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 published the artcile< Piperazinyl Bicyclic Derivatives as Selective Ligands of the α2δ-1 Subunit of Voltage-Gated Calcium Channels>, Application of C7H6BrNO2, the main research area is piperazinyl quinazolinone preparation calcium channel.
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.
ACS Medicinal Chemistry Letters published new progress about Acid chlorides Role: RCT (Reactant), RACT (Reactant or Reagent). 20776-50-5 belongs to class bromides-buliding-blocks, and the molecular formula is C7H6BrNO2, Application of C7H6BrNO2.
Referemce:
Bromide – Wikipedia,
bromide – Wiktionary