192443-41-7Relevant academic research and scientific papers
3D pharmacophore models for 1,2,3,4-tetrahydroisoquinoline derivatives acting as anticonvulsant agents
De Luca, Laura,Gitto, Rosaria,Barreca, Maria Letizia,Caruso, Roberta,Quartarone, Silvana,Citraro, Rita,De Sarro, Giovambattista,Chimirri, Alba
, p. 388 - 400 (2007/10/03)
A 3D pharmacophore model predicting anticonvulsant activity was obtained for a series of 6,7-dimethoxy-1,2,3,4-tetrahydroisoquinoline derivatives recently disclosed as a new class of non-competitive AMPA receptor antagonists. The training set included 17
Tetrahydroisoquinolines as subtype selective estrogen agonists/antagonists
Chesworth, Richard,Zawistoski, Michael P.,Lefker, Bruce A.,Cameron, Kimberly O.,Day, Robert F.,Mangano, F. Michael,Rosati, Robert L.,Colella, Stacy,Petersen, Donna N.,Brault, Amy,Lu, Bihong,Pan, Lydia C.,Perry, Pia,Ng, Oicheng,Castleberry, Tessa A.,Owen, Thomas A.,Brown, Thomas A.,Thompson, David D.,DaSilva-Jardine, Paul
, p. 2729 - 2733 (2007/10/03)
Two series of 6-hydroxy and 7-hydroxy tetrahydroisoquinolines were prepared. Evaluating a range of C-1, C-4, and N-substituents led to the discovery of ER α and ER β selective analogs.
Synthesis and structure-activity studies of novel orally active non-terpenoic 2,3-oxidosqualene cyclase inhibitors
Dehmlow, Henrietta,Aebi, Johannes D.,Jolidon, Synèse,Ji, Yu-Hua,Von der Mark, Elisabeth M.,Himber, Jacques,Morand, Olivier H.
, p. 3354 - 3370 (2007/10/03)
New orally active non-terpenoic inhibitors of human 2,3-oxidosqualene cyclase (hOSC) are reported. The starting point for the optimization process was a set of compounds derived from a fungicide project, which in addition to showing high affinity for OSC from Candida albicans showed also high affinity for human OSC. Common structural elements of these inhibitors are an amine residue and an electrophilic carbonyl C atom embedded in a benzophenone system, which are at a distance of about 10.7 ?. Considering that the keto moiety is in a potentially labile position, modifications of the substitution pattern at the benzophenone as well as annelated heteroaryl systems were explored. Our approach combined testing of the compounds first for increased binding affinity and for increased stability in vitro. Most promising compounds were then evaluated for their efficacy in lowering plasma total cholesterol (TC) and plasma low-density lipoprotein cholesterol (LDL-C) in hyperlipidemic hamsters. In this respect, the most promising compounds are the benzophenone derivative 1·fumarate and the benzo[d]-isothiazol 24·fumarate, which lowered TC by 40% and 33%, respectively.
Aminoalkyl-substituted benzo-heterocyclic compounds
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, (2008/06/13)
Aminoalkyl-substituted benzo-heterocyclic compounds of the formula STR1 wherein M, Q, R and T are as defined in the specification, as well as acid addition salts thereof. These compounds are useful as cholesterol level lowering agents and as antimycotic agents.
