A series of lH-pyrrolo[3,2-b]pyridine (3a-3f) and fUroP,2-b]pyridine derivatives (4a-4g) were evaluated on human a7 nicotinic acetylcholine receptors (nAChRs) using two-electrode voltage clamp (TEVC) recording. A repr...A series of lH-pyrrolo[3,2-b]pyridine (3a-3f) and fUroP,2-b]pyridine derivatives (4a-4g) were evaluated on human a7 nicotinic acetylcholine receptors (nAChRs) using two-electrode voltage clamp (TEVC) recording. A representative 2-(2-methoxyphenyl)- furo[3,2-b]pyridine 4f as negative allosteric modulator (NAM) selectively inhibited alpha7 nAChR over a3p4, a4p2 nAChRs and 5-HT3a receptor, with a potency of IC50 of 5.51 |1M and a maximum inhibition rate of 87.8%. The preliminary analysis of structure-activity relationship (SAR) suggested that compound 4f could serve as a basis for further discovery of potent and selective a7 nAChR NAMs.展开更多
The reaction mechanism of 2-methoxybenzaldehyde, 4-bromo-indanone, malononitrile and ammonium acetate one-pot to form 6-（2-methoxyphenyl）-2-amino-6-bromo-5 Hindeno[1,2-b]pyridine-3-carbonitrile was studied by densit...The reaction mechanism of 2-methoxybenzaldehyde, 4-bromo-indanone, malononitrile and ammonium acetate one-pot to form 6-（2-methoxyphenyl）-2-amino-6-bromo-5 Hindeno[1,2-b]pyridine-3-carbonitrile was studied by density functional theory. The geometries of the reactants, transition states, intermediates and products were optimized at the PW91/DNP level. Vibration analysis was carried out to confirm the transition state structure. Reaction pathways were investigated in this study. The result indicates that the reaction Re→ TSB1→IMB1→ TSB2→ IMB2→TSB3→IMB3→TSB4→IMB4→TSB5→IMB5→TSB6→IMB6→TSB7→IMB7→ TSB8→IMB8→TSB9→IMB9→P2 is the main pathway, the activation energy of which is the lowest. The dominant product predicted theoretically is in agreement with the experiment results.展开更多
Cu doped ZnO nanocrystalline powder(10 mol%) has been found to be an efficient catalyst for the one‐pot multi‐component synthesis of fully substituted new indeno[1,2‐b]pyridines through a com-bination of 1,3‐indan...Cu doped ZnO nanocrystalline powder(10 mol%) has been found to be an efficient catalyst for the one‐pot multi‐component synthesis of fully substituted new indeno[1,2‐b]pyridines through a com-bination of 1,3‐indandione, propiophenone or acetophenone derivatives, aromatic aldehydes, and ammonium acetate in ethanol/H2 O at room temperature. The methodology is mild, efficient and high to excellent yielding.展开更多
基金National Natural Science Foundation(Grant No.21572011,81537410)Ministry of Science and Technology(Grant No.2014ZX09507003-006-004)
文摘A series of lH-pyrrolo[3,2-b]pyridine (3a-3f) and fUroP,2-b]pyridine derivatives (4a-4g) were evaluated on human a7 nicotinic acetylcholine receptors (nAChRs) using two-electrode voltage clamp (TEVC) recording. A representative 2-(2-methoxyphenyl)- furo[3,2-b]pyridine 4f as negative allosteric modulator (NAM) selectively inhibited alpha7 nAChR over a3p4, a4p2 nAChRs and 5-HT3a receptor, with a potency of IC50 of 5.51 |1M and a maximum inhibition rate of 87.8%. The preliminary analysis of structure-activity relationship (SAR) suggested that compound 4f could serve as a basis for further discovery of potent and selective a7 nAChR NAMs.
基金Project supported by the Scientific and Technological Research Program of Chongqing Municipal Education Commission(KJ1601215,KJ15012002)the Ministry of Education “Chunhui Plan”(Z2016177)
文摘The reaction mechanism of 2-methoxybenzaldehyde, 4-bromo-indanone, malononitrile and ammonium acetate one-pot to form 6-（2-methoxyphenyl）-2-amino-6-bromo-5 Hindeno[1,2-b]pyridine-3-carbonitrile was studied by density functional theory. The geometries of the reactants, transition states, intermediates and products were optimized at the PW91/DNP level. Vibration analysis was carried out to confirm the transition state structure. Reaction pathways were investigated in this study. The result indicates that the reaction Re→ TSB1→IMB1→ TSB2→ IMB2→TSB3→IMB3→TSB4→IMB4→TSB5→IMB5→TSB6→IMB6→TSB7→IMB7→ TSB8→IMB8→TSB9→IMB9→P2 is the main pathway, the activation energy of which is the lowest. The dominant product predicted theoretically is in agreement with the experiment results.
基金Financial support of this work from the Research Council of Mazandaran University
文摘Cu doped ZnO nanocrystalline powder(10 mol%) has been found to be an efficient catalyst for the one‐pot multi‐component synthesis of fully substituted new indeno[1,2‐b]pyridines through a com-bination of 1,3‐indandione, propiophenone or acetophenone derivatives, aromatic aldehydes, and ammonium acetate in ethanol/H2 O at room temperature. The methodology is mild, efficient and high to excellent yielding.
