Category: 859833-21-9

Ouach, Aziz published the artcileBis(het)aryl-1,2,3-triazole quinuclidines as α7 nicotinic acetylcholine receptor ligands: Synthesis, structure affinity relationships, agonism activity, [¹⁸F]-radiolabeling and PET study in rats, Recommanded Product: 1-(3-(4,4,5,5-Tetramethyl-1,3,2-dioxaborolan-2-yl)benzyl)piperidine, the publication is European Journal of Medicinal Chemistry (2019), 449-469, database is CAplus and MEDLINE.

In this paper we describe the design and synthesis of bis(Het)Aryl-1,2,3-triazole quinuclidine α7R ligands using an efficient three-step sequence including a Suzuki-Miyaura cross coupling reaction with com. available and home-made boron derivatives The exploration of SAR required the preparation of uncommon boron derivatives Forty final drugs were tested for their ability to bind the target and nine of them exhibited Ki values below nanomolar concentrations The best scores were always obtained when the 5-phenyl-2-thiophenyl core was attached to the triazole. The selectivity of these compounds towards the nicotinic α4β2 and serotoninergic 5HT3 receptors was assessed and their brain penetration was quantified by the preparation and in vivo evaluation of two [¹⁸F] radiolabeled derivatives It can be expected from our results that some of these compounds will be suitable for further developments and will have effects on cognitive disorders.

European Journal of Medicinal Chemistry published new progress about 859833-21-9. 859833-21-9 belongs to piperidines, auxiliary class Piperidine,Boronic acid and ester,Benzene,Boronic Acids,Boronate Esters, name is 1-(3-(4,4,5,5-Tetramethyl-1,3,2-dioxaborolan-2-yl)benzyl)piperidine, and the molecular formula is C18H28BNO2, Recommanded Product: 1-(3-(4,4,5,5-Tetramethyl-1,3,2-dioxaborolan-2-yl)benzyl)piperidine.

Referemce:
https://en.wikipedia.org/wiki/Piperidine,
Piperidine | C5H11N – PubChem

Patel, Gautam published the artcileKinase Scaffold Repurposing for Neglected Disease Drug Discovery: Discovery of an Efficacious, Lapatanib-Derived Lead Compound for Trypanosomiasis, Name: 1-(3-(4,4,5,5-Tetramethyl-1,3,2-dioxaborolan-2-yl)benzyl)piperidine, the publication is Journal of Medicinal Chemistry (2013), 56(10), 3820-3832, database is CAplus and MEDLINE.

Lapatinib analogs such as I (X = O, CH₂) were prepared as trypanocidal agents for use as lead compounds in the development of treatments for human African trypanosomiasis which do not require i.v. administration. Lapatinib was previously shown to kill T. brucei with low micromolar EC₅₀ values; analogs replacing the methylfurylquinazoline moiety with a heteroarylsulfonylphenylquinazolinyl moiety were prepared and tested against both T. brucei and human hepatocarcinoma cells. 4-Anilinoquinazolines, particularly I (X = O) (NEU617), were found to be highly potent and orally bioavailable inhibitors of trypanosome replication. I (X = O) blocks duplication of the kinetoplast and arrests cytokinesis in T. brucei, which may make it useful as a chem. tool for studying regulation of the trypanosome cell cycle.

Journal of Medicinal Chemistry published new progress about 859833-21-9. 859833-21-9 belongs to piperidines, auxiliary class Piperidine,Boronic acid and ester,Benzene,Boronic Acids,Boronate Esters, name is 1-(3-(4,4,5,5-Tetramethyl-1,3,2-dioxaborolan-2-yl)benzyl)piperidine, and the molecular formula is C18H28BNO2, Name: 1-(3-(4,4,5,5-Tetramethyl-1,3,2-dioxaborolan-2-yl)benzyl)piperidine.

Referemce:
https://en.wikipedia.org/wiki/Piperidine,
Piperidine | C5H11N – PubChem