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Greener Synthetic Aternatives to
Pharmaceutically And Industrially Important Compounds Prof. (Dr.) Anshu Dandia
Department of Chemistry, University of Rajasthan, Jaipur-302004, India Mob: 9414073436; Email: dranshudandia@yahoo.co.in
Heterocycles have a central position in organic chemistry and nitrogen heterocycles in particular exhibit diverse biological and harmacological activities due in part to the similarities with many natural and synthetic molecules with known biological activity. Heterocyclic spiro compounds exhibiting structural rigidity because of conformational restriction are of interest in synthetic organic chemistry. Indeed, the presence of a spiro carbon atom induces a relatively large steric strain and allows basic, acidic, thermal or photopromoted rearrangement of these products, yielding new and often unexpected heterocycles. Therefore, the synthesis of these spiro embraced structures was of considerable interest in the pharmaceutical and agricultural chemistry. Further, the introduction of fluorine into biological molecules often results in significant changes in their chemical, physical, and biological properties.
Creation of molecular complexity and diversity from simple substrates, with simultaneous consideration of the economic and environmental aspects, constitutes a great challenge in modern organic chemistry, both from academic and industrial points of view. In this context, green chemistry can be an important key in order to produce cleaner and efficient synthetic processes. In view of our interest on molecular diversity and search for new leads in drug designing program, aimed at achieving simple and environmentally compatible synthetic methodologies, we have synthesized wide variety of fluorinated novel spiro and annulated heterocycles and biologically important scaffolds incorporating pyrimidine, triazole, pyrazole, benzothiazole, benzimidazole nuclei, etc. by coupling non-conventional strategy with greener solvents or catalysts. In an effort to optimize the processes, a wide range of different solvents and catalysts were investigated and in most of the cases the best solvent was found to be water with catalytic amount of L-proline and PTC. Chemo/regio/diastereoselectivity was also observed in some cases which was confirmed by single crystal X-ray crystal determination.
Phototoxicity and cytotoxity of representative compounds were studied against leukemia and adenocarcinoma-derived cell lines in comparision to the normal human karatinocytes and it was found that phototoxicity of compounds is higher in the tumor cell lines in comparision to the normal ones (NCTC 2544). Anti tubercular activity of some spiro derivatives were studied against Mycobacterium tuberculosis H37Rv in BAVTEC 460 radiometric system. These compounds were effective against M. tuberculosis and showed 90-95% inhibition. Detailed synthetic procedureand pharmacological activities of these compounds will be presented in conference.
References; A. Dandia, R. Singh, S. Bhaskaran, Ultrasonics Sonochemistry. In press, 2009; A. Dandia, K. Arya, Bioorg. Med. Chem. Lett. 18, 2008, 114; A. Dandia, R. Singh, S. Khaturia, J. Fluorine Chem. 128, 2007, 524; A. Dandia, R. Singh, S. Khaturia, Bioorg. Med. Chem. 14, 2006, 1303; A. Dandia, R. Singh, P. Sarawgi, Org. Prep. and Proce. Int. 37, 2005, 397; A. Dandia, K. Arya, M. Sati, S. Gautam, Tetrahedron 60, 2004, 5253; A. Dandia, M. Sati, K. Arya, A. Loupy, Green Chem. 4, 2002, 599.
Contribution of Jaina Mathematicians
Dr. (Mrs.) Padmavathamma, M Sc, Ph D
Professor of Mathematics (Retired), Department of Studies In Mathematics University of Mysore, Manasagangotri Mysore-570 006 Mob: 9845938749; E-mail: Padma_vathamma@yahoo.com
Mathematics is one of the important branches of Science from time immemorial. Being an inseparable part of science, it has retained its privileged place as Queen of all Sciences. The contribution of Indian mathematicians towards the development of mathematics is unique and valuable. Many Jaina mathematicians have saliently contributed. It is perceived among common people that mathematics is difficult to learn. The skill of explaining such difficult material in simple and exact forms is one of the specialties of Jaina mathematicians. Tattvarthadhigama Sutra, Sthananga Sutra, Jambudvipa Prajnñapti, Tiloyapannatti, Ksetrasamasa, Ganitasarasangraha and Vyavaharaganita are important ancient Jaina mathematical works. The object of this paper is to present some of these works.
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