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Bioactivity-guided synthesis of gramine derivatives as new MT 1 and 5-HT 1A receptors agonists.
- Source :
- Journal of Asian Natural Products Research; Jun2017, Vol. 19 Issue 6, p610-622, 13p
- Publication Year :
- 2017
-
Abstract
- Twenty-four gramine derivatives were synthesized and evaluated on MT1and 5-HT1Areceptorsin vitro. Among them, seven derivatives (7,8,16,19,20,21,and24)exhibited higher agonisting activities on MT1or 5-HT1Areceptors. Compared with gramine, derivatives7,8,16,19,20,21,and24displayed 1.6–3.5-fold increase in agonistic rates on 5-HT1Areceptor. Particularly, derivatives7,19,and21exhibited significant agonistic activities on MT1and 5-HT1Areceptors with EC50values of 0.51, 0.39, 0.50 mΜ and 0.28, 0.46, 0.23 mΜ, respectively. The preliminary structure–activity relationships of gramine derivatives were summarized for further investigation on MT1and 5-HT1Areceptors as new potential agonists. [ABSTRACT FROM PUBLISHER]
Details
- Language :
- English
- ISSN :
- 10286020
- Volume :
- 19
- Issue :
- 6
- Database :
- Complementary Index
- Journal :
- Journal of Asian Natural Products Research
- Publication Type :
- Academic Journal
- Accession number :
- 123394575
- Full Text :
- https://doi.org/10.1080/10286020.2017.1323885