Month: November 2021

El Rayes, SM; Ali, IAI; Fathalla, W; Mahmoud, MAA 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 published Synthesis and Biological Activities of Some New Benzotriazinone Derivatives Based on Molecular Docking; Promising HepG2 Liver Carcinoma Inhibitors in 2020, Cited 24. Application In Synthesis 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.

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).

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.. Application In Synthesis of Benzo[d][1,2,3]triazin-4(3H)-one

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

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

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. 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

Authors 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 in ROYAL SOC CHEMISTRY 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. Recommanded Product: 104-10-9. The Name is 2-(4-Aminophenyl)ethanol. Through research, I have a further understanding and discovery of 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.

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

Recommanded Product: Diphenylmethanamine. Peng, K; Luo, Q; Zhang, YC; Xia, JB in [Peng, Kai; Luo, Qi; Zhang, Yichi; Xia, Jiangbin] Wuhan Univ, Coll Chem & Mol Sci, Hubei Key Lab Organ & Polymer Optoelect Mat, Wuhan 430072, Peoples R China; [Xia, Jiangbin] Wuhan Univ, Coll Chem & Mol Sci, Minist Educ, Engn Res Ctr Organosilicon Cpds & Mat, Wuhan 430072, Peoples R China published Novel synthesis of poly(3,4-dinitro-thiophen-2-yl arylamine) derivatives via facile C-Br/N-H bulk polycondensation and its application of thermalsensor in 2020.0, Cited 42.0. The Name is Diphenylmethanamine. Through research, I have a further understanding and discovery of 91-00-9.

C-Br/N-H bulk polycondensation is firstly proposed and corresponding poly(3,4-dinitm-thiophen-2-yl aryl-amine)s derivatives have been successfully obtained with quantitative yield. Typical crystal analysis reveals that its effective reaction points distance (RPD, distance between Br and H atom) is 5.083 angstrom, which is 66.7% longer than the sum of van der Waals radius (r(w)) of bromine and hydrogen atoms (3.05 angstrom). Carbazole-based monomer was explored as a thermalsensor with excellent relative sensitivity (S-a) of 0.45% K-1.

Recommanded Product: Diphenylmethanamine. Welcome to talk about 91-00-9, If you have any questions, you can contact Peng, K; Luo, Q; Zhang, YC; Xia, JB or send Email.

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

Authors Matsumoto, K; Takeda, S; Hirokane, T; Yoshida, M in AMER CHEMICAL SOC published article about BOND FORMATION; DERIVATIVES; ARYLATION; BINAM; BIPHENOLS; PHENOLS in [Matsumoto, Kenji; Takeda, Satoshi; Hirokane, Tsukasa; Yoshida, Masahiro] Tokushima Bunri Univ, Fac Pharmaceut Sci, 180 Nishihama Boji, Yamashiro, Tokushima 7708514, Japan in 2019.0, Cited 58.0. Application In Synthesis of 2-(4-Aminophenyl)ethanol. The Name is 2-(4-Aminophenyl)ethanol. Through research, I have a further understanding and discovery of 104-10-9

The first catalytic oxidative aniline-aniline cross-coupling reaction using oxygen as the terminal oxidant is reported. Anilines possessing a pyrrolidino group can be preferentially oxidized under mild aerobic conditions and reacted with other anilines to afford a variety of nonsymmetrical 2-aminobiphenyls with high selectivities. A heterogeneous palladium catalyst is used for the dehydrogenative cross-coupling of anilines with structurally diverse arenes. This reaction does not require stoichiometric oxidants and is an economical and environmentally friendly method.

Application In Synthesis of 2-(4-Aminophenyl)ethanol. Welcome to talk about 104-10-9, If you have any questions, you can contact Matsumoto, K; Takeda, S; Hirokane, T; Yoshida, M or send Email.

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

Product Details of 91-00-9. Recently I am researching about SULFOXONIUM YLIDES; BOND ACTIVATION; RH(III)-CATALYZED SYNTHESIS; ORGANIC-SYNTHESIS; DIAZO-COMPOUNDS; PRIMARY AMINES; BENZYLAMINES; ANNULATION; ALKYNES; FUNCTIONALIZATION, Saw an article supported by the NSFCNational Natural Science Foundation of China (NSFC) [81373259, 81573286, 81602954]. Published in ROYAL SOC CHEMISTRY in CAMBRIDGE ,Authors: Nie, RF; Lai, RZ; Lv, SY; Xu, YY; Guo, L; Wang, QT; Wu, Y. The CAS is 91-00-9. Through research, I have a further understanding and discovery of Diphenylmethanamine

A water-mediated C-H activation using sulfoxonium ylides is reported, providing a general, green and step-economic approach to construct a C-C bond and varieties of useful N-heterocycle scaffolds. Notably, the water-mediated activation, in contrast to that in organic solvents, shows great potential in pharmaceutical, biochemistry and chemical industries.

