Interactions of a boron-containing levodopa derivative on D2 dopamine receptor and its effects in a Parkinson disease model

Synthesis, In Silico, and Biological Evaluation of a Borinic Tryptophan-Derivative That Induces Melatonin-like Amelioration of Cognitive Deficit in Male Rat

“…All affinity values were underestimated by 3–4 orders of magnitude. This is in agreement with similar procedures for the affinity estimation in G-protein-coupled receptors [ 21 , 29 , 33 ].…”

“…In addition, the hydrogen bonds between the amine in the indole moiety of the compounds and a threonine or tyrosine residue were shared in the complexes; the exposed oxygen from the boron-containing ring is also able to interact. Conversely to that reported for other boron-containing compounds in complexes with metabotropic receptors, including amine receptors [ 21 , 26 , 31 ], the boron atom (marked with an asterisk in Figure 5 ) exhibited no direct interaction with any residue in the binding sites.…”

“…The mechanisms for potential therapeutic action of BCCs in the nervous system involve neuronal action through enzyme inhibition [ 14 ], acting as ligands of membrane receptors [ 13 , 15 ], regulating immune response [ 16 ], glial activities [ 17 ], and levels and the action of brain-derived growth factors [ 18 , 19 ]. Thus, action of BCCs on neuronal disease models are increasing [ 20 , 21 ]. Among these are those suggesting multitarget beneficial action [ 22 ], those showing a pro-survival effect on human-derived SH-SY5Y cells such as an Aβ-toxicity model [ 15 , 23 ], as well as the ameliorative properties in in vitro and in vivo models of AD [ 24 , 25 ].…”

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“…[36] Dopaboroxazolidone, boron containing compound of boroxazolidones group, has potential as an attractive neuroactive drug against many neuromotor disorders. [37] Microelements such as sulfur and iron are integral part of certain proteins like CDGSH iron-sulfur domain-containing protein 1 localized on the outer membrane of mitochondria and plays key roles in regulating cell death and oxidative stress. [38] CONCLUSION Such combination of activities is ideal for the treatment of microbial infections with inflammatory consequences.…”

Alzheimer ve Parkinson Hastalıklarında Bor İçeren Bileşiklerin Nörokoruyucu Etkisi

“…afinitesinin Levadopa'ya göre daha yüksek olduğunu ve PH oluşturulan farelerde motor performans değerlendirmesinde 91,33 mg/kg DPBX uygulamasının 18 mg/kg MPTP'nin neden olduğu semptomların azaltılmasında 50 mg/kg Levadopa'ya benzer etki gösterdiğini bildirmişlerdir. Ek olarak DPBX'in, substantia nigradaki nöron kaybını azalttığı ifade edilmiştir[79]. Sıçanlarda 20 mg/kg BA uygulamasının tirozin hidroksilaz (TH) aktivitesini arttırdığı ve PH patogenezinde antioksidan aktivite ile dopaminerjik sistemi koruyabileceği bildirilmiştir.…”