Publications by authors named "M Hrabinova"
We aimed to prepare novel dibenzo [a,d][7]annulen derivatives that act on N-methyl-d-aspartate (NMDA) receptors with potential neuroprotective effects. Our approach involved modifying the tropane moiety of MK-801, a potent open-channel blocker known for its psychomimetic side effects, by introducing a seven-membered ring with substituted base moieties specifically to alleviate these undesirable effects. Our in silico analyses showed that these derivatives should have high gastrointestinal absorption and cross the blood-brain barrier (BBB).
View Article and Find Full Text PDFThe investigation into human butyrylcholinesterase (BChE) inhibitors as therapeutic agents for Alzheimer's disease (AD) holds significant promise, addressing both symptomatic relief and disease progression. In the pursuit of novel drug candidates with a selective BChE inhibition pattern, we focused on naturally occurring template structures, specifically Amaryllidaceae alkaloids of the carltonine-type. Herein, we explored a series of compounds implementing an innovative chemical scaffold built on the 3- and 4-benzyloxy-benzylamino chemotype.
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- * Researchers investigated 29 novel reactivators, emphasizing the zwitterionic strategy and discovering 17 mono-oxime and nine bisoxime reactivators that show significant promise.
- * The top compounds, particularly 55, 57, and 58, outperform existing clinical antidotes like pralidoxime in reactivating potency, highlighting their potential for treating OP poisoning more effectively.
Article Synopsis
- Researchers are exploring new drug options for Alzheimer's disease by focusing on multi-target directed ligands (MTDLs) that can address the disease's complexity more effectively.
- They modified the drug amiridine, a known cholinesterase inhibitor, by combining it with other compounds to create MTDLs that also possess additional benefits, such as NMDA receptor affinity and antioxidant effects.
- The study's findings, particularly regarding a top compound called 5d, suggest that these new amiridine-based drugs could offer a broader therapeutic approach for treating Alzheimer's disease.
Article Synopsis
- A-234 is a new generation nerve agent implicated in the poisoning of a former Russian spy in 2018, leading to its inclusion in the Chemical Weapons Convention.
- Research indicates limited information on A-234's chemical properties, biological effects, and effective treatments, with findings showing the agent is stable but exhibits significant toxicity similar to VX.
- Current antidotes, especially oximes like HI-6 and methoxime, show minimal effectiveness in reactivating inhibited enzymes, while atropine and diazepam provide better therapeutic outcomes against A-234 lethality.