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

An article Chemical profiling of HIV-1 capsid-targeting antiviral PF74 WOS:000546723400025 published article about THERMAL SHIFT ASSAYS; CYCLOPHILIN-A; REPLICATION; INFECTION; PROTEIN; ROLES; INHIBITION; DISCOVERY; POTENT; CELLS in [Wang, Lei; Vernekar, Sanjeev Kumar V.; Do, Ha T.; Sahani, Rajkumar Lalji; Xie, Jiashu; Wang, Zhengqiang] Univ Minnesota, Coll Pharm, Ctr Drug Design, Minneapolis, MN 55455 USA; [Casey, Mary C.] Univ Missouri, Christopher S Bond Life Sci Ctr, Dept Mol Microbiol & Immunol, Sch Med, Columbia, MO 65211 USA; [Kirby, Karen A.; Du, Haijuan; Zhang, Huanchun; Tedbury, Philip R.; Sarafianos, Stefan G.] Emory Univ, Dept Pediat, Lab Biochem Pharmacol, Sch Med, Atlanta, GA 30322 USA; [Hachiya, Atsuko] Natl Hosp Org, Clin Res Ctr, Nagoya Med Ctr, Nagoya, Aichi 4600001, Japan; [Wang, Lei] Dalian Univ Technol, Sch Chem Engn, Dept Pharm, Dalian 116024, Peoples R China in 2020.0, Cited 51.0. COA of Formula: C13H13N. The Name is Diphenylmethanamine. Through research, I have a further understanding and discovery of 91-00-9

The capsid protein (CA) of HIV-1 plays essential roles in multiple steps of the viral replication cycle by assembling into functional capsid core, controlling the kinetics of uncoating and nuclear entry, and interacting with various host factors. Targeting CA represents an attractive yet underexplored antiviral approach. Of all known CA-targeting small molecule chemotypes, the peptidomimetic PF74 is particularly interesting because it binds to the same pocket used by a few important host factors, resulting in highly desirable antiviral phenotypes. However, further development of PF74 entails understanding its pharmacophore and mitigating its poor metabolic stability. We report herein the design, synthesis, and evaluation of a large number of PF74 analogs aiming to provide a comprehensive chemical profiling of PF74 and advance the understanding on its detailed binding mechanism and pharmacophore. The analogs, containing structural variations mainly in the aniline domain and/or the indole domain, were assayed for their effect on stability of CA hexamers, antiviral activity, and cytotoxicity. Selected analogs were also tested for metabolic stability in liver microsomes, alone or in the presence of a CYP3A inhibitor. Collectively, our studies identified important pharmacophore elements and revealed additional binding features of PF74, which could aid in future design of improved ligands to better probe the molecular basis of CA-host factor interactions, design strategies to disrupt them, and ultimately identify viable CA-targeting antiviral leads. (C) 2020 Elsevier Masson SAS. All rights reserved.

