Piperazinyl Bicyclic Derivatives as Selective Ligands of the α2δ-1 Subunit of Voltage-Gated Calcium Channels was written by Fernandez, Ariadna;Diaz, Jose Luis;Garcia, Monica;Rodriguez-Escrich, Sergi;Lorente, Adriana;Enrech, Raquel;Dordal, Albert;Portillo-Salido, Enrique;Porras, Monica;Fernandez, Begona;Reinoso, Raquel F.;Vela, Jose Miguel;Almansa, Carmen. And the article was included in ACS Medicinal Chemistry Letters in 2021.Product Details of 109-85-3 The following contents are mentioned in the article:
The synthesis and pharmacol. activities of a new series of piperazinyl quinazolin-4-(3H)-one derivatives I [R1 = H, 5-Br, 6-(4-pyridinyl), 8-Br, etc.; R2 = 2-methoxyethyl, benzyl, 2-furylmethyl, etc.; R3 = H, Me, Pr, n-Bu, etc.; R4 = piperazin-1-yl, (3R,5S)-3,5-dimethylpiperazin-1-yl, (S)-3-methylpiperazin-1-yl, etc.] acting toward the α2δ-1 subunit of voltage-gated calcium channels (Cavα2δ-1) were reported. Different positions of a micromolar HTS hit were explored, and best activities were obtained for compounds I containing a small alkyl group in position 3 of the quinazolin-4-(3H)-one scaffold and a 3-methyl-piperazin-1-yl- or 3,5-dimethyl-piperazin-1-yl-Bu group in position 2. The activity was shown to reside in the R enantiomer of the chain in position 2, and several eutomers reached single digit nanomolar affinities. Final modification of the central scaffold to reduce lipophilicity provided the pyrido[4,3-d]pyrimidin-4(3H)-one II, which showed high selectivity for Cavα2δ-1 vs. Cavα2δ-2, probably linked to its improved analgesic efficacy-safety ratio in mice over pregabalin. This study involved multiple reactions and reactants, such as 2-Methoxyethylamine (cas: 109-85-3Product Details of 109-85-3).
2-Methoxyethylamine (cas: 109-85-3) belongs to ethers. Volatile esters with characteristic odours are used in synthetic flavours, perfumes, and cosmetics. Certain volatile esters are used as solvents for lacquers, paints, and varnishes. Esterification is the general name for a chemical reaction in which two reactants (typically an alcohol and an acid) form an ester as the reaction product. Esters are common in organic chemistry and biological materials.Product Details of 109-85-3
Referemce:
Ether – Wikipedia,
Ether | (C2H5)2O – PubChem