Drug Development of Biologically Important Natural and Synthetic Molecules

Design and Synthesis of New Anti-osteoporotic Agents Osteoporosis has emerged as leading health care issues worldwide. Osteoporosis is a bone disorder and according to International Osteoporosis Foundation (IOF) Worldwide, more than 8.9 million fractures occur annually, resulting in an osteoporotic fracture every 3 seconds. Considering the wide impact of this disease, we here at CSIR-CDRI developed efficient protocol for the synthesis of natural isoflavonoids (medicarpin and cajanin) and their new derivatives, and demonstrated their differential actions in osteoblasts and parameters of acquisition of PBM in growing female rats (Mol. Cell. Endocrinol. 2010, 325, 101-109; J. Nutritional Biochem., 2012, 23, 27-38; Osteoporosis International, 2012, 23, 1151-1161). We prepared a series of new pterocarpans and showed that they hold therapeutic promise in postmenopausal osteoporosis (US-8686028 dated 01-04-2014). Several New leads were identified as potent osteogenic agents and one of the pterocarpans CDRI-1500 (Pteroheal) significantly stimulated callus formation and increased fracture healing at only 1.0 mg/kg/day dose in adult rats. Pteroheal (CDRI-1500) is currently under development mode and it is found safe in regulatory toxicology and pharmacology studies. Pteroheal is now ready for Licensing and we are looking for industrial partner for further development.

Design and Synthesis of New Anti-diabetic Agents: During the drug development program on the management of diabetes and energy metabolism, we have identified various 6-aryl-2H-pyran-2-one-3-carbonitriles as PPARγ agonists (BMCL 15, 3356-3360, 2005), functionalized acetophenones (BMCL 15, 3394-3397, 2005), annulated benzofurans (BMC 15, 727-734, 2007; MC 4, 18-24, 2008) as novel protein tyrosine phosphatase-1B inhibitors and several nature mimicking furanyl-2-pyranones, 3,4,5-triarylpyrroles and 1,3-teraryls as antihyperglycemic agents (BMCL 14, 1089-1092, 2004; BMCL 17, 2425-2429, 2007; BMCL 19, 2158-2161, 2009). Recently we report discovery of molecular modeling-assisted new biaryl-4-carbonitriles, which exhibited anti-hyperglycemic and anti-dyslipidemic activities in in vitro and in various in vivo animal models (Mol. Cell. Endocrinol. 394, 1-12, 2014).

Chemical Biology and Applied Chemistry:Development of New Organic Fluorescent Probes for Diagnostics, Theranostics and Technological Devices
✓Design and Synthesis of New Organelle Specific Bioimaging Agents


✓Design and Synthesis of New Fluorescent Chemosensors and Chemodosimeters



✓Design and Synthesis of New Donor-Acceptor Based Fluorescent Dyes for Devices



✓Development of New Synthetic Approaches for Privileged Heterocyclic Compounds