Affiliation: Charles University
Country: Czech Republic
Janockova J, Dolezal R, Nepovimova E, Kobrlova T, Benkova M, Kuca K, et al
. Investigation of New Orexin 2 Receptor Modulators Using In Silico and In Vitro Methods. Molecules. 2018;23: pubmed publisher
..It was shown that L4 was the most potent antagonistic ligand to orexin A and displayed an IC50 of 2.2 µM, offering some promise mainly for the treatment of insomnia. ..
Sepsova V, Krusek J, Zdarova Karasova J, Zemek F, Musilek K, Kuca K, et al
. The interaction of quaternary reversible acetylcholinesterase inhibitors with the nicotinic receptor. Physiol Res. 2014;63:771-7 pubmed
..However, since no positive modulation was observed, the new compounds do not seem to be promising candidates for MG treatment, even though their cytotoxic effect was relatively low. ..
Korabecny J, Andrs M, Nepovimova E, Dolezal R, Babkova K, Horova A, et al
. 7-Methoxytacrine-p-Anisidine Hybrids as Novel Dual Binding Site Acetylcholinesterase Inhibitors for Alzheimer's Disease Treatment. Molecules. 2015;20:22084-101 pubmed publisher
..Indeed, the novel derivatives proved to be effective non-specific cholinesterase inhibitors showing non-competitive AChE inhibition patterns. This compounds' behavior was confirmed in the subsequent molecular modeling studies. ..
Honegr J, Dolezal R, Malinak D, Benkova M, Soukup O, Almeida J, et al
. Rational Design of a New Class of Toll-Like Receptor 4 (TLR4) Tryptamine Related Agonists by Means of the Structure- and Ligand-Based Virtual Screening for Vaccine Adjuvant Discovery. Molecules. 2018;23: pubmed publisher
..Moreover, two compounds from the series show also significant ability to elicit production of interleukin 6. ..
Hepnarova V, Korabecny J, Matoušková L, Jost P, Muckova L, Hrabinova M, et al
. The concept of hybrid molecules of tacrine and benzyl quinolone carboxylic acid (BQCA) as multifunctional agents for Alzheimer's disease. Eur J Med Chem. 2018;150:292-306 pubmed publisher
..23â€¯Î¼M). A non-selective pattern of cholinesterase inhibition is likely to be valuable during the onset as well as later stages of AD. ..
Soukup O, Kristofikova Z, Jun D, Tambor V, Ripova D, Kuca K. The interaction of standard oxime reactivators with hemicholinium-3 sensitive choline carriers. Toxicol Lett. 2012;212:315-9 pubmed publisher
..The influence of reactivators on the carriers could be unfavorable in the case of their prolonged administration in vivo. From this point of view, the application of methoxime appears to be the best...
Soukup O, Dolezal R, Malinak D, Marek J, Salajkova S, Pasdiorova M, et al
. Synthesis, antimicrobial evaluation and molecular modeling of 5-hydroxyisoquinolinium salt series; the effect of the hydroxyl moiety. Bioorg Med Chem. 2016;24:841-8 pubmed publisher
Horak M, Holubova K, Nepovimova E, Krusek J, Kaniaková M, Korabecny J, et al
. The pharmacology of tacrine at N-methyl-d-aspartate receptors. Prog Neuropsychopharmacol Biol Psychiatry. 2017;75:54-62 pubmed publisher
Spilovská K, Korabecny J, Sepsova V, Jun D, Hrabinova M, Jost P, et al
. Novel Tacrine-Scutellarin Hybrids as Multipotent Anti-Alzheimer's Agents: Design, Synthesis and Biological Evaluation. Molecules. 2017;22: pubmed publisher
..Kinetic studies performed on hAChE with the most active compound in the study, K1383, pointed out to a mixed, non-competitive enzyme inhibition. These findings were further corroborated by docking studies. ..