associated with an increase in potentiation activity. Among the isomeric diamino pentamides, 15 potentiated the antibacterial activity of clarithromycin to the greatest extent In addition to these amide derivatives, the desoxy derivatives 16 and 18 were the more potent potentiators within this triamine series. The relative location of the primary amines, as indicated by the relative differences in the potentiation observed with 16 compared to 14, appears to be a critical factor in determining potentiation activity. Cell-based membrane permeabilization and efflux inhibition studies in E. coli ATCC 25922 suggest that the potentiation of clarithromycin activity by 16 reflects its ability to inhibit efflux pump activity and to a lesser extent its actions as a permeabilizer of the outer leaflet of the outer cell membrane. (C) 2019 Elsevier Masson SAS. All rights reserved.

COA of Formula: C13H13N. About Diphenylmethanamine, If you have any questions, you can contact Blankson, G; Parhi, AK; Kaul, M; Pilch, DS; LaVoie, EJ or concate me.

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

Meng, GY; Guo, TJ; Ma, TC; Zhang, J; Shen, YC; Sharpless, KB; Dong, JJ in [Meng, Genyi; Guo, Taijie; Ma, Tiancheng; Zhang, Jiong; Shen, Yucheng; Sharpless, Karl Barry; Dong, Jiajia] Univ Chinese Acad Sci, Ctr Excellence Mol Synth, Shanghai Inst Organ Chem, Key Lab Organofluorine Chem,Chinese Acad Sci, Shanghai, Peoples R China published Modular click chemistry libraries for functional screens using a diazotizing reagent in 2019, Cited 33. COA of Formula: C13H13N. The Name is Diphenylmethanamine. Through research, I have a further understanding and discovery of 91-00-9.

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.

COA of Formula: C13H13N. 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

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.

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

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