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.COA of Formula: C6H14N2 This article mentions the following:
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. In the experiment, the researchers used many compounds, for example, (S)-2-Ethylpiperazine (cas: 207284-20-6COA of Formula: C6H14N2).
(S)-2-Ethylpiperazine (cas: 207284-20-6) belongs to piperazine derivatives. Piperazine causes primary dermal irritation and skin burns at high concentrations. Piperazine also causes eye irritation in humans. Outside the body, piperazine has a remarkable power to dissolve uric acid and producing a soluble urate, but in clinical experience it has not proved equally successful. COA of Formula: C6H14N2
Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics