Omran, Anahid published the artcileSynthesis of 3-(3-hydroxyphenyl)pyrrolidine dopamine D3 receptor ligands with extended functionality for probing the secondary binding pocket, Category: alcohols-buliding-blocks, the publication is Bioorganic & Medicinal Chemistry Letters (2018), 28(10), 1897-1902, database is CAplus and MEDLINE.
A series of 3-(3-hydroxyphenyl)pyrrolidine analogs which incorporate N-alkyl groups and N-butylamide-linked benzamide functionality were synthesized and their in vitro binding affinities at human dopamine receptors were evaluated. The authors’ ligand design strategy was to take the 3-(3-hydroxyphenyl)pyrrolidine scaffold and extend functionality from the orthosteric binding site to the secondary binding pocket for enhancing affinity and selectivity for the D3 receptor. The N-alkyl analogs constitute a homologous series from N-pentyl to N-decyl to probe the length/bulk tolerance of the secondary binding pocket of the D3 receptor. Enantiomeric 3-(3-hydroxyphenyl)pyrrolidine analogs were also prepared to test the chirality preference of the orthosteric binding site for this scaffold. Benzamide analogs were prepared to enhance affinity and/or selectivity based upon the results of the homologous series.
Bioorganic & Medicinal Chemistry Letters published new progress about 6346-09-4. 6346-09-4 belongs to alcohols-buliding-blocks, auxiliary class Amine,Aliphatic hydrocarbon chain,Ether, name is 4,4-Diethoxybutan-1-amine, and the molecular formula is C8H19NO2, Category: alcohols-buliding-blocks.
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