APARNA KASANI
Email: kasaniaparna@hotmail.com
EMPLOYMENT
Group Leader, NAEJA Pharmaceutical Inc., Canada. June 2007-Current
(working as a full time employee for Pfizer Global Research & Development)
Leading a group of scientists in medicinal chemistry lead optimization project.
Involved in the structure activity relationship studies and parallel synthesis.
Solved key chemistry problems and developed several small drug like molecules
Senior Research Scientist, NAEJA Pharmaceutical Inc., Canada July 2004-June 2007
(worked as a full time employee for Pfizer Global Research & Development)
Performed lead optimization of two chemical series (pyrazole and isoxazole) in dermatology project and evaluated SAR data in collaboration with Pfizer.
Developed new chemical entities (several piperazine lactams, lactones, benzofurans, and indoles) as dopamine partial agonist in the treatment of CNS Schizophrenia disease, and its structure activity relationship.
Several imidazopyridine, benzimidazole and imidazopyrimidine series of compounds were synthesized. Several key chemistry problems were solved. This lead to two candidate compounds as antihypertensive agents
Research Scientist, NAEJA Pharmaceutical Inc., Canada Feb 2002- June 2004
(worked as a Full time employee Pfizer Global Research & Development)
Synthesized analogues of Aliskiren (antihypertensive agent) involving several steps and solved key chemistry problems.
Developed novel chemotypes using structure based drug design. Resulted in two new series (amino pyrimidine and piperazinone based renin inhibitors) of lead generation for cardiovascular disease.
Performed lead optimization and evaluation of Structure-Activity relationship (SAR). Identified small molecules with improved properties (100 fold improvement in efficacy).
Some of the results were disclosed in 3 publications and few conference abstracts.
Successfully completed UCSD intensive medicinal chemistry course.
Research Associate, Department of Chemistry, University of Alberta, Canada Jan 2000- Feb 2002
Post-Doctoral Associate, Department of Chemistry, University of Alberta, June 1998-Jan 2000
Mentor: Professor Ronald G. Cavell (Sponsored by NOVA Chemicals, Calgary, and NSERC, Canada)
Synthesised novel organo phosphorus-nitrogen compounds and their metallorganic compounds
Developed organometallic catalysts for olefin polymerization
Some of these compounds were active catalysts for polymerization of olefins and in this regard, five US patents were filed.
Post-Doctoral Associate, Department of Chemistry, University of Ottawa, April 1996-June1998
Mentor: Professor Sandro Gambarotta (Sponsored by NSERC Canada)
Synthesized organometallic compounds containing bulky amides and aryloxides.
Activation of small molecules (Ethylene, RNCO etc.) were explored.
Supervised several undergraduates and graduates within the research group.
EDUCATION
Ph. D., Chemistry, Indian Institute of Science, Bangalore, India, 1996
M. Sc., Chemistry, Hyderabad Central University, Hyderabad, India, 1990
B. Sc., Osmania University, Hyderabad, India, 1988
AWARDS
Pfizer Recognition for outstanding performance and lasting contribution on Pfizer-Naeja medicinal chemistry collaboration 2005.
Pfizer Recognition of Excellence Award to CNS group, Naeja Pharmaceuticals Inc. from Pfizer Global Research and Development, Ann Arbor Labs, Naeja Pharmaceuticals Inc, 2004.
Pfizer Recognition of Excellence Award to Cardiovascular Group, Naeja Pharmaceuticals Inc. from Pfizer Global Research and Development, Ann Arbor Labs, 2002.
Dr. J. C. Ghosh Medal for the best Ph.D., thesis, Indian Institute of Science, Bangalore, India 1996.
Council of Scientific and Industrial Research (CSIR), New Delhi, India, Senior Research Fellowship (1993 - 1996).
Council of Scientific and Industrial Research (CSIR), New Delhi, India, Junior Research Fellowship (1991 -1993).
PUBLICATIONS
1. Cardiovascular agents: Renin Inhibitors and factor Xa Inhibitors, Aparna Kasani, Rajendra Subedi, Michael stier, Daniel Holsworth and Samarendra Maiti, Heterocycles, 2007, Accepted for publication (Review article).
2. Discovery of 6-ethyl-2,4-diaminopyrimidine-based small molecule renin inhibitors Daniel D. Holsworth, Mehran Jalaie, Thomas Belliotti, Cuiman Cai, Wendy Collard, Suzie Ferreira, Noel A. Powell, Michael Stier, Erli Zhang, Pat McConnell, Igor Mochalkin, Michael J. Ryan, John Bryant, Tingsheng Li, Aparna Kasani, Rajendra Subedi, Samarendra N. Maiti, and Jeremy J. Edmunds, Bioorg. Med. Chem. Lett., 17, 2007, 3575-3580.
3. Ketopiperazine-based renin inhibitors: Optimization of the C ring , Daniel D. Holsworth, Cuiman Cai, Xue-Min Cheng, Wayne L. Cody, Dennis M. Downing, Noe Erasga, Chitase Lee, Noel A. Powell, Jeremy J. Edmunds, Michael Stier, Mehran Jalaie, Erli Zhang, Pat McConnell, Michael J. Ryan, John Bryant, Tingsheng Li, Aparna Kasani, Eric Hall, Rajendra Subedi, Mohammad Rahim and Samarendra Maiti, Bioorg. Med. Chem. Lett., 16, 2006, 2500-2504.
4. First Group 4 Biscarbene complex, K. Aparna, R. P. Kamalesh Babu, R. McDonald, R. G. Cavell, Angew. Chem., Int. Ed. Engl ., 2001, 40, 4400 4402.
5. Transition metal free Ziegler-Natta type catalysts for Olefin polymerization Novel aluminum methandiide complexes, K. Aparna, Q. Wang, R.G. Cavell, J. Mol. Catalysis ., 2001 , ( Invited Article , In Press).
6. Monomeric alkalimetal (Li, Na, K) complexes of Bis(iminophosphorano)methanides. R. P. Kamalesh Babu, K. Aparna, R. McDonald, R. G. Cavell, Organometallics ., 2001,20, 2001, 1451-1455.
7. Early transition metal and Lanthanide bis(iminophosphorano)methandiide complexes; pincer and bridging bisphosphorus metal carbenes. R. G. Cavell, R. P. Kamalesh Babu, K. Aparna, J. Organomet. Chem ., 2001,617-618, P158-169( Invited Review ).
8. Dimeric bridged and chelated alkali metal (Li and Na) Bis(iminophosphorano)methanide complexes with contrasting structures. R. P. Kamalesh Babu, K. Aparna, R. McDonald, R. G. Cavell, Inorg. Chem .,39, 2000,4981-4984.
9. Carbon-Carbon double bond formation reactions of the unique spirocyclic aluminum bis(iminