Category: 93-97-0

Recently I am researching about VON-WILLEBRAND-FACTOR; PLATELET ACTIVATION; PREVENTS THROMBOSIS; LACTIC-ACIDOSIS; METFORMIN; RISK; ADHESION; PRODRUG, Saw an article supported by the National Natural Science Foundation of ChinaNational Natural Science Foundation of China (NSFC) [81673710, 81973580]; National Major Scientific and Technological Special Project for Significant New Drugs Development [2019ZX09201005-005-001, 2019ZX09201005-005-004]; Applied Basic Research Programs of Department of Science and Technology of Sichuan Province [2019YJ0095]; National Science Foundation for Young Scientists of China [81803866]; China Postdoctoral Science FoundationChina Postdoctoral Science Foundation [2018M640932, 2019T120854]; Innovative Chinese Medicine and Health Products Research Academician Workstation of Academician Zhang Boli and Academician Zhu Beiwei, West China Hospital, Sichuan University [HXYS19001, HXYS19002]; Postdoctoral Interdisciplinary Research Project of Sichuan University [2019JCXK3245]; Post-Doctor Research Project, West China Hospital, Sichuan University [2018HXBH061, 2019HXBH024]; Sichuan Science and Technology Department Emergency Project for COVID-19 [2020YFS0554]. Formula: C14H10O3. Published in ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER in ISSY-LES-MOULINEAUX ,Authors: Xin, G; Ming, Y; Ji, CJ; Wei, ZL; Li, SY; Morris-Natschke, SL; Zhang, XY; Yu, K; Li, YP; Zhang, BL; Zhang, JH; Xing, ZH; He, YR; Chen, Z; Yang, XJ; Niu, H; Lee, KH; Huang, W. The CAS is 93-97-0. Through research, I have a further understanding and discovery of Benzoic anhydride

Platelet thrombosis is the main pathogeny resulting in the low curability of ischemic stroke, a leading cause of mortality and disability worldwide. Metformin, a biguanide derivative that is the first-line oral medicine for type 2 diabetes, alleviates the severity of ischemic stroke in diabetic patients and suppresses platelet activation in experimental animal model. However, the clinical implementation of commercial biguanide analogs for stroke related to platelet thrombosis remains challenging due to its weak potency, poor pharmacokinetic characteristics and possible hypoglycemia. Here, twenty-three biguanide derivatives were designed and synthesized based on the principles of bioisosteres. These derivatives were evaluated for the activity of antiplatelet thrombosis in vivo. We found that N-tri-fluoromethanesulfonyl biguanide derivative, compound b10, uniquely prevented cerebral infarction as well as neuronal function injury, and significantly decrease the mortality rate of ischemic stroke in the middle cerebral artery occlusion mice without significant side effects. We verified that b10 directly inhibited platelets thrombus formation and decreased the compactness of stroke thrombi. Particularly, b10 exhibited good potency to inhibit human platelet activation including platelet aggregation, adhesion, pseudopodia formation, integrin GPIIb/IIIa activation, CD62P expression and clot retraction. Meanwhile, the pharmacokinetics assessment showed that b10 had satisfying pharmacological characteristics including a longer duration and a higher oral absorption ratio than its parent compound. In addition, b10 remarkably ameliorated not only stroke related to platelet thrombosis but also carotid artery thrombus formation. It is concluded that the novel potent antiplatelet thrombotic agent derived from biguanide is a promising candidate for stroke treatment. (C) 2020 Elsevier Masson SAS. All rights reserved.

About Benzoic anhydride, If you have any questions, you can contact Xin, G; Ming, Y; Ji, CJ; Wei, ZL; Li, SY; Morris-Natschke, SL; Zhang, XY; Yu, K; Li, YP; Zhang, BL; Zhang, JH; Xing, ZH; He, YR; Chen, Z; Yang, XJ; Niu, H; Lee, KH; Huang, W or concate me.. Formula: C14H10O3

Reference:
Isothiazole – Wikipedia,
,Isothiazole – ScienceDirect.com

An article Expedient Synthesis of Alphitolic Acid and Its Naturally Occurring 2-O-Ester Derivatives WOS:000466442100024 published article about OCCURRING PENTACYCLIC TRITERPENES; BETULINIC ACID; GLYCOGEN-PHOSPHORYLASE; MASLINIC ACID; INHIBITORS; LUPANES; ACCESS; LEAVES in [Park, Somin; Cho, Jihee; Jeon, Hongjun; Sung, Sang Hyun; Lee, Seunghee; Kim, Sanghee] Seoul Natl Univ, Coll Pharm, 1 Gwanak Ro, Seoul 08826, South Korea in 2019, Cited 32. Computed Properties of C14H10O3. The Name is Benzoic anhydride. Through research, I have a further understanding and discovery of 93-97-0

