Have interest in drug design, synthesis and technology development of drugs. Among the approaches being followed in drug designing include the modifications of natural products to incorporate pharmacophores for dual activities for efficient management of complex diseases like metabolic syndrome, anti-metabolite approach for infectious diseases and pro-drug synthesis.

A product, 16-dehydro-pregnenolone with generic name CENTATIN has completed phase III human trial as lipid lowering and further trials in combination with Atorvastatin are being followed by Cadila Pharma, Ahmedabad (US Patent 6,579, 862 B1, 2003; US Patent 6, 875, 758, 2005; European Patent 1 020 191 A1 1999). It binds with the farnesoid X receptor (FXR) on hepatic membrane to antagonize the salvage of bile acids, cholesterol metabolites as a result these metabolites are excreted into faeces (Molecular Endocrinology 16, 1590, 2002). The delineation of FXR antagonistic activity in CENTATIN which has no functional groups of bile acids has been well cited in journal of medicinal chemistry (J. Med. Chem. 48, 5383, 2005). In 2008 September, we received ‘CSIR Technology Award’ for this innovation. In continuation with above chemistry of pregnane series, we completed a novel process of Guggulsterone (US Patent 7, 365, 218 B2, 2008; UK Patent GB 2412373 B, 2007). All the above works were carried out to find a synthetic substitute for ‘Gugulipid’. However, we continued our work to establish newer activities in Gugulipid to promote it as treatment for life style diseases and established its anti-dementia effect (US Patent 6, 896, 901 B2, 2005). The work was sponsored by Monsanto, a US company.

Stimulation of ß3 adrenoceptors by selective agonists improves insulin action and stimulates energy metabolism (thermogenesis) in various rodent models of obesity and type 2 diabetes. This led us to amalgamate pharmacophore for ß3 adrenoceptor with flavones and chalcones which are natural antioxidants present in fruits and vegetables as oxidative stress has been implicated as causal factor of vascular complications in diabetes. Few compounds have exhibited significant antidiabetic activity (Bio-org. Med. Chem. 12, 883-889, 2004; Bio-org. Med. Chem. Lett. 17, 799-802, 2007). We are currently in the process of following few selected molecules for the drug development (Patent Appl. US 11,018,923, 2004; US 11, 052, 833, 2005; US 12, 376, 909, 2009).

In the area of anti-metabolite, we have prepared various acyclic and furanoside analogs of purine, pyrazolo[3,4-d] pyrimidine and their isosteres to follow their anti-leishmanial activity, a neglected disease. A simple pyrazolo [3, 4-d] pyrimidine nucleoside has been found to inhibit amastigotes proliferation by ~ 95% in hamsters (Nucleosides, Nucleotides & Nucleic Acids 25, 55-60, 2006). We had also developed a very good process for nucleoside drug Acyclovir which was handed over to Ranbaxy laboratories.

A novel process of conversion of quinine to quinidine was developed and process handed over to Tamilnadu Government to avoid deforestation of Cinchona plantation (Research & Industry 30, 181, 1985). Quinidine is now widely used as organic catalysis for asymmetric induction. Pursuing our interest in technology development we developed a process for Primaquine Diphosphate and prepared its pro-drug (Elubaquine) which was developed as a drug and marketed by Piramal Health Care.

CDRI Technology Award 1994