Accepted Abstracts: Pharmaceut Reg Affairs
Molecular hybridization is a strategy of rational design of new ligands or prototypes based on the recognition of pharmacophoric sub-units in the molecular structure of two or more known bioactive derivatives. The adequate fusion of these sub-units, lead to the design of new hybrid architecture that maintain pre-selected characteristics of the original template. The natural product bioactives are essential sources for rational design and for hybridization. They offer promising and amazing chemical diversity thereby inspiring the development of, structurally diverse new molecules to play a major role in drug discovery. The promising natural anti-mycobacterials include carbazole alkaloids such as Clausine and Micromeline, isolated independently from several sources and dibenzofuran based on secondary metabolite of lichen Usnic acid isolated from Cladonia substellata, were shown to have moderate antitubercular activity. Modified natural product like synthetic analogues of dibenzofuran and carbazole exhibited significantly improved in vitro as well as in vivo antitubercular activity against M.tuberculosis H37Rv. Structure activity relationship (SAR) studies direct that the presence of dibenzo[b,d]furan or carbazole moiety play a vital role on their pharmacological properties. On the other hand, 1,2,3-triazoles conjugated with a wide range of heterocyclic moieties exhibited potent antitubercular activity. We present here natural product integrated molecular hybrids and their in vitro antimycobacterial activity against Mycobacterium tuberculosis H37Rv.
KANTEVARI SRINIVAS obtained his Ph.D. degree (1996) from Department of Chemistry, Indian Institute of Technology (IIT), New Delhi. He was research associate (1996-97) at National Institute of Immunology (NII) New Delhi. Later he was a post-doctoral Fellow (2001-2003) with Prof. Graham Ellis-Davies at Department of Pharmacology and physiology, Drexel University College of Medicine, Philadelphia, USA and Research Associate (2006-2008) at Department of Neuroscience Mt Sinai School of Medicine, New York, USA. He has been associated with Indian Institute of Chemical Technology (IICT), Hyderabad since 1997 and presently he is Sr. scientist. His research interests are in the area of Fragment based, receptor targeted approaches for drug design and discovery and the development of new photolabile compounds to control cellular chemistry. Presently 7 students are working for Ph.D. and 4 students for Master?s dissertation work. He has 56 Publications and 5 patents for his credit. He is an editorial board member for open Journal of catalysis, member, and editorial board of reviewers for ARKIVOC, and expert reviewer for various journals international reputation. He was also developed several processes for APIs and drug molecules of interest and involved in transferring the technologies.