The expedient synthesis of alphitolic acid (1) as well as its natural C-3-epimer and 2-O-ester derivatives was accomplished in a few steps from the readily commercially available betulin (9). A Rubottom oxidation delivered an alpha-hydroxy group in a stereo-and chemoselective manner. The diastereoselective reduction of the a-hydroxy ketone was key to accessing the 1,2-diol moiety of this class of natural products. Our concise and stereoselective synthetic protocol allowed the gram-scale synthesis of these natural products, which will facilitate future biological evaluations.

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Reference:
Isothiazole – Wikipedia,
,Isothiazole – ScienceDirect.com

An article B(C6F5)(3)-Catalyzed Direct C3 Alkylation of Indoles and Oxindoles WOS:000543700400038 published article about H BOND ACTIVATION; CATALYZED METHYLATION; BORYLATION; REACTIVITY; COMPLEXES; METHANOL; FUNCTIONALIZATION; GENERATION; PYRROLES; AGONIST in [Basak, Shyam; Melen, Rebecca L.; Morrill, Louis C.] Cardiff Univ, Sch Chem, Cardiff Catalysis Inst, Cardiff CF10 3AT, Wales; [Alvarez-Montoya, Ana; Winfrey, Laura; Pulis, Alexander P.] Univ Leicester, Sch Chem, Leicester LE1 7RH, Leics, England in 2020, Cited 60. The Name is Benzoic anhydride. Through research, I have a further understanding and discovery of 93-97-0. Name: Benzoic anhydride

The direct C3 alkylation of indoles and oxindoles is a challenging transformation, and only a few direct methods exist. Utilizing the underexplored ability of triaryl boranes to mediate the heterolytic cleavage of alpha-nitrogen C-H bonds in amines, we have developed a catalytic approach for the direct C3 alkylation of a wide range of indoles and oxindoles using amine-based alkylating agents. We also employed this borane-catalyzed strategy in an alkylation-ring opening cascade.

Name: Benzoic anhydride. Welcome to talk about 93-97-0, If you have any questions, you can contact Basak, S; Alvarez-Montoya, A; Winfrey, L; Melen, RL; Morrill, LC; Pulis, AP or send Email.

Reference:
Isothiazole – Wikipedia,
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I found the field of Chemistry very interesting. Saw the article Pd(II)-Catalyzed Enantioselective gamma-C(sp(3))-H Functionalizations of Free Cyclopropylmethylamines published in 2020. Application In Synthesis of Benzoic anhydride, Reprint Addresses Yu, JQ (corresponding author), Scripps Res Inst, Dept Chem, La Jolla, CA 92037 USA.. The CAS is 93-97-0. Through research, I have a further understanding and discovery of Benzoic anhydride

Prized for their ability to reliably forge stereocenters with precise regiocontrol from simple and abundant starting materials, substrate-directable enantioselective reactions are widely used in modern organic synthesis. As such, enantioselective C(sp(3))-H functionalization reactions directed by innate functional groups could provide new routes to introduce molecular complexity within the inert hydrocarbon moiety, but to date this approach has been met with little success. While free primary aliphatic amines are common, versatile intermediates in synthesis, they are traditionally unreactive in C(sp(3))-H activation reactions. Herein we report the Pd-catalyzed enantioselective C(sp(3))-H functionalization of free aliphatic amines (cyclopropylmethylamines) enabled by a chiral bidentate thioether ligand. This ligand’s privileged bidentate coordination mode and thioether motif favor the generation of the requisite mono(amine)-Pd(II) intermediate, thus enabling the enantioselective C-H activation of free amines. The resulting C-Pd(II) species could engage in either Pd(II)/Pd(IV) or Pd(II)/Pd(0) catalytic cycles, enabling access to a diverse range of products through (hetero)arylation, carbonylation, and olefination reactions. Consequently, this versatile reactivity offers medicinal chemists a general strategy to rapidly prepare and functionalize biologically relevant amines.

Application In Synthesis of Benzoic anhydride. Bye, fridends, I hope you can learn more about C14H10O3, If you have any questions, you can browse other blog as well. See you lster.

