5 documents found, page 1 of 1
Synthesis and Biological Assessment of Furoquinolines, Pyrroloquinolines and An...
Martins, C; Carreiras, MC; Mendes, E; de los Rios, C; Léon, R; Ramsay, R; Marco-Contelles, J
Synthesis, biological evaluation and molecular modelling of diversely functiona...
Marco, JL; de los Rios, C; Garcia, AG; Villarroya, M; Carreiras, MC; Martins, C; Eleuterio, A; Morreale, A; Orozco, M; Luque, FJThe synthesis and the biological activity of compounds 5-40 as inhibitors of acetyleholinesterase (AChE) and butyrylcholinesterase (BuChE), as well as modulators of voltage-dependent Ca2+ channels and nicotinic receptors, are described. These molecules are tacrine analogues, which have been prepared from polyfunctionalized 6-amino-5-cyano-4H-pyrans, 6-amino-5-cyano-pyridines and 5-amino-2-aryl-3-cyano-1,3-oxazo...
Novel tacrine derivatives that block neuronal calcium channels
de los Rios, C; Marco, JL; Carreiras, MDC; Chinchon, PM; Garcia, AG; Villarroya, MA new series of tacrine (9-amino-1,2,3,4-tetrahydroacridine) derivatives were synthesized and their effects on Ca-45 (2+) entry into bovine adrenal chromaffin cells stimulated with dimethylphenylpiperazinium (DMPP) or K+, studied. At 3 PM, compound 1 did not affect Ca-45(2+) uptake evoked by DMPP. Compounds 14, 15 and 17 inhibited the effects of DMPP by 30%. Compounds 3, 9 and tacrine blocked the DMPP signal by...
Synthesis and acetylcholinesterase/butyrylcholin-esterase inhibition activity o...
Marco, JL; de los Rios, C; Carreiras, MC; Banos, JE; Badia, A; Vivas, NMThe acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE) inhibition activities of a series of 4-amino-2,3-diaryl-5,6,7,8-tetrahydrofuro[2,3-b]quinolines (10-12)/4-amino-5,6,7,8-tetrahydro-2,3-diphenylthieno[2,3-b]quinoline (14) and 4-amino-5,6,7,8,9-pentahydro-2,3-diphenylcyclohepta[e]furo[2,3-b]pyridine (13)/4amino-5,6,7,8,9-pentahydro-2,3-phenylcyclohepta[e]thieno[2,3-b]pyridine (15) are described. T...
Synthesis and acetylcholinesterase/butyrylcholinesterase inhibition activity of...
Marco, JL; de los Rios, C; Carreiras, MC; Banos, JE; Badia, A; Vivas, NMThe synthesis and preliminary results for acetylcholinesterase and butyrylcholinesterase inhibition activity of a series of pyrano[2,3-b]quinolines (2, 3) and benzonaphthyridines (5, 6) derivatives are described. These molecules are tacrine-like analogues which have been prepared from readily available polyfunctionalized ethyl [6-amino-5-cyano-4H-pyrans and 6-amino-5-cyanopyridine s]-3-carboxylates via Friedlan...