Synthesis of some substituted indole derivatives and study of their characteristics with and without the formation of inclusion complexes

Abstract

Indole and its derivatives occupy a unique place in medicinal Chemistry due to their newlinewide range of pharmacological and biological activities. The beauty of Indole moiety newlineis that it provides a privilege scaffold for the discovery of more active, less toxic, newlinenovel drugs with diverse modes of action. The incorporation of Indole nucleus in newlinecertain organic compounds especially in certain aromatics and heterocycles has made newlineit versatile heterocyclic possessing significant pharmacological activities like newlineanticancer, antitubercular, antibacterial, antifungal, antiviral, antioxidant and many newlineothers. Hence, with an objective of discovering potent pharmacological activities, in newlinethe present work, different newly substituted indoles have been synthesized by newlinecondensing some aromatic and heterocyclic aldehydes with a key compound, 2- newlineAmino-1,3,4-thiadiazino[6,5b] Indole, which in turn is synthesized by methanolic newlinerefluxation of Indole-2,3-dione with thiosemicarbazide. The formation of the synthesized compounds has been confirmed from their elemental analysis and spectral newlinestudies such as UV, FTIR and PMR. newlineThe synthesized compounds are found to be sparingly soluble in polar solvents like newlinewater, which may be a restraining factor in decreasing their pharmacological newlineactivities. So, with an objective of increasing the solubility and bioaccessibility of newlinethese compounds, their inclusion complexes are prepared with a suitable host newlinemolecule, and#946;-cyclodextrin, a useful molecular encapsulant. newline