Rational Design, Synthesis and Characterization of Novel Sibutramine Derivatives as Anti-Obesity Activity

Abstract

Sibutramine is a medication that is often used orally to treat obesity (marketed under the names Meridia in the US and Reductil in Europe and other countries). It is classed as a Schedule IV prohibited drug in the United States because it is an amphetaminerelated centrally acting stimulant. Due to worries that the medication raises the risk of heart attack and stroke in people with a history of heart disease, sibutramine was taken off the market in Canada and the United States in October 2010. To overcome the associated problem, a strategy was developed where selective modification of this drug was performed by chemically reacting with a substrate (4-aminophenol) to form a new derivative [4-((4-(1-(1-(dimethylamino)-3-methylbutyl)cyclobutyl)phenyl) amino)phenol]. This novel derivative was comprehensively characterized by sophisticated analytical instruments such as FTIR, ¹H-NMR, 13C-NMR, and Mass spectroscopic spectroscopy.