Tag: M.W=300-400

Montgomery, Deanna; Anand, Jessica P.; Griggs, Nicholas W.; Fernandez, Thomas J.; Hartman, Joshua G.; Sanchez-Santiago, Ashley A.; Pogozheva, Irina D.; Traynor, John R.; Mosberg, Henry I. published the artcile< Novel dimethyltyrosine-tetrahydroisoquinoline peptidomimetics with aromatic tetrahydroisoquinoline substitutions show in vitro Kappa and Mu opioid receptor agonism>, HPLC of Formula: 893566-75-1, the main research area is dimethyltyrosine tetrahydroisoquinoline peptidomimetic synthesis opioid receptor agonist; peptidomimetic opioid structure activity mol docking cocain addiction; bromination quinoline substitution protection Suzuki coupling; cocaine addiction; dimethyltyrosine−tetrahydroisoquinoline; multifunctional ligands; opioids; peptidomimetics; synthesis.

The dimethyltyrosine-tetrahydroisoquinoline (Dmt-Tiq) scaffold was originally developed in the production of selective delta opioid receptor (DOR) antagonists. Installation of a 7-benzyl pendant on the tetrahydroisoquinoline core of this classic opioid scaffold introduced kappa opioid receptor (KOR) agonism. Further modification of this pendant resulted in retention of KOR agonism and the addition of mu opioid receptor (MOR) partial agonism, a bifunctional profile with potential to be used in the treatment of cocaine addiction.

ACS Chemical Neuroscience published new progress about Bromination. 893566-75-1 belongs to class tetrahydroisoquinoline, and the molecular formula is C14H18BrNO2, HPLC of Formula: 893566-75-1.

Referemce:
Tetrahydroisoquinoline – Wikipedia,
1,2,3,4-Tetrahydroisoquinoline | C9H11N – PubChem

Montgomery, Deanna; Anand, Jessica P.; Griggs, Nicholas W.; Fernandez, Thomas J.; Hartman, Joshua G.; Sanchez-Santiago, Ashley A.; Pogozheva, Irina D.; Traynor, John R.; Mosberg, Henry I. published the artcile< Novel dimethyltyrosine-tetrahydroisoquinoline peptidomimetics with aromatic tetrahydroisoquinoline substitutions show in vitro Kappa and Mu opioid receptor agonism>, HPLC of Formula: 893566-75-1, the main research area is dimethyltyrosine tetrahydroisoquinoline peptidomimetic synthesis opioid receptor agonist; peptidomimetic opioid structure activity mol docking cocain addiction; bromination quinoline substitution protection Suzuki coupling; cocaine addiction; dimethyltyrosine−tetrahydroisoquinoline; multifunctional ligands; opioids; peptidomimetics; synthesis.

The dimethyltyrosine-tetrahydroisoquinoline (Dmt-Tiq) scaffold was originally developed in the production of selective delta opioid receptor (DOR) antagonists. Installation of a 7-benzyl pendant on the tetrahydroisoquinoline core of this classic opioid scaffold introduced kappa opioid receptor (KOR) agonism. Further modification of this pendant resulted in retention of KOR agonism and the addition of mu opioid receptor (MOR) partial agonism, a bifunctional profile with potential to be used in the treatment of cocaine addiction.

ACS Chemical Neuroscience published new progress about Bromination. 893566-75-1 belongs to class tetrahydroisoquinoline, and the molecular formula is C14H18BrNO2, HPLC of Formula: 893566-75-1.

Referemce:
Tetrahydroisoquinoline – Wikipedia,
1,2,3,4-Tetrahydroisoquinoline | C9H11N – PubChem

Malamas, Michael S.; Lamani, Manjunath; Farah, Shrouq I.; Mohammad, Khadijah A.; Miyabe, Christina Yume; Rajarshi, Girija; Wu, Simiao; Zvonok, Nikolai; Chandrashekhar, Honrao; Wood, JodiAnne; Makriyannis, Alexandros published the artcile< Design and Synthesis of Highly Potent and Specific ABHD6 Inhibitors>, Category: tetrahydroisoquinoline, the main research area is design synthesis biol activity ABHD6 inhibitor SAR; monoacylglycerol lipase; neuroinflammation.; neuroprotection; α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid; α/β-hydrolase domain containing 6.

