Category: 175205-82-0

Discovery and optimization of adamantyl carbamate inhibitors of 11灏?HSD1 was written by Tice, Colin M.;Zhao, Wei;Krosky, Paula M.;Kruk, Barbara A.;Berbaum, Jennifer;Johnson, Judith A.;Bukhtiyarov, Yuri;Panemangalore, Reshma;Scott, Boyd B.;Zhao, Yi;Bruno, Joseph G.;Howard, Lamont;Togias, Jennifer;Ye, Yuan-Jie;Singh, Suresh B.;McKeever, Brian M.;Lindblom, Peter R.;Guo, Joan;Guo, Rong;Nar, Herbert;Schuler-Metz, Annette;Gregg, Richard E.;Leftheris, Katerina;Harrison, Richard K.;McGeehan, Gerard M.;Zhuang, Linghang;Claremon, David A.. And the article was included in Bioorganic & Medicinal Chemistry Letters in 2010.Category: pyridine-derivatives This article mentions the following:

Synthesis of 2-adamantyl carbamate derivatives of piperidines and pyrrolidines led to the discovery of 2-adamantanyl (3R)-3-tert.-butoxycarbonylaminopyrrolidine-1-carboxylate with an IC₅₀ of 15.2 nM against human 11灏?HSD1 in adipocytes. Optimization for increased adipocyte potency, metabolic stability and selectivity afforded 1-carbamoyladmanatan-4-yl (3R)-(3-cyano- and 5-cyanopyrdinylamino)pyrrolidine-1-carboxylate, both of which were >25% orally bioavailable in rat. In the experiment, the researchers used many compounds, for example, 2-Bromo-3-(trifluoromethyl)pyridine (cas: 175205-82-0Category: pyridine-derivatives).

2-Bromo-3-(trifluoromethyl)pyridine (cas: 175205-82-0) belongs to pyridine derivatives. Pyridine has a conjugated system of six 锜?electrons that are delocalized over the ring. The molecule is planar and, thus, follows the H鐪塩kel criteria for aromatic systems. Pyridine groups exist in countless molecules, and their applications include catalysis, drug design, molecular recognition, and natural product synthesis.Category: pyridine-derivatives

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Enantioselective synthesis of trifluoromethyl substituted piperidines with multiple stereogenic centers via hydrogenation of pyridinium hydrochlorides was written by Chen, Mu-Wang;Ye, Zhi-Shi;Chen, Zhang-Pei;Wu, Bo;Zhou, Yong-Gui. And the article was included in Organic Chemistry Frontiers in 2015.Computed Properties of C6H3BrF3N This article mentions the following:

An enantioselective iridium-catalyzed hydrogenation of trifluoromethyl substituted pyridinium hydrochlorides is described. Introduction of a trifluoromethyl group increases the reactivity due to the electron-withdrawing effect. Three stereogenic centers could be generated in one operation. This methodol. provides a convenient route to chiral poly-substituted piperidines I (R = Me, Et; Ar = Ph, 4-MeC₆H₄, 4-MeOC₆H₄, 2-naphthyl, etc.) and II (Ar = Ph, 4-CF₃C₆H₄, 3,5-F₂C₆H₃, 1-naphthyl) with up to 90% ee. In the experiment, the researchers used many compounds, for example, 2-Bromo-3-(trifluoromethyl)pyridine (cas: 175205-82-0Computed Properties of C6H3BrF3N).

2-Bromo-3-(trifluoromethyl)pyridine (cas: 175205-82-0) belongs to pyridine derivatives. Pyridines are an important class of heterocycles and occur in polysubstituted forms in many naturally occurring biologically active compounds, drug molecules and chiral ligands. Pyridine, its benzo and pyridine-based compounds play diverse roles in organic chemistry. Pyridine-based materials are valued for their optical and physical properties as well as their medical potential. Computed Properties of C6H3BrF3N

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Piperazine Sulfonamides as Potent, Selective, and Orally Available 11灏?Hydroxysteroid Dehydrogenase Type 1 Inhibitors with Efficacy in the Rat Cortisone-Induced Hyperinsulinemia Model was written by Xiang, Jason;Wan, Zhao-Kui;Li, Huan-Qiu;Ipek, Manus;Binnun, Eva;Nunez, Jill;Chen, Lihren;McKew, John C.;Mansour, Tarek S.;Xu, Xin;Suri, Vipin;Tam, May;Xing, Yuzhe;Li, Xiangping;Hahm, Seung;Tobin, James;Saiah, Eddine. And the article was included in Journal of Medicinal Chemistry in 2008.HPLC of Formula: 175205-82-0 This article mentions the following:

11灏?Hydroxysteroid dehydrogenase type 1 (11灏?HSD1) is the enzyme that converts cortisone to cortisol. Evidence suggests that selective inhibition of 11灏?HSD1 could treat diabetes and metabolic syndrome. Presented herein are the synthesis, structure-activity relationship, and in vivo evaluation of piperazine sulfonamides as 11灏?HSD1 inhibitors. Through modification of our initial lead I (R¹ = 3,4-Cl₂, R² = H, X = N), we have identified potent and selective 11灏?HSD1 inhibitors such as I [R¹ = 3-(1,2,4-triazol-1-yl), 3-(MeO₂CCMe₂O), R² = F, X = C] with good pharmacokinetic properties. In the experiment, the researchers used many compounds, for example, 2-Bromo-3-(trifluoromethyl)pyridine (cas: 175205-82-0HPLC of Formula: 175205-82-0).

2-Bromo-3-(trifluoromethyl)pyridine (cas: 175205-82-0) belongs to pyridine derivatives. In contrast to benzene, Pyridine’s electron density is not evenly distributed over the ring, reflecting the negative inductive effect of the nitrogen atom. Pyridine groups exist in countless molecules, and their applications include catalysis, drug design, molecular recognition, and natural product synthesis.HPLC of Formula: 175205-82-0

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Discovery of vinylcycloalkyl-substituted benzimidazole TRPM8 antagonists effective in the treatment of cold allodynia was written by Calvo, Raul R.;Meegalla, Sanath K.;Parks, Daniel J.;Parsons, William H.;Ballentine, Shelley K.;Lubin, Mary Lou;Schneider, Craig;Colburn, Raymond W.;Flores, Christopher M.;Player, Mark R.. And the article was included in Bioorganic & Medicinal Chemistry Letters in 2012.Related Products of 175205-82-0 This article mentions the following:

Thermosensitive transient receptor potential melastatin 8 (TRPM8) antagonists are considered to be potential therapeutic agents for the treatment of cold hypersensitivity. The discovery of a new class of TRPM8 antagonists that shows in vivo efficacy in the rat chronic constriction injury (CCI)-induced model of neuropathic pain is described. In the experiment, the researchers used many compounds, for example, 2-Bromo-3-(trifluoromethyl)pyridine (cas: 175205-82-0Related Products of 175205-82-0).

2-Bromo-3-(trifluoromethyl)pyridine (cas: 175205-82-0) belongs to pyridine derivatives. Pyridine is diamagnetic and has a diamagnetic susceptibility of 閳?8.7 鑴?10閳? cm3璺痬ol閳?.The molecular electric dipole moment is 2.2 debyes. The standard enthalpy of formation is 100.2 kJ璺痬ol閳? in the liquid phase and 140.4 kJ璺痬ol閳? in the gas phase. Many analogues of pyridine are known where N is replaced by other heteroatoms . Substitution of one C閳ユ弻 in pyridine with a second N gives rise to the diazine heterocycles (C4H4N2), with the names pyridazine, pyrimidine, and pyrazine.Related Products of 175205-82-0

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Propionamide Derivatives as Dual 渭-Opioid Receptor Agonists and 蟽₁ Receptor Antagonists for the Treatment of Pain was written by Garcia, Monica;Llorente, Virginia;Garriga, Lourdes;Christmann, Ute;Rodriguez-Escrich, Sergi;Virgili, Marina;Fernandez, Begona;Bordas, Magda;Ayet, Eva;Burgueno, Javier;Pujol, Marta;Dordal, Albert;Portillo-Salido, Enrique;Gris, Georgia;Vela, Jose Miguel;Almansa, Carmen. And the article was included in Journal of Medicinal Chemistry in 2021.SDS of cas: 175205-82-0 This article mentions the following:

A new series of propionamide derivatives was developed as dual 渭-opioid receptor agonists and 蟽₁ receptor antagonists. Modification of a high-throughput screening hit originated a series of piperazinylcycloalkylmethyl propionamides, which were explored to overcome the challenge of achieving balanced dual activity and convenient drug-like properties. The lead compound identified, 18g (I), showed good analgesic effects in several animal models of both acute (paw pressure) and chronic (partial sciatic nerve ligation) pain, with reduced gastrointestinal effects in comparison with oxycodone. In the experiment, the researchers used many compounds, for example, 2-Bromo-3-(trifluoromethyl)pyridine (cas: 175205-82-0SDS of cas: 175205-82-0).