Reference:
Isothiazole – Wikipedia,
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An article Entry to 1,2,3,4-Tetrasubstituted Arenes through Addressing the Meta Constraint in the Palladium/Norbornene Catalysis WOS:000514255300043 published article about ALKYLATION-ALKENYLATION REACTIONS; C-H FUNCTIONALIZATION; EFFICIENT SYNTHESIS; ARYL IODIDES; ARYLATION; PSYMBERIN; ACYLATION; ROUTE in [Wang, Jianchun; Zhou, Yun; Xu, Xiaolong; Dong, Guangbin] Univ Chicago, Dept Chem, 5735 S Ellis Ave, Chicago, IL 60637 USA; [Zhou, Yun] China Agr Univ, Dept Appl Chem, Beijing 100193, Peoples R China; [Xu, Xiaolong] ShanghaiTech Univ, Sch Phys Sci & Technol, Shanghai 201210, Peoples R China; [Liu, Peng] Univ Pittsburgh, Dept Chem, Pittsburgh, PA 15260 USA in 2020, Cited 51. The Name is Benzoic anhydride. Through research, I have a further understanding and discovery of 93-97-0. Category: isothiazole

Arenes with four different contiguous substituents, i.e. 1,2,3,4-tetrasubstituted arenes, are commonly found in bioactive compounds, but they are nontrivial to access via conventional methods. Through addressing the meta constraint in the palladium/norbornene (Pd/NBE) cooperative catalysis, which is the difficulty of tolerating a sizable meta substituent in aryl halide substrates, here a modular and regioselective approach is realized for preparing 1,2,3,4-tetrasubstituted arenes. One key is the use of a C2-amide-substituted NBE, and a combined experimental and computational study reveals its role in promoting the NBE insertion and the ortho C-H metalation steps. The scope is broad: a variety of electrophiles and nucleophiles could be introduced to the ortho and ipso positions, respectively, with 1,4-disubstituted aryl halides, leading to diverse unsymmetrical contiguous tetrasubstituted arenes. Application of this approach has been demonstrated in streamlined syntheses of several bioactive compounds.

Category: isothiazole. About Benzoic anhydride, If you have any questions, you can contact Wang, JC; Zhou, Y; Xu, XL; Liu, P; Dong, GB or concate me.

Reference:
Isothiazole – Wikipedia,
,Isothiazole – ScienceDirect.com

SDS of cas: 93-97-0. I found the field of Plant Sciences; Pharmacology & Pharmacy very interesting. Saw the article Oleanolic Acid Derivatives as Potential Inhibitors of HIV-1 Protease published in 2019, Reprint Addresses Rivas, F; Parra, A (corresponding author), Univ Granada, Fac Ciencias, Dept Quim Organ, E-18071 Granada, Spain.; Reyes-Zurita, FJ (corresponding author), Univ Granada, Fac Ciencias, Dept Bioquim & Biol Mol 1, E-18071 Granada, Spain.. The CAS is 93-97-0. Through research, I have a further understanding and discovery of Benzoic anhydride.

Pentacyclic triterpenes, such as oleanolic acid (I), are promising scaffolds for diversification through the use of combinatorial methods to obtain derivatives that improve their biological properties, increasing their bioavailability and enhancing their therapeutic efficacy. The purpose of this study was to evaluate the influence that derivatives of oleanolic acid, conjugated with one or two amino acids and an acyl group, might exert on HIV-1 protease inhibition. The in vitro studies conducted suggested that the presence of a carboxyacyl group generally improves the inhibition of HIV-1 protease, especially when a phthaloyl group is present, with IC50 concentration values below 5 mu M. The gain in activity of three 3-phthaloyl derivatives, with sub-micromolar IC50 values, was between 60- and 100-fold more active than oleanolic acid. A molecular docking study has also been performed to elucidate the mode of binding to the protease by these oleanolic acid derivatives. In general, the derivatives that exhibited the highest inhibitory activity of HIV-1 protease also showed the highest binding energies in docking simulations. The overall results suggest that the coupling of one or two amino acids and a phthaloyl group to oleanolic acid improves HIV-1 protease inhibition, implying that these triterpene derivatives may be promising antiviral agents against HIV.

SDS of cas: 93-97-0. Bye, fridends, I hope you can learn more about C14H10O3, If you have any questions, you can browse other blog as well. See you lster.

