Second Generation Chiral PVPs Useful in Drug Discovery

Novel chiral-substituted poly-N-vinylpyrrolidinones (Chiral PVPs) having superior stereoselectivity, enantioselectivity and regioselectivity have been developed. These Chiral PVPs offer advanced chiral recognition and enantioselective synthesis, allowing for the production of various chiral pharmaceuticals and compounds of commercial interest. Further, these Chiral PVPs are easy and inexpensive to produce, have long shelf-life and stable at high temperatures (>120oC).

The Chiral PVPs work by stabilizing and encapsulating bimetallic nanoclusters, that in turn catalyze various asymmetric oxidation reactions resulting in excellent chemical and optical yields, such as in the enantioselective oxidation of cyclic diols and polyols, alkenes (to produce chiral syndihydroxylated products), and unactivated C-H bond of cycloalkanes (to produce chiral oxygenated cycloalkanes). They also allow for regioselective C-H oxidation of medium-sized and complex bioactive natural products or drug molecules to produce oxidized drug analogs with enhanced physical property and functional groups, leading to a library of new drug analogs. Additionally, these Chiral PVPs have demonstrated catalytic asymmetric desymmetrization/ring closing reactions; these reactions are believed to be unprecedented and can help expand the avenues for drug discovery.

ADVANTAGES:

• Yield: They allow for the synthesis of a wide range of chiral compounds with superior yields
• Range of Products: They can allow for a wide range of chiral reactions, some of which we believe to be unprecedented and can aid in the discovery of new pharmaceutical products
• Cost Reduction: They can reduce the cost of industrial chiral reactions due to their reduced use of reagents, ease of recoverability, long shelf-life, and high-temperature stability (>120oC)
• Non-Toxic: They are non-toxic and hence can be easily interacted with biological entities
• Inexpensive: These Chiral PVPs are easy and inexpensive to produce

APPLICATIONS:

• Drug Discovery: Tool for drug discovery/developing new libraries of drugs
• Commercial Synthesis: Synthesis of bioactive enantiomerically pure molecules
• Drug Delivery and Interactions: Chiral drug delivery, nanodelivery of siRNA and selective interactions with proteins, DNA and RNA