2-Bromo-3-(trifluoromethyl)pyridine (cas: 175205-82-0) belongs to pyridine derivatives. Pyridine has a dipole moment and a weaker resonant stabilization than benzene (resonance energy 117 kJ路mol鈭? in pyridine vs. 150 kJ路mol鈭? in benzene). Pyridine groups exist in countless molecules, and their applications include catalysis, drug design, molecular recognition, and natural product synthesis.SDS of cas: 175205-82-0

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Discovery of a biarylamide series of potent, state-dependent Na_V1.7 inhibitors was written by Schenkel, Laurie B.;DiMauro, Erin F.;Nguyen, Hanh N.;Chakka, Nagasree;Du, Bingfan;Foti, Robert S.;Guzman-Perez, Angel;Jarosh, Michael;La, Daniel S.;Ligutti, Joseph;Milgram, Benjamin C.;Moyer, Bryan D.;Peterson, Emily A.;Roberts, John;Yu, Violeta L.;Weiss, Matthew M.. And the article was included in Bioorganic & Medicinal Chemistry Letters in 2017.Electric Literature of C6H3BrF3N This article mentions the following:

State-dependent Na_V1.7 inhibitors. The Na_V1.7 ion channel has garnered considerable attention as a target for the treatment of pain. Herein we detail the discovery and structure-activity relationships of a novel series of biaryl amides. Optimization led to the identification of several state-dependent, potent and metabolically stable inhibitors which demonstrated promising levels of selectivity over Na_V1.5 and good rat pharmacokinetics. Compound I, which demonstrated preferential inhibition of a slow inactivated state of Na_V1.7, was advanced into a rat formalin study where upon reaching unbound drug levels several fold over the rat Na_V1.7 IC₅₀ it failed to demonstrate a robust reduction in nociceptive behavior. In the experiment, the researchers used many compounds, for example, 2-Bromo-3-(trifluoromethyl)pyridine (cas: 175205-82-0Electric Literature of C6H3BrF3N).

2-Bromo-3-(trifluoromethyl)pyridine (cas: 175205-82-0) belongs to pyridine derivatives. The pyridine ring occurs in many important compounds, including agrochemicals, pharmaceuticals, and vitamins. Reduced pyridines, namely tetrahydropyridines, dihydropyridines and piperidines, are found in numerous natural and synthetic compounds. The synthesis and reactivity of these compounds have often been driven by the fact many of these compounds have interesting and unique pharmacological properties. Electric Literature of C6H3BrF3N

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

A Base-Promoted Reductive Coupling Platform for the Divergent Defluorofunctionalization of Trifluoromethylarenes was written by Wright, Shawn E.;Bandar, Jeffrey S.. And the article was included in Journal of the American Chemical Society in 2022.Product Details of 175205-82-0 This article mentions the following:

Trifluoromethylarenes ArCF₃ [Ar = di-Et phenylphosphonate, 3-(benzyloxy)-5-(trifluoromethyl)phenyl, 3-fluoropyridin-2-yl, etc.] reductive coupling method that dramatically expands the scope of difluorobenzylic substructures ArC(F₂)R [R = (hydroxyimino)methyl, (dimethylamino)[(trimethylsilyl)oxy]methyl, morpholin-4-yl[(trimethylsilyl)oxy]methyl, etc.] accessible via C-F bond functionalization was reported. Catalytic quantities of a Lewis base, in conjunction with a disilane reagent in formamide solvent, led to the replacement of a single trifluoromethyl fluorine atom with a silylated hemiaminal functional group. The reaction proceeds through a difluorobenzyl silane intermediate that can also be isolated. Together, these defluorinated products are shown to provide rapid access to over 20 unique difluoroalkylarene scaffolds. In the experiment, the researchers used many compounds, for example, 2-Bromo-3-(trifluoromethyl)pyridine (cas: 175205-82-0Product Details of 175205-82-0).

2-Bromo-3-(trifluoromethyl)pyridine (cas: 175205-82-0) belongs to pyridine derivatives. Pyridine has a dipole moment and a weaker resonant stabilization than benzene (resonance energy 117 kJ·mol−1 in pyridine vs. 150 kJ·mol−1 in benzene). Pyridine groups exist in countless molecules, and their applications include catalysis, drug design, molecular recognition, and natural product synthesis.Product Details of 175205-82-0

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

An efficient coupling of N-tosylhydrazones with 2-halopyridines: synthesis of 2-α-styrylpyridines endowed with antitumor activity was written by Lawson, Marie;Hamze, Abdallah;Peyrat, Jean-Francois;Bignon, Jerome;Dubois, Joelle;Brion, Jean-Daniel;Alami, Mouad. And the article was included in Organic & Biomolecular Chemistry in 2013.Application of 175205-82-0 This article mentions the following:

