ABSTRACT

Mitragynine (1) is the major alkaloid in the traditional medicinal herb Mitragyna speciosa Korth. (Adkins et al. 2011; Raffa et al. 2013; Takayama 2004; Takayama et al. 2005; Watanabe et al. 1999), and has been proven to exhibit analgesic activity (Horie et al. 1995, 2005; Matsumoto et al. 1996a,b, 1997, 2005; Thongpraditchote et al. 1998; Tohda et al. 1997; Watanabe et al. 1997) mediated by opioid receptors. This natural product has been used as a seed molecule for the development of new analgesic in medicinal chemistry. This chapter covers published work on the syntheses of mitragynine derivatives, the evaluation of their analgesic activities, and the structure-activity relationship studies of mitragynine analogs.