Fine-tuning than complete disruption of 2-arachidonoylglycerol (2-AG) metabolism in the brain represents a promising pharmacol. approach to limit potential untoward effects associated with complete blockade of monoacylglycerol lipase (MGL), the primary hydrolase of 2-AG. This could be achieved through a/b-hydrolase domain containing 6 (ABHD6) inhibition, which will provide a smaller and safer contribution to 2-AG regulation in the brain. Pharmacol. studies with ABHD6 inhibitors have recently been reported, where modulation of ABHD6 activity either through CB1R-dependent or CB1R-independent processes showed promise in preclin. models of epilepsy, neuropathic pain and inflammation. Furthermore in the periphery, ABHD6 modulates 2-AG and other fatty acid monoacylglycerols (MAGs) and is implicated in Type-2 diabetes, metabolic syndrome and potentially other diseases. Herein, we report the discovery of single-digit nanomolar potent and highly specific ABHD6 inhibitors with >1000-fold selectivity against MGL and FAAH. The new ABHD6 inhibitors provide early leads to develop therapeutics for neuroprotection and the treatment of inflammation and diabetes.

ChemMedChem published new progress about Brain. 893566-75-1 belongs to class tetrahydroisoquinoline, and the molecular formula is C14H18BrNO2, Category: tetrahydroisoquinoline.

Referemce:
Tetrahydroisoquinoline – Wikipedia,
1,2,3,4-Tetrahydroisoquinoline | C9H11N – PubChem

Lee, Wongyu; Kim, Dongwook; Seo, Sangwon; Chang, Sukbok published the artcile< Photoinduced α-C-H Amination of Cyclic Amine Scaffolds Enabled by Polar-Radical Relay>, Product Details of C14H18BrNO2, the main research area is cyclic amine photoinduced amination regioselective polar radical relay; Amination; Amines; Radicals; Reaction Mechanisms; Sustainability.

Herein, a polar-radical relay strategy for α-C-H amination of cyclic amines with N-chloro-N-sodio-carbamates is reported. The relay is initiated by in situ generation of a cyclic iminium intermediate using N-iodosuccinimide oxidant as an initiator, which then operates through a series of polar (addition and elimination) and radical (homolysis, hydrogen- and halogen atom transfer) reactions to enable the challenging C-N bond formation in a controlled manner. A broad range of α-amino cyclic amines were readily accessed with excellent regioselectivity, and the superb applicability was further demonstrated by functionalization of biol. relevant compounds

Angewandte Chemie, International Edition published new progress about Aminals Role: SPN (Synthetic Preparation), PREP (Preparation). 893566-75-1 belongs to class tetrahydroisoquinoline, and the molecular formula is C14H18BrNO2, Product Details of C14H18BrNO2.

Referemce:
Tetrahydroisoquinoline – Wikipedia,
1,2,3,4-Tetrahydroisoquinoline | C9H11N – PubChem

Wang, Le; Doherty, George A.; Judd, Andrew S.; Tao, Zhi-Fu; Hansen, T. Matthew; Frey, Robin R.; Song, Xiaohong; Bruncko, Milan; Kunzer, Aaron R.; Wang, Xilu; Wendt, Michael D.; Flygare, John A.; Catron, Nathaniel D.; Judge, Russell A.; Park, Chang H.; Shekhar, Shashank; Phillips, Darren C.; Nimmer, Paul; Smith, Morey L.; Tahir, Stephen K.; Xiao, Yu; Xue, John; Zhang, Haichao; Le, Phuong N.; Mitten, Michael J.; Boghaert, Erwin R.; Gao, Wenqing; Kovar, Peter; Choo, Edna F.; Diaz, Dolores; Fairbrother, Wayne J.; Elmore, Steven W.; Sampath, Deepak; Leverson, Joel D.; Souers, Andrew James published the artcile< Discovery of A-1331852, a First-in-Class, Potent, and Orally-Bioavailable BCL-XL Inhibitor>, Quality Control of 893566-75-1, the main research area is tumor BCLXL BCL2 apoptosis A1155463 structure based drug design.

