Synthesis, evaluation and computational studies on a series of acetophenone based 1-(aryloxypropyl)-4-(chloroaryl) piperazines as potential atypical antipsychotics

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“…The log BB values and molecular parameters values are important for blood brain barrier penetration and are calculated as log BB values are 0.26, 0.24 respectively. Topological polar surface area (TPSA) and log P computed for both the compounds are same, TPSA is 32.78 and log P is 3.371 indicated that both of these compounds have a good potential to penetrate the blood brain barrier and show CNS activity 63 . were evaluated using in vitro by radio ligand binding assays (Fig.…”

Design, synthesis, and biological evaluation of structurally constrained hybrid analogues containing ropinirole moiety as a novel class of potent and selective dopamine D3 receptor ligands

“…Interaction of the phenyl piperazine fragment with the dopamine D3 receptor would generate binding affinity, and the ropinirole moiety was expected to impart the selectivity for the D3 receptor by occupying extracellular binding pocket of the D3 receptor . Furthermore, arylpiperazine derivatives may enhance the physicochemical properties of compounds to penetrate the blood–brain barrier and show the desired CNS efficacy . On the basis of the crystal structure of the human D3R, as well as the basic design principals of combination, we have devised and synthesized novel indoline‐2‐ones derivatives (Figure ): (i) introduction of two important moiety of ropinirole and BP897; (ii) connection of the two moiety with a carbon chain containing 2–3 carbon atoms in order to adjust the spatial distance of the two fragments; and (iii) various substituted phenylpiperazines were also investigated.…”

Piperazine scaffold: A remarkable tool in generation of diverse pharmacological agents

“…Amongst the different piperazine derivatives synthesized byBali et al., compounds 148a and 148bwere reported as the most promising antipsychotic agents[249]. In another series of piperazine derivatives synthesized by Bali et al, compounds 149a and 149b were reported as the most promising antipsychotic agents[250]. In a series of compounds developed by Park et al, compound 150 was reported to exhibit maximum affinity towards 5-HT 2c and 5-HT 6 receptors[251].…”