Citation
Wang, Xuebao, et al. "Synthesis and Evaluation of Phenylxanthine Derivatives as Potential Dual A2AR Antagonists/MAO-B Inhibitors for Parkinson's Disease." Molecules (Basel, Switzerland), vol. 22, no. 6, 2017.
Wang X, Han C, Xu Y, et al. Synthesis and Evaluation of Phenylxanthine Derivatives as Potential Dual A2AR Antagonists/MAO-B Inhibitors for Parkinson's Disease. Molecules. 2017;22(6).
Wang, X., Han, C., Xu, Y., Wu, K., Chen, S., Hu, M., Wang, L., Ye, Y., & Ye, F. (2017). Synthesis and Evaluation of Phenylxanthine Derivatives as Potential Dual A2AR Antagonists/MAO-B Inhibitors for Parkinson's Disease. Molecules (Basel, Switzerland), 22(6). https://doi.org/10.3390/molecules22061010
Wang X, et al. Synthesis and Evaluation of Phenylxanthine Derivatives as Potential Dual A2AR Antagonists/MAO-B Inhibitors for Parkinson's Disease. Molecules. 2017 Jun 17;22(6) PubMed PMID: 28629145.
TY - JOUR
T1 - Synthesis and Evaluation of Phenylxanthine Derivatives as Potential Dual A2AR Antagonists/MAO-B Inhibitors for Parkinson's Disease.
AU - Wang,Xuebao,
AU - Han,Chao,
AU - Xu,Yong,
AU - Wu,Kaiqi,
AU - Chen,Shuangya,
AU - Hu,Mangsha,
AU - Wang,Luyao,
AU - Ye,Yun,
AU - Ye,Faqing,
Y1 - 2017/06/17/
PY - 2017/05/15/received
PY - 2017/06/13/revised
PY - 2017/06/14/accepted
PY - 2017/6/21/entrez
PY - 2017/6/21/pubmed
PY - 2018/3/27/medline
KW - adenosine A2AR antagonist
KW - monoamine oxidase B inhibitor
KW - parkinson′s disease
KW - phenylxanthine derivatives
JF - Molecules (Basel, Switzerland)
JO - Molecules
VL - 22
IS - 6
N2 - The aim of this research was to prove the speculation that phenylxanthine (PX) derivatives possess adenosine A2A receptor (A2AR)-blocking properties and to screening and evaluate these PX derivatives as dual A2AR antagonists/MAO-B inhibitors for Parkinson's disease. To explore this hypothesis, two series of PX derivatives were prepared and their antagonism against A2AR and inhibition against MAO-B were determined in vitro. In order to evaluate further the antiparkinsonian properties, pharmacokinetic and haloperidol-induced catalepsy experiments were carried out in vivo. The PX-D and PX-E analogues acted as potent A2AR antagonists with Ki values ranging from 0.27 to 10 μM, and these analogues displayed relatively mild MAO-B inhibition potencies, with inhibitor dissociation constants (Ki values) ranging from 0.25 to 10 μM. Further, the compounds PX-D-P6 and PX-E-P8 displayed efficacious antiparkinsonian properties in haloperidol-induced catalepsy experiments, verifying that these two compounds were potent A2AR antagonists and MAO-B inhibitors. We conclude that PX-D and PX-E analogues are a promising candidate class of dual-acting compounds for treating Parkinson's disease.
SN - 1420-3049
UR - https://www.unboundmedicine.com/medline/citation/28629145/Synthesis_and_Evaluation_of_Phenylxanthine_Derivatives_as_Potential_Dual_A2AR_Antagonists/MAO_B_Inhibitors_for_Parkinson's_Disease_
L2 - https://www.mdpi.com/resolver?pii=molecules22061010
DB - PRIME
DP - Unbound Medicine
ER -
