Tags

Type your tag names separated by a space and hit enter

Design, synthesis and inhibitory activities of 8-(substituted styrol-formamido)phenyl-xanthine derivatives on monoamine oxidase B.
Chem Pharm Bull (Tokyo). 2012; 60(3):385-90.CP

Abstract

The design and synthesis of two series of 8-(substituted styrol-formamido)phenyl-xanthine derivatives are described. Their in vitro monoamine oxidase B (MAO-B) inhibition were tested and the effect of substituents on the N-7, phenyl and the substituted positions are discussed. It was observed that compound 9b displayed significant MAO-B inhibition activity and selectivity, fluorine substitution plays a key role in the selectivity of MAO-B inhibition, and the styrol-formamido group at position-3' may enhance the activity and selectivity of 8-phenyl-xanthine analogues. These results suggest that such compounds may be utilized for the development of new candidate MAO-B inhibitors for treatment of Parkinson's disease.

Authors+Show Affiliations

School of Pharmacy, Wenzhou Medical College, Department of Heurology, the First Affiliated Hospital of Wenzhou Medical College, Zhejiang, PR China.No affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info available

Pub Type(s)

Journal Article
Research Support, Non-U.S. Gov't

Language

eng

PubMed ID

22382421

Citation

Hu, Suwen, et al. "Design, Synthesis and Inhibitory Activities of 8-(substituted Styrol-formamido)phenyl-xanthine Derivatives On Monoamine Oxidase B." Chemical & Pharmaceutical Bulletin, vol. 60, no. 3, 2012, pp. 385-90.
Hu S, Nian S, Qin K, et al. Design, synthesis and inhibitory activities of 8-(substituted styrol-formamido)phenyl-xanthine derivatives on monoamine oxidase B. Chem Pharm Bull (Tokyo). 2012;60(3):385-90.
Hu, S., Nian, S., Qin, K., Xiao, T., Li, L., Qi, X., Ye, F., Liang, G., Hu, G., He, J., Yu, Y., & Song, B. (2012). Design, synthesis and inhibitory activities of 8-(substituted styrol-formamido)phenyl-xanthine derivatives on monoamine oxidase B. Chemical & Pharmaceutical Bulletin, 60(3), 385-90.
Hu S, et al. Design, Synthesis and Inhibitory Activities of 8-(substituted Styrol-formamido)phenyl-xanthine Derivatives On Monoamine Oxidase B. Chem Pharm Bull (Tokyo). 2012;60(3):385-90. PubMed PMID: 22382421.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Design, synthesis and inhibitory activities of 8-(substituted styrol-formamido)phenyl-xanthine derivatives on monoamine oxidase B. AU - Hu,Suwen, AU - Nian,Siyun, AU - Qin,Kuiyou, AU - Xiao,Tong, AU - Li,Lingna, AU - Qi,Xiaolu, AU - Ye,Faqing, AU - Liang,Guang, AU - Hu,Guoxin, AU - He,Jincai, AU - Yu,Yinfei, AU - Song,Bo, PY - 2012/3/3/entrez PY - 2012/3/3/pubmed PY - 2012/9/11/medline SP - 385 EP - 90 JF - Chemical & pharmaceutical bulletin JO - Chem Pharm Bull (Tokyo) VL - 60 IS - 3 N2 - The design and synthesis of two series of 8-(substituted styrol-formamido)phenyl-xanthine derivatives are described. Their in vitro monoamine oxidase B (MAO-B) inhibition were tested and the effect of substituents on the N-7, phenyl and the substituted positions are discussed. It was observed that compound 9b displayed significant MAO-B inhibition activity and selectivity, fluorine substitution plays a key role in the selectivity of MAO-B inhibition, and the styrol-formamido group at position-3' may enhance the activity and selectivity of 8-phenyl-xanthine analogues. These results suggest that such compounds may be utilized for the development of new candidate MAO-B inhibitors for treatment of Parkinson's disease. SN - 1347-5223 UR - https://www.unboundmedicine.com/medline/citation/22382421/Design_synthesis_and_inhibitory_activities_of_8__substituted_styrol_formamido_phenyl_xanthine_derivatives_on_monoamine_oxidase_B_ L2 - https://joi.jlc.jst.go.jp/JST.JSTAGE/cpb/60.385?lang=en&from=PubMed DB - PRIME DP - Unbound Medicine ER -