Modification of the anabaseine pyridine nucleus allows achieving binding and functional selectivity for the α3β4 nicotinic acetylcholine receptor subtype

Identification of α7 Nicotinic Acetylcholine Receptor Silent Agonists Based on the Spirocyclic Quinuclidine‐Δ2‐Isoxazoline Scaffold: Synthesis and Electrophysiological Evaluation

“…The residue was purified by silica gel column chromatography (cyclohexane/EtOAc 2:3) to provide 28-35 as pure compounds. General procedure for borane deprotection:Asolution of CF 3 COOH (5 equiv) in acetone (3.5 mL mmol À1 28-35)w as added dropwise, under argon, to an ice-cooled stirred solution of 28-35 in acetone (3.5 mL mmol À1 [28][29][30][31][32][33][34][35]. After disappearance of the starting material (TLC with cyclohexane/EtOAc 2:3, CH 2 Cl 2 /MeOH 95:5), the mixture was concentrated under reduced pressure, and the residue was diluted with water.T he aqueous solution (pH 1-2) was extracted with Et 2 O( 1).…”

“…However, the structure–activity relationships (SARs) of silent agonists are still poorly defined, and in this study, we expand the chemical space of putative silent compounds and aim to provide further insight into their molecular interactions with the α7 nAChR. To this end, we first explored the series of known quaternary ammonium compounds 6 – 16 for their α7 nAChR silent‐agonist activity (Table ); these compounds were chosen from an array of selective nicotinic agonists studied by our research group . Among the screened compounds, 11 , 14 , and 15 (Figure ) turned out to behave as silent agonists (Table ).…”

“…To this end, we first explored the series of knownq uaternary ammonium compounds 6-16 [25,26] for their a7n AChRs ilent-agonist activity (Table 1);t hese compounds were chosen from an array of selective nicotinic agonists studied by our research group. [25][26][27][28][29][30][31][32][33][34] Among the screened compounds, 11, 14,a nd 15 ( Figure 2) turned out to behave as 1,N S-6740 [16] 0.06 AE 0.02 [b] 118 AE 22 [d] 2,K C-1 [20] 0.083 AE 0.009 [b] 17.8 AE 2.4 [d] 3,d iEPP [22,23] 0.002 AE 0.003 1.3 AE 0.3 4,TFM-diEPP [23] 0. (Table 1).…”

Quantitative structure–activity relationship (QSAR) directed the discovery of 3‐(pyridin‐2‐yl)benzenesulfonamide derivatives as novel herbicidal agents

“…In general, the development of novel pesticides includes a number of different methods, ranging from explorations of known chemical skeletons, to the high‐throughput screening of accumulations of agents in the endeavour to find new or formerly unidentified chemical scaffolds with favoured biological activities . An important type of structural frame is pyridine, which has broadly been utilised as a critical intermediate for agrochemicals and pharmaceuticals . At present, more than 70 products contain the pyridine unit among commercial pesticide varieties, for instance, imidacloprid, cyantraniliprole, fluopyram, pyribencarb, fluroxypyr and pyroxsulam.…”

“…14,15 An important type of structural frame is pyridine, which has broadly been utilised as a critical intermediate for agrochemicals and pharmaceuticals. 16,17 At present, more than 70 products contain the pyridine unit among commercial pesticide varieties, for instance, imidacloprid, cyantraniliprole, fluopyram, pyribencarb, fluroxypyr and pyroxsulam. Since the pesticides involving the pyridine element have the general features of high efficiency, low toxicity, and good compatibility with the ecological environment, they meet the requirements of integrated pest management, and these chemicals have already received great interest from contemporary agricultural chemists.…”