68295-48-7Relevant articles and documents
Antimalarial activity of novel pyrrolizidinyl derivatives of 4-aminoquinoline
Sparatore, Anna,Basilico, Nicoletta,Casagrande, Manolo,Parapini, Silvia,Taramelli, Donatella,Brun, Reto,Wittlin, Sergio,Sparatore, Fabio
, p. 3737 - 3740 (2008)
Two pyrrolizidinylalkyl derivatives of 4-amino-7-chloroquinoline (MG2 and MG3) were prepared and tested in vitro against CQ-sensitive and CQ-resistant strains of Plasmodium falciparum and in vivo in a Plasmodium berghei mouse model of infection. Both compounds exhibited excellent activity in all tests and low toxicity against mammalian cells. Preliminary studies of the acute toxicity and of the metabolism of the most active compound MG3 indicate a promising profile as a new antimalarial drug candidate.
BICYCLOAMINE-SUBSTITUTED-N-BENZENESULFONAMIDE COMPOUNDS WITH SELECTIVE ACTIVITY IN VOLTAGE-GATED SODIUM CHANNELS
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Paragraph 0179, (2015/06/11)
Disclosed are compounds of Formula (A-a), or a salt thereof, Where "B1" and "R1" through "R5" are as defined herein, which compounds have properties for blocking Nav 1.7 ion channels found in peripheral and sympathetic neurons. Also described are pharmaceutical formulations comprising the compounds of Formula (A-a) or their salts, and methods of treating neuropathic pain disorders using the same.
Synthesis and nicotinic receptor activity of chemical space analogues of N -(3 R)-1-azabicyclo[2.2.2]oct-3-yl-4-chlorobenzamide (PNU-282,987) and 1,4-diazabicyclo[3.2.2]nonane-4-carboxylic acid 4-bromophenyl ester (SSR180711)
Bréthous, Lise,Garcia-Delgado, Noemi,Schwartz, Julian,Bertrand, Sonia,Bertrand, Daniel,Reymond, Jean-Louis
supporting information; experimental part, p. 4605 - 4618 (2012/07/28)
The Chemical Universe Generated Databases up to 11 atoms of CNOF (GDB-11) and up to 13 atoms of CNOClS (GDB-13) were used to enumerate analogues of the diamine part of two known α7 nicotinic receptor agonists and construct libraries of virtual analogues of these drugs. The libraries were scored using structure-based (docking to the nicotine binding site of the acetylcholine binding protein 1uw6.pdb) or ligand-based (similarity to the parent drugs) methods, and the top-scoring virtual ligands were inspected for easily accessible synthetic targets. In total, 21 diamines were prepared and acylated with aromatic carboxylic or oxycarbonic acids to produce 85 analogues of the parent drugs. The compounds were profiled by electrophysiology in Xenopus oocytes expressing human nicotinic acetylcholine receptor (nAChR) subtypes α7, α3β2, α4β2, α3β4, or α4β4. Characterization of selected compounds revealed eight inhibitors of the α7 nicotinic receptor and three positive allosteric modulators of the α3β2 nAChR.