Herein we describe the discovery of A-1331852(I), a first-in-class orally active BCL-XL inhibitor that selectively and potently induces apoptosis in BCL-XL dependent tumor cells. This mol. was generated by re-engineering our previously reported BCL-XL inhibitor A-1155463 using structure-based drug design. Key design elements included rigidification of the A-1155463 pharmacophore and introduction of sp3-rich moieties capable of generating highly productive interactions within the key P4 pocket of BCL-XL. A-1331852 has since been used as a critical tool mol. for further exploring BCL-2 family protein biol., while also representing an attractive entry into a drug discovery program.

ACS Medicinal Chemistry Letters published new progress about Antitumor agents. 893566-75-1 belongs to class tetrahydroisoquinoline, and the molecular formula is C14H18BrNO2, Quality Control of 893566-75-1.

Referemce:
Tetrahydroisoquinoline – Wikipedia,
1,2,3,4-Tetrahydroisoquinoline | C9H11N – PubChem

Malamas, Michael S.; Lamani, Manjunath; Farah, Shrouq I.; Mohammad, Khadijah A.; Miyabe, Christina Yume; Rajarshi, Girija; Wu, Simiao; Zvonok, Nikolai; Chandrashekhar, Honrao; Wood, JodiAnne; Makriyannis, Alexandros published the artcile< Design and Synthesis of Highly Potent and Specific ABHD6 Inhibitors>, Related Products of 893566-75-1, the main research area is design synthesis biol activity ABHD6 inhibitor SAR; monoacylglycerol lipase; neuroinflammation.; neuroprotection; α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid; α/β-hydrolase domain containing 6.

Fine-tuning than complete disruption of 2-arachidonoylglycerol (2-AG) metabolism in the brain represents a promising pharmacol. approach to limit potential untoward effects associated with complete blockade of monoacylglycerol lipase (MGL), the primary hydrolase of 2-AG. This could be achieved through a/b-hydrolase domain containing 6 (ABHD6) inhibition, which will provide a smaller and safer contribution to 2-AG regulation in the brain. Pharmacol. studies with ABHD6 inhibitors have recently been reported, where modulation of ABHD6 activity either through CB1R-dependent or CB1R-independent processes showed promise in preclin. models of epilepsy, neuropathic pain and inflammation. Furthermore in the periphery, ABHD6 modulates 2-AG and other fatty acid monoacylglycerols (MAGs) and is implicated in Type-2 diabetes, metabolic syndrome and potentially other diseases. Herein, we report the discovery of single-digit nanomolar potent and highly specific ABHD6 inhibitors with >1000-fold selectivity against MGL and FAAH. The new ABHD6 inhibitors provide early leads to develop therapeutics for neuroprotection and the treatment of inflammation and diabetes.

ChemMedChem published new progress about Brain. 893566-75-1 belongs to class tetrahydroisoquinoline, and the molecular formula is C14H18BrNO2, Related Products of 893566-75-1.

Referemce:
Tetrahydroisoquinoline – Wikipedia,
1,2,3,4-Tetrahydroisoquinoline | C9H11N – PubChem

Lee, Wongyu; Kim, Dongwook; Seo, Sangwon; Chang, Sukbok published the artcile< Photoinduced α-C-H Amination of Cyclic Amine Scaffolds Enabled by Polar-Radical Relay>, Electric Literature of 893566-75-1, the main research area is cyclic amine photoinduced amination regioselective polar radical relay; Amination; Amines; Radicals; Reaction Mechanisms; Sustainability.

Herein, a polar-radical relay strategy for α-C-H amination of cyclic amines with N-chloro-N-sodio-carbamates is reported. The relay is initiated by in situ generation of a cyclic iminium intermediate using N-iodosuccinimide oxidant as an initiator, which then operates through a series of polar (addition and elimination) and radical (homolysis, hydrogen- and halogen atom transfer) reactions to enable the challenging C-N bond formation in a controlled manner. A broad range of α-amino cyclic amines were readily accessed with excellent regioselectivity, and the superb applicability was further demonstrated by functionalization of biol. relevant compounds

Angewandte Chemie, International Edition published new progress about Aminals Role: SPN (Synthetic Preparation), PREP (Preparation). 893566-75-1 belongs to class tetrahydroisoquinoline, and the molecular formula is C14H18BrNO2, Electric Literature of 893566-75-1.

Referemce:
Tetrahydroisoquinoline – Wikipedia,
1,2,3,4-Tetrahydroisoquinoline | C9H11N – PubChem