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Pyrimido[1,2-b]indazole derivatives : selective inhibitors of human monoamine oxidase B with neuroprotective activityJismy, Badr ...Structurally diverse heterotricyclic compounds are recognized as monoamine oxidase (MAO) inhibitors and thus represent an appealing scaffold in development and optimization of novel MAO inhibitors. ... Herein we explored the chemical space of pyrimido[1,2-b]indazoles as MAO inhibitors by preparing a small library of (hetero)aryl derivatives. An efficient synthetic strategy was developed starting from commercially available 1H-indazol-3-amines, which were converted to various 3-bromoheterotricyclic derivatives and further functionalized via Suzuki-Miyaura coupling reaction. Derivatives 4a-t selectively inhibited human MAO-B isoform in a reversible and competitive manner as confirmed by kinetic experiments and docking studies. Selected derivatives were not cytotoxic to neuroblastoma SH-SY5Y cells. Moreover, analogue 4i protected human neuroblastoma SH-SY5Y cells against 6-hydroxydopamine-induced cell death, which confirms the applicability of the pyrimido[1,2-b]indazoles as potential antiparkinsonian agents.Source: European journal of medicinal chemistry. - ISSN 0223-5234 (Vol. 209, 2021, str. 1-16)Type of material - article, component part ; adult, seriousPublish date - 2021Language - englishCOBISS.SI-ID - 31851523
Author
Jismy, Badr |
El Qami, Abdelkarim |
Pišlar, Anja |
Frlan, Rok |
Kos, Janko, 1959- |
Gobec, Stanislav, 1970- |
Knez, Damijan, farmacevt |
Abarbri, Mohamed
Topics
Parkinsonova bolezen |
monoamine oxidase |
Parkinson's disease |
neuroprotection |
pyrimido[1,2-b]indazoles |
inhibitors |
antimicrobial activity |
quaternary ammonium salts |
bacteria |
fungi |
virus |
cytotoxicity |
mixtures
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Database name | Field | Year |
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Links to authors' personal bibliographies | Links to information on researchers in the SICRIS system |
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Jismy, Badr | |
El Qami, Abdelkarim | |
Pišlar, Anja | 32035 |
Frlan, Rok | 26512 |
Kos, Janko, 1959- | 04648 |
Gobec, Stanislav, 1970- | 15284 |
Knez, Damijan, farmacevt | 36438 |
Abarbri, Mohamed |
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