Category: 209911-63-7

Let¡¯s face it, organic chemistry can seem difficult to learn, Product Details of 209911-63-7, Especially from a beginner¡¯s point of view. Like 209911-63-7, Name is 4′-(Dibromomethyl)-[1,1′-biphenyl]-2-carbonitrile, molecular formula is isothiazole, belongs to isothiazole compound. In a document, author is Zhang, Xuqing, introducing its new discovery.

Discovery of an Isothiazole-Based Phenylpropanoic Acid GPR120 Agonist as a Development Candidate for Type 2 Diabetes

We have discovered a novel series of isothiazole-based phenylpropanoic acids as GPR120 agonists. Extensive structure activity relationship studies led to the discovery of a potent GPR120 agonist 4x, which displayed good EC50 values in both calcium and beta-arrestin assays. It also presented good pharmaceutical properties and a favorable PK profile. Moreover, it demonstrated in vivo antidiabetic activity in C57BL/6 DIO mice. Studies in WT and knockout DIO mice showed that it improved glucose handling during an OGTT via GPR120. Overall, 4x possessed promising antidiabetic effect and good safety profile to be a development candidate.

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

 

Electric Literature of 209911-63-7, The transformation of simple hydrocarbons into more complex and valuable products via catalytic C¨CH bond functionalisation has revolutionised modern synthetic chemistry. 209911-63-7, Name is 4′-(Dibromomethyl)-[1,1′-biphenyl]-2-carbonitrile, SMILES is N#CC1=CC=CC=C1C2=CC=C(C(Br)Br)C=C2, belongs to isothiazole compound. In a article, author is Amirhamzeh, Amirali, introduce new discover of the category.

Synthesis and docking study of diaryl-isothiazole and 1,2,3-thiadiazole derivatives as potential neuroprotective agents

Neuroinflammation has been implicated in pathophysiology of many neurodegenerative diseases. The p38 MAP kinase signaling pathway and COX-1 have active roles in initiation and perpetuation of neuroinflammatory process which have deteriorating effects on neurons. In order to develop new anti-neuroinflammatory compounds some 4-aryl-5-(methylthiophen-2-yl) isothiazoles and 5-aryl-4-(methylthiophen-2-yl)-1,2,3-thiadiazoles were synthesized. Docking studies have revealed that these structures could be potential mutual inhibitors of p38 alpha and COX-1 and could be considered for neuroprotective effects. In order to assess CNS penetrability of these compounds, a QSAR model of blood-brain barrier penetration has been developed and LogBB of compounds has been predicted. All compounds showed LogBB as greater than zero which indicates their potential CNS penetrability.

Electric Literature of 209911-63-7, Consequently, the presence of a catalyst will permit a system to reach equilibrium more quickly, but it has no effect on the position of the equilibrium as reflected in the value of its equilibrium constant.I hope my blog about 209911-63-7 is helpful to your research.

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

 

Synthetic Route of 209911-63-7, As an important bridge between the micro and macro material world, chemistry is one of the main methods and means for humans to understand and transform the material world. 209911-63-7, Name is 4′-(Dibromomethyl)-[1,1′-biphenyl]-2-carbonitrile, SMILES is N#CC1=CC=CC=C1C2=CC=C(C(Br)Br)C=C2, belongs to isothiazole compound. In a article, author is Jorgensen, Charlotte G., introduce new discover of the category.

Synthesis and pharmacology of glutamate receptor ligands: new isothiazole analogues of ibotenic acid

The naturally occurring heterocyclic amino acid ibotenic acid (Ibo) and the synthetic analogue thioibotenic acid (Thio-Ibo) possess interesting but dissimilar pharmacological activity at ionotropic and metabotropic glutamate receptors (iGluRs and mGluRs). Therefore, a series of Thio-Ibo analogues was synthesized. The synthesis included introduction of substituents by Suzuki and Grignard reactions on 4-halogenated 3-benzyloxyisothiazolols, reduction of the obtained alcohols, followed by introduction of the amino acid moiety by use of 2-(N-tert-butoxycarbonylimino) malonic acid diethyl ester. The obtained Thio-Ibo analogues ( 1, 2a- g) were characterized in functional assays on recombinant mGluRs and in receptor binding assays on native iGluRs. At mGluRs, the activity at Group II was retained for compounds with small substituents (2a – 2d), whereas the Group I and Group III receptor activities for all new compounds were lost. Detection of NMDA receptor affinity prompted further characterization, and two-electrode voltage-clamp recordings at recombinant NMDA receptor subtypes NR1/NR2A-D expressed in Xenopus oocytes were carried out for compounds with small substituents ( chloro, bromo, methyl or ethyl, compounds 2a – d). This series of Thio-Ibo analogues defines a structural threshold for NMDA receptor activation and reveals that the individual subtypes have different steric requirements for receptor activation. The compounds 2a and 2c are the first examples of agonists discriminating individual NMDA subtypes.

Synthetic Route of 209911-63-7, Each elementary reaction can be described in terms of its molecularity, the number of molecules that collide in that step. The slowest step in a reaction mechanism is the rate-determining step.you can also check out more blogs about 209911-63-7.

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

 

Synthetic Route of 209911-63-7, The transformation of simple hydrocarbons into more complex and valuable products via catalytic C¨CH bond functionalisation has revolutionised modern synthetic chemistry. 209911-63-7, Name is 4′-(Dibromomethyl)-[1,1′-biphenyl]-2-carbonitrile, SMILES is N#CC1=CC=CC=C1C2=CC=C(C(Br)Br)C=C2, belongs to isothiazole compound. In a article, author is Gedi, Vinayakumar, introduce new discover of the category.

Identification and characterization of inhibitors of Haemophilus influenzae acetohydroxyacid synthase

Acetohydroxyacid synthase (AHAS), a potential target for antimicrobial agents, catalyzes the first common step in the biosynthesis of branched-chain amino acids. The gene coding for the AHAS catalytic subunit from Haemophilus influenzae (Hi) was cloned, overexpressed in Escherichia coli, and purified. To identify new inhibitory scaffolds, we used a high-throughput screen to test 221 small diverse chemical compounds against Hi-AHAS. Compounds were selected for their ability to inhibit AHAS in vitro. The screen identified 3 compounds, each representing a structural class, as Hi-AHAS inhibitors with an IC(50) in the low micromolar range (4.4-14.6 mu M). The chemical scaffolds of the three compounds were oxa-1-thia-4-aza-cyclopenta[b]naphthalene (KHG25229), phenyl-2,3-dihydro-isothiazole (KHG25386), and phenyl-pyrrolidine-3-carboxylic acid phenylamide (KHG25056). Further, molecular docking of the two most potent chemicals, KHG25229 and KHG25386, in Hi-AHAS yielded binding energies of -10.41 and -9.21 kcal/mol, respectively. The binding modes were consistent with inhibition mechanisms, as both chemicals oriented outside the active site. As the need for novel antibiotic classes to combat drug resistant bacteria increases, screening compounds that act against Hi-AHAS may assist in the identification of potential new anti-Hi drugs. (C) 2011 Elsevier Inc. All rights reserved.

Synthetic Route of 209911-63-7, The reactant in an enzyme-catalyzed reaction is called a substrate. Enzyme inhibitors cause a decrease in the reaction rate of an enzyme-catalyzed reaction.I hope my blog about 209911-63-7 is helpful to your research.

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