Reference:
Isothiazole – Wikipedia,
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An article Understanding monoacylation of symmetrical diamines: A kinetic study of acylation reaction of m-phenylenediamine and benzoic anhydride in microreactor WOS:000561589200006 published article about CONTINUOUS-FLOW PROCESS; PRIMARY AMINES; DERIVATIVES; INHIBITORS; DESIGN; POTENT in [Xu, Qilin; Su, Weike] Zhejiang Univ Technol, Coll Pharmaceut Sci, Key Lab Green Pharmaceut Technol & Related Equipm, Minist Educ, Hangzhou 310014, Peoples R China; [Fan, Huachun; Yao, Hongmiao; Wang, Duoheng; Yu, Hangwei; Chen, Bingbing; Yu, Zhiqun; Su, Weike] Zhejiang Univ Technol, Collaborat Innovat Ctr Yangtze River Delta Reg Gr, Natl Engn Res Ctr Proc Dev Act Pharmaceut Ingredi, Hangzhou 310014, Peoples R China in 2020, Cited 41. The Name is Benzoic anhydride. Through research, I have a further understanding and discovery of 93-97-0. Recommanded Product: 93-97-0

Monoacylated symmetrical diamines are building blocks or intermediates of several well-established drugs. However, for the symmetrical diamines, the two amine groups located in a similar chemical environment make the selective monoacylation rather difficult and no kinetics study has ever been reported before. To comprehend this kind of reaction more deeply, a continuous flow microfluidic system was developed to evaluate the reaction kinetics of m-phenylenediamine and benzoic anhydride. At first, the reaction order of each reactant, pre-exponential factors and activation energies were determined in turn. The possible reaction mechanism was postulated from the reaction order. Then, a series of validation experiments were designed to show the accuracy and the applied range (concentration and temperature) of the kinetic model. Next, to obtain a controlled selectivity, the effects of initial concentration, reaction temperature and molar ratio on the selectivity were investigated through the model simulation. In the end, under the conditions optimized by the kinetic model, 96.9% selectivity and 92.5% yield were obtained in the microreactor.

Welcome to talk about 93-97-0, If you have any questions, you can contact Xu, QL; Fan, HC; Yao, HM; Wang, DH; Yu, HW; Chen, BB; Yu, ZQ; Su, WK or send Email.. Recommanded Product: 93-97-0

Reference:
Isothiazole – Wikipedia,
,Isothiazole – ScienceDirect.com

SDS of cas: 93-97-0. Authors Sakai, T; Matsuo, Y; Okuda, K; Hirota, K; Tsuji, M; Hirayama, T; Nagasawa, H in NATURE RESEARCH published article about in [Sakai, Takayuki; Tsuji, Mieko; Hirayama, Tasuku; Nagasawa, Hideko] Gifu Pharmaceut Univ, Lab Pharmaceut & Med Chem, Gifu, Gifu 5011196, Japan; [Matsuo, Yoshiyuki; Hirota, Kiichi] Kansai Med Univ, Inst Biomed Sci, Dept Human Stress Response Sci, 2-5-1 Shin Machi, Hirakata, Osaka 5731010, Japan; [Okuda, Kensuke] Kobe Pharmaceut Univ, Lab Bioorgan & Nat Prod Chem, 4-19-1 Motoyama Kita, Kobe, Hyogo 6588558, Japan in 2021, Cited 52. The Name is Benzoic anhydride. Through research, I have a further understanding and discovery of 93-97-0

To develop antitumor drugs capable of targeting energy metabolism in the tumor microenvironment, we produced a series of potent new biguanide derivatives via structural modification of the arylbiguanide scaffold. We then conducted biological screening using hypoxia inducible factor (HIF)-1- and unfolded protein response (UPR)-dependent reporter assays and selective cytotoxicity assay under low glucose conditions. Homologation studies of aryl-(CH2)(n)-biguanides (n=0-6) yielded highly potent derivatives with an appropriate alkylene linker length (n=5, 6). The o-chlorophenyl derivative 7l (n=5) indicated the most potent inhibitory effects on HIF-1- and UPR-mediated transcriptional activation (IC50; 1.0 +/- 0.1 mu M, 7.5 +/- 0.1 mu M, respectively) and exhibited selective cytotoxicity toward HT29 cells under low glucose condition (IC50; 1.9 +/- 0.1 mu M). Additionally, the protein expression of HIF-1 alpha induced by hypoxia and of GRP78 and GRP94 induced by glucose starvation was markedly suppressed by the biguanides, thereby inhibiting angiogenesis. Metabolic flux and fluorescence-activated cell sorting analyses of tumor cells revealed that the biguanides strongly inhibited oxidative phosphorylation and activated compensative glycolysis in the presence of glucose, whereas both were strongly suppressed in the absence of glucose, resulting in cellular energy depletion and apoptosis. These findings suggest that the pleiotropic effects of these biguanides may contribute to more selective and effective killing of cancer cells due to the suppression of various stress adaptation systems in the tumor microenvironment.

