Methodology development
Despite the tremendous efforts in the development/use of synthetic methods in drug
discovery project, organic synthesis is still the rate limiting factor (slowest/consumes
maximum time slab). In this regard, development of novel synthetic toolsfor the
rapid access to pharmacophores of diverse scaffolds in stepeconomicaland thosein
completely stereo- (diastereo- and enantioselectivity) controlled mannerwould expedite
the process. In this perspective, our group will put effortsin the development of
transition-metal based catalytic systems for molecular transformations with the
aim to construct diverse scaffolds of therapeutic relevance.
Asymmetric Synthesis
Synthesis of a single enantiomer of drug molecules is essential for their specific
biomedical properties, as biological receptor sites are chiral in general (usually
proteins).As a result, except few, all 15 drugs approved by US-FDA are single-enantiomer
(in 2015). Thus, the synthesis of enantioenriched building blocks/pharmacophores
is an urgent and privileged subject for academic research as well as for pharmaceutical
development. Align with our methodology development part; we will focus on development
of Transition-metal/chiral ligand (NHC) catalytic system for asymmetric molecular
transformation and synthesis of chiral bioactive molecules.
Medicinal Chemistry
➤As a part of medicinal chemistry front, we will focus on the design and synthesis
of novel class of drug molecules (by introducing asymmetry in the molecule or bioisosteres).
We will also work on discovery of new class of natural product inspired hybrid molecules
in the search of potent candidates for various therapeutic targets.
➤Development of multidrug resistance in pathogens is threatening to public health.
In such case, development of new mode of action using un-natural drugs could be
a probable solution.Despite the fact of favourable pharmaceutical features associated
with silicon and boron, very little is currently explored in therapeutics, unlike
‘deuterium click’. After finding the place of boron-based drug molecule, Velcade®
in the market and few in pipe lines, it provides a rare venue to medicinal chemists
to explore in this area. It may also create improved therapeutic properties and
high IP values. By introducing tricoordinated boronin the drug molecule and exploiting
its Lewis acidic character with therapeutic target could alter the mode of action/efficacy.
We wish to explore this arena in medicinal chemistry.