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

Category: amides-buliding-blocks. In 2019.0 J MED CHEM published article about CYCLIC-NUCLEOTIDE PHOSPHODIESTERASES; CAMP-SPECIFIC PHOSPHODIESTERASE; LONG-TERM-MEMORY; PROTEIN-KINASE; MOLECULAR-MECHANISMS; ADENYLYL-CYCLASE; STRUCTURAL BASIS; AMP PRODUCTION; KNOCKOUT MICE; DROSOPHILA in [Gurney, Mark E.; Nugent, Richard A.; Mo, Xuesheng; Sindac, Janice A.] Tetra Discovery Partners Inc, 38 Fulton St West, Grand Rapids, MI 49503 USA; [Hagen, Timothy J.] Northern Illinois Univ, Dept Chem & Biochem, 1425 West Lincoln Highway, De Kalb, IL 60115 USA; [Fox, David, III] Beryllium Discovery Corp, 7869 NE Day Rd West, Bainbridge Isl, WA 98110 USA; [O’Donnell, James M.; Zhang, Chong; Xu, Ying] SUNY Buffalo, Dept Pharmaceut Sci, Sch Pharm & Pharmaceut Sci, Buffalo, NY 14214 USA; [Zhang, Han-Ting] West Virginia Univ, Hlth Sci Ctr, Rockefeller Neurosci Inst, Dept Behav Med & Psychiat, 1 Med Ctr Dr, Morgantown, WV 26506 USA; [Zhang, Han-Ting] West Virginia Univ, Hlth Sci Ctr, Rockefeller Neurosci Inst, Dept Physiol Pharmacol & Neurosci, 1 Med Ctr Dr, Morgantown, WV 26506 USA; [Groppi, Vincent E.] Univ Michigan, Michigan Drug Discovery, Life Sci Inst, 210 Washtenaw Ave, Ann Arbor, MI 48103 USA; [Bailie, Marc] INDS Inc, 6111 Jackson Rd,Suite 100, Ann Arbor, MI 48103 USA; [White, Ronald E.] White Global Pharma Consultants, 31 Kinglet Dr, South Cranbury, NJ 08512 USA; [Romero, Donna L.] Pharma Vat Consulting LLC, 1201 Turnberry Ridge Court, Chesterfield, MO 63005 USA; [Vellekoop, A. Samuel; Walker, Joel R.; Surman, Matthew D.; Zhu, Lei; Campbell, Robert F.] Albany Mol Res Inc, 21 Corp Circle, Albany, NY 12203 USA; [Fox, David, III] UCB Pharma, 7869 NE Day Rd West, Bainbridge Isl, WA 98110 USA; [Zhang, Chong] Janssen China R&D, 65 Guiqing Rd,Bldg A,Floor 6, Shanghai 200233, Peoples R China; [Campbell, Robert F.] Walter Reed Army Inst Res, 503 Robert Grant Ave, Silver Spring, MD 20910 USA in 2019.0, Cited 81.0. The Name is 2-(4-Aminophenyl)ethanol. Through research, I have a further understanding and discovery of 104-10-9.

Novel pyridine- and pyrimidine-based allosteric inhibitors are reported that achieve PDE4D subtype selectivity through recognition of a single amino acid difference on a key regulatory domain, known as UCR2, that opens and closes over the catalytic site for cAMP hydrolysis. The design and optimization of lead compounds was based on iterative analysis of X-ray crystal structures combined with metabolite identification. Selectivity for the activated, dimeric form of PDE4D provided potent memory enhancing effects in a mouse model of novel object recognition with improved tolerability and reduced vascular toxicity over earlier PDE4 inhibitors that lack subtype selectivity. The lead compound, 28 (BPN14770), has entered midstage, human phase 2 clinical trials for the treatment of Fragile X Syndrome.

Welcome to talk about 104-10-9, If you have any questions, you can contact Gurney, ME; Nugent, RA; Mo, XS; Sindac, JA; Hagen, TJ; Fox, D; O’Donnell, JM; Zhang, C; Xu, Y; Zhang, HT; Groppi, VE; Bailie, M; White, RE; Romero, DL; Vellekoop, AS; Walker, JR; Surman, MD; Zhu, L; Campbell, RF or send Email.. Category: amides-buliding-blocks

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

Authors El Rayes, SM; Ali, IAI; Fathalla, W; Mahmoud, MAA in AMER CHEMICAL SOC 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. Computed Properties of 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

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).

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

Recommanded Product: 91-00-9. Recently I am researching about ASYMMETRIC-SYNTHESIS; HYDROPHOSPHONYLATION; AMINALIZATION; IMINES; ACID, Saw an article supported by the National Natural Science Foundation of ChinaNational Natural Science Foundation of China (NSFC) [51373067]. Published in AMER CHEMICAL SOC in WASHINGTON ,Authors: Liu, YX; Wang, JD; Wei, ZL; Cao, JG; Liang, DP; Lin, YJ; Duan, HF. The CAS is 91-00-9. Through research, I have a further understanding and discovery of Diphenylmethanamine

N,N’-Acetals are sensitive compounds, and the challenging asymmetric synthesis of acyclic N,N’-acetals by the general addition of amines to ketimines has never been reported so far. In this study, highly enantioselective addition of aryl amines to isatin-derived ketimines catalyzed by chiral urea derived from quinine was developed. A series of new acyclic N,N’-acetals were constructed by this protocol in high to excellent yields (78-99%) and high to excellent enantioselectivities (76-96% ee).

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