Structure Activity relationship of Bioactive Compounds from Medicinal Plants

Abstract

Natural products provide a starting point for new synthetic compounds with diverse structures and often with multiple stereocenters that can be challenging synthetically. Many structural features common to natural products (e.g., chiral centers, aromatic rings, complex ring systems, degree of molecule saturation, and number and ratio of heteroatoms) have been shown to be highly relevant to drug discovery efforts. Since, the escalation of interest in combinatorial chemistry and the subsequent realization that these compound libraries may not always be very diverse, many synthetic and medicinal chemists are exploring the creation of natural product and natural-product like libraries that combine the structural features of natural products with the compound-generating potential of combinatorial chemistry. In conclusion, in the present study structural modification of two natural products was carried out for structure activity relationship studies. Including sixteen new compounds twenty four derivatives along with a novel embelin-ninhydrin adduct were prepared from embelin. A new and three known mangiferin derivatives were also prepared. All these compounds were characterized by physical and spectral properties. The derivatives of embelin and mangiferin were tested for in vitro antioxidant properties. Some of the derivatives showed potent in vitro antioxidant properties compared to the parent moieties. The potent antioxidant compounds also exhibited potent analgesic and anti-inflammatory activities. Hence, the structural modification of natural compounds played an important role to improve the biological activities. Embelin exhibited potent anticonvulsant properties. It exhibited potent antidiabetic properties in alloxan induced diabetes, protective effect against acetic acid induced colitis and neuroprotective effect against global cerebral ischemia in rats. Hence, new biological properties of embelin were established, which supports the traditional claim of the plant. newline newline