Novel agonists of benzodiazepine receptors: Design, synthesis, binding assay and pharmacological evaluation of 1,2,4-triazolo[1,5-a]pyrimidinone and 3-amino-1,2,4-triazole derivatives

Design, synthesis, pharmacological evaluation, and docking study of new acridone-based 1,2,4-oxadiazoles as potential anticonvulsant agents

“…Presumably, the designed compounds can act as anticonvulsant agents (such as diazepam and estazolam) through benzodiazepine (BZD) receptors; they have the requirements for binding to these receptors: an aromatic ring (A), a coplanar proton-accepting group in a suitable distance (B), and second out-of-plane aromatic ring (C) that the last case could potentiate binding to the receptor especially for agonists ( Fig. 2) [9]. Thus we report here, the synthesis, pharmacological evaluation, and docking study of 10-(3-aryl- [1,2,4]oxadiazol-5-ylmethyl)-10H-acridin-9-one derivatives 11a-n as potential anticonvulsant agents.…”

Novel 4-thiazolidinone derivatives as agonists of benzodiazepine receptors: design, synthesis and pharmacological evaluation

“…We recorded the duration of loss of righting reflex, which represents the sleeping time. Since pentobarbital may cause hypothermia, animals were located on the top of an electric blanket (set at 37° C) after administration of pentobarbital (Faizi et al, 2015[6]).…”

“…Immediately after entering to the dark compartment, an unpleasant electrical shock (0.5 mA, 2 seconds) was delivered to the mouse from bottom of the compartment. On the second day (testing day), animal was located in the light compartment and the delay time for each mouse to enter the dark compartment was recorded (Faizi et al, 2015[6]).…”

“…Furthermore, the previously reported article revealed that thiazolidinone derivatives exhibit anticonvulsant activity (Tripathi et al, 2014[21]). Based on these evidences and our earlier published papers on flexible novel heterocyclic compounds (Akbarzadeh et al, 2003[1]; Almasirad et al, 2004[4]; Zarghi et al, 2005[24]; Almasirad et al, 2007[5]; Zarghi et al, 2008[22]; Mahdavi et al, 2010[13]; Faizi et al, 2012[7]; Tabatabai et al, 2013[20]; Zarghi et al, 2008[22][23]; Faizi, et al, 2015[6]) , some new thiazolidinone derivatives that have the essential pharmacophore groups for binding to the BZD's receptors were developed (Figure 1(Fig. 1)).…”

Design, synthesis, and evaluation of anticonvulsant activities of benzoxazole derivatives containing the 1,2,4‐triazolone moiety

“…Presumably, the designed compounds will act as anticonvulsant agents through BZD receptors, because they have the essential features like diazepam for binding to those receptors: an aromatic ring (A), a coplanar proton‐accepting group in a suitable distance (B), and second out‐of‐plane aromatic ring (C). The pharmacophore moieties A and B are essential for interaction with the GABA A receptor, while the part C could potentiate binding to the receptor (Figure ) …”