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Novel coumarin-pyridazine hybrids as selective MAO-B inhibitors for the Parkinson's disease therapy.

Abstract：

:The 3-pyridazinylcoumarin scaffold was previously reported as an efficient core for the discovery of reversible and selective inhibitors of MAO-B, a validated drug target for PD therapy which also plays an important role in the AD progress. Looking for its structural optimization, novel compounds of hybrid structure coumarin-pyridazine, differing in polarizability and lipophilicity properties, were synthesized and tested against the two MAO isoforms, MAO-A and MAO-B (compounds 17a-f and 18a-f). All the designed compounds selectively inhibited the MAO-B isoenzyme, exhibiting many of them IC50 values ranging from sub-micromolar to nanomolar grade and lacking neuronal toxicity. The 7-bromo-3-(6-bromopyridazin-3-yl)coumarin (18c), the most potent compound of these series (IC50 = 60 nM), was subjected to further in vivo studies in a reserpine-induced mouse PD model. The obtained results suggest a promising potential for 18c as antiparkinsonian agent. Molecular modeling studies also provided valuable information about the enzyme-drug interactions and the potential pharmacokinetic profile of the novel compounds.

journal_name

Bioorg Chem

journal_title

Bioorganic chemistry

authors

Rodríguez-Enríquez F,Costas-Lago MC,Besada P,Alonso-Pena M,Torres-Terán I,Viña D,Fontenla JÁ,Sturlese M,Moro S,Quezada E,Terán C

doi

10.1016/j.bioorg.2020.104203

subject

Has Abstract

pub_date

2020-11-01 00:00:00

pages

104203

eissn

0045-2068

issn

1090-2120

pii

S0045-2068(20)31500-5

journal_volume

104

pub_type

杂志文章

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