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Substituted 4-phenyl-2-aminoimidazoles and 4-phenyl-4,5-dihydro-2- aminoimidazoles as voltage-gated sodium channel modulatorsZidar, Nace ...Voltage-gated sodium channels play an integral part in neurotransmission and their dysfunction is frequently a cause of various neurological disorders. On the basis of the structure of marine ... alkaloid clathrodin, twenty eight new analogs were designed, synthesized and tested for their ability to block human NaV1.3, NaV1.4 and NaV1.7 channels, as well as for their selectivity against human cardiac isoform NaV1.5, using automated patch clamp electrophysiological assay. Several compounds exhibited promising activities on different NaV channel isoforms in the medium micromolar range and some of the compounds showed also moderate isoform selectivities. The most promising results were obtained for the NaV1.3 channel, for which four compounds were found to possess IC50 values lower than 15 ŽM. All of the active compounds bind to the open-inactivated states of the channels and therefore act as state-dependent modulators. The obtained results validate the approach of using natural products driven chemistry for drug discovery starting points andrepresent a good fundation for future design of selective NaV modulators.Vir: European journal of medicinal chemistry. - ISSN 0223-5234 (Vol. 74, 2014, str. 23-30)Vrsta gradiva - članek, sestavni delLeto - 2014Jezik - angleškiCOBISS.SI-ID - 3585905
Avtor
Zidar, Nace |
Jakopin, Žiga |
Madge, David J. |
Chan, Fiona |
Tytgat, Jan |
Peigneur, Steve |
Sollner Dolenc, Marija |
Tomašič, Tihomir |
Ilaš, Janez |
Peterlin-Mašič, Lucija |
Kikelj, Danijel
Teme
voltage-gated sodium channel |
NaV channel modulator |
marine alkaloid |
clathrodin |
pyrrole-2-aminoimidazole |
4-phenyl-2-aminoimidazole
Vnos na polico
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Povezave do osebnih bibliografij avtorjev | Povezave do podatkov o raziskovalcih v sistemu SICRIS |
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Zidar, Nace | 28905 |
Jakopin, Žiga | 26496 |
Madge, David J. | |
Chan, Fiona | |
Tytgat, Jan | |
Peigneur, Steve | |
Sollner Dolenc, Marija | 08519 |
Tomašič, Tihomir | 28334 |
Ilaš, Janez | 24400 |
Peterlin-Mašič, Lucija | 19317 |
Kikelj, Danijel | 01463 |
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