Abstract:
Malaria afflicts more than 3 million people annually, and this debilitating and
deadly infectious disease results into a heavy toll on susceptible population around the
globe. The present chemotherapy which includes individual drugs and combinations
was designed and developed to target the pathogenic blood stages in humans and to
address the constant threat of drug resistance. However the use of artemisinin-based
combination therapy which still now was considered safe and effective is under threat
due to depleting efficacy of artemisinin in endemic areas. Hence the efforts to find
effective, safe and low cost drugs for malaria have to be given priority. This
exploratory activity is an effort in this direction.
The presentation of various chapters are as follows-
The first chapter contains a review of the literature highlighting the recent
developments in the hybrid antimalarials based on amino quinoline pharmacophore.
The basis for the design and selection of the prototype molecules comes into view in
the second chapter. Synthesis as well as antimalarial evaluation of pyrrolidinoaminoalkane
derivatives of quinoline and some new quinolinomethanols have been
discussed in the third chapter. Applications of the 1-formyl-9H-β-carboline for the
synthesis of fused β-carbolines which may be considered as analogues of naturally
occurring alkaloids via aza-Diels-Alder, multicomponent, ring closing metathesis,
Pomeranz-Fritsch and Friedel Craft reactions have been described in the fourth
chapter. The results related to the biological screening of these fused β-carbolines are
presented at the end of the chapter. The list of publications originating from this
endeavour is included at the end. All the chapters have separate bibliography and
compound numbering in Arabic.