Welcome to talk about 93-97-0, If you have any questions, you can contact Sakai, T; Matsuo, Y; Okuda, K; Hirota, K; Tsuji, M; Hirayama, T; Nagasawa, H or send Email.. SDS of cas: 93-97-0

Reference:
Isothiazole – Wikipedia,
,Isothiazole – ScienceDirect.com

Application In Synthesis of Benzoic anhydride. Authors Yue, WJ; Zhang, CY; Yin, L in CELL PRESS published article about in [Yue, Wen-Jun; Zhang, Cheng-Yuan; Yin, Liang] Univ Chinese Acad Sci, Chinese Acad Sci, CAS Key Lab Synthet Chem Nat Subst, Ctr Excellence Mol Synth,Shanghai Inst Organ Chem, 345 Lingling Rd, Shanghai 200032, Peoples R China in 2019, Cited 66. The Name is Benzoic anhydride. Through research, I have a further understanding and discovery of 93-97-0

Two catalytic asymmetric vinylogous aldol-type reactions of aldehydes with ally! phosphonate and allyl sulfone have been uncovered in good to high yields for the first time, The bulky ligand-(R)-DTBM-SEGPHOS-was found to be the key to perfectly control both regio- and enantioselectivities. Transformations of the vinylogous products (including Horner-Wadsworth-Emmons and Julia olefinations) were successfully realized by virtue of the phosphonate and sulfone moieties. Moreover, the present methodology was successfully applied in the asymmetric synthesis of natural products.

Application In Synthesis of Benzoic anhydride. Welcome to talk about 93-97-0, If you have any questions, you can contact Yue, WJ; Zhang, CY; Yin, L or send Email.

Reference:
Isothiazole – Wikipedia,
,Isothiazole – ScienceDirect.com

An article The Trifluoromethyl Group as a Bioisosteric Replacement of the Aliphatic Nitro Group in CB1 Receptor Positive Allosteric Modulators WOS:000469304500015 published article about INDOLES; CATALYST; DISCOVERY; ROUTE; MILD; PAIN in [Tseng, Chih-Chung; Zanato, Chiara; Massarenti, Chiara; Dall’Angelo, Sergio; Zanda, Matteo; Greig, Iain R.] Univ Aberdeen, Kosterlitz Ctr Therapeut, Aberdeen AB25 2ZD, Scotland; [Baillie, Gemma; Ross, Ruth A.] Univ Toronto, Dept Pharmacol & Toxicol, Toronto, ON M5S 1A8, Canada; [Donvito, Giulia; Mustafa, Mohammed A.; Juola, Sophie E.; Lichtman, Aron H.] Virginia Commonwealth Univ, Dept Pharmacol & Toxicol, Richmond, VA 23298 USA; [Lichtman, Aron H.] Virginia Commonwealth Univ, Dept Med Chem, Richmond, VA 23298 USA; [Zanda, Matteo] CNR, ICRM, Via Mancinelli 7, I-20131 Milan, Italy; [Harrison, William T. A.] Univ Aberdeen, Dept Chem, Aberdeen AB24 3UE, Scotland; [Zanda, Matteo] Loughborough Univ, Ctr Sensing & Imaging Sci, Sir David Davies Bldg, Loughborough LE11 3TU, Leics, England in 2019, Cited 37. The Name is Benzoic anhydride. Through research, I have a further understanding and discovery of 93-97-0. COA of Formula: C14H10O3

The first generation of CB1 positive allosteric modulators (e.g., ZCZ011) featured a 3-nitroalkyl-2-phenyl-indole structure. Although a small number of drugs include the nitro group, it is generally not regarded as being drug-like, and this is particularly true for aliphatic nitro groups. There are very few case studies where an appropriate bioisostere replaced a nitro group that had a direct role in binding. This may be indicative of the difficulty of replicating its binding interactions. Herein, we report the design and synthesis of ligands targeting the allosteric binding site on the CB, cannabinoid receptor, in which a CF3 group successfully replaced the aliphatic NO2. In general, the CF3-bearing compounds were more potent than their NO2 equivalents and also showed improved in vitro metabolic stability. The CF3 analogue (1) with the best balance of properties was selected for further pharmacological evaluation. Pilot in vivo studies showed that (+/-)-1 has similar activity to (+/-)-ZCZ011, with both showing promising efficacy in a mouse model of neuropathic pain.

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Reference:
Isothiazole – Wikipedia,
,Isothiazole – ScienceDirect.com