The synthesis of 2-α-styrylpyridines has been carried out by using the coupling of polyoxygenated N-tosylhydrazones with various 2-halopyridines. We demonstrated that the use of a catalytic amount of PdCl₂(MeCN)₂ in combination with a bidentate ferrocene DPPF or a monodentate alkyl phosphine ^tBu₂MeP-HBF₄ constitutes an efficient protocol for this coupling, providing 2-α-styrylpyridines in satisfactory to good yields. Among evaluated, compound I was found to exhibit excellent antiproliferative and antimitotic activities comparable to that of the reference compound isoCA-4. In the experiment, the researchers used many compounds, for example, 2-Bromo-3-(trifluoromethyl)pyridine (cas: 175205-82-0Application of 175205-82-0).

2-Bromo-3-(trifluoromethyl)pyridine (cas: 175205-82-0) belongs to pyridine derivatives. Pyridine has a conjugated system of six π electrons that are delocalized over the ring. The molecule is planar and, thus, follows the Hückel criteria for aromatic systems. Many analogues of pyridine are known where N is replaced by other heteroatoms . Substitution of one C–H in pyridine with a second N gives rise to the diazine heterocycles (C4H4N2), with the names pyridazine, pyrimidine, and pyrazine.Application of 175205-82-0

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Propionamide Derivatives as Dual μ-Opioid Receptor Agonists and σ₁ Receptor Antagonists for the Treatment of Pain was written by Garcia, Monica;Llorente, Virginia;Garriga, Lourdes;Christmann, Ute;Rodriguez-Escrich, Sergi;Virgili, Marina;Fernandez, Begona;Bordas, Magda;Ayet, Eva;Burgueno, Javier;Pujol, Marta;Dordal, Albert;Portillo-Salido, Enrique;Gris, Georgia;Vela, Jose Miguel;Almansa, Carmen. And the article was included in Journal of Medicinal Chemistry in 2021.SDS of cas: 175205-82-0 This article mentions the following:

A new series of propionamide derivatives was developed as dual μ-opioid receptor agonists and σ₁ receptor antagonists. Modification of a high-throughput screening hit originated a series of piperazinylcycloalkylmethyl propionamides, which were explored to overcome the challenge of achieving balanced dual activity and convenient drug-like properties. The lead compound identified, 18g (I), showed good analgesic effects in several animal models of both acute (paw pressure) and chronic (partial sciatic nerve ligation) pain, with reduced gastrointestinal effects in comparison with oxycodone. In the experiment, the researchers used many compounds, for example, 2-Bromo-3-(trifluoromethyl)pyridine (cas: 175205-82-0SDS of cas: 175205-82-0).

2-Bromo-3-(trifluoromethyl)pyridine (cas: 175205-82-0) belongs to pyridine derivatives. Pyridine has a dipole moment and a weaker resonant stabilization than benzene (resonance energy 117 kJ·mol−1 in pyridine vs. 150 kJ·mol−1 in benzene). Pyridine groups exist in countless molecules, and their applications include catalysis, drug design, molecular recognition, and natural product synthesis.SDS of cas: 175205-82-0

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Cobalt-Catalyzed Cross-Coupling Reactions of Arylboronic Esters and Aryl Halides was written by Duong, Hung A.;Wu, Wenqin;Teo, Yu-Yuan. And the article was included in Organometallics in 2017.Reference of 175205-82-0 This article mentions the following:

An efficient cobalt catalyst system for the Suzuki-Miyaura cross-coupling reaction of arylboronic esters and aryl halides has been identified. In the presence of cobalt(II)/terpyridine catalyst and potassium methoxide, a diverse array of (hetero)biaryls have been prepared in moderate to excellent yields. In the experiment, the researchers used many compounds, for example, 2-Bromo-3-(trifluoromethyl)pyridine (cas: 175205-82-0Reference of 175205-82-0).

2-Bromo-3-(trifluoromethyl)pyridine (cas: 175205-82-0) belongs to pyridine derivatives. The pyridine ring occurs in many important compounds, including agrochemicals, pharmaceuticals, and vitamins. Many analogues of pyridine are known where N is replaced by other heteroatoms . Substitution of one C–H in pyridine with a second N gives rise to the diazine heterocycles (C4H4N2), with the names pyridazine, pyrimidine, and pyrazine.Reference of 175205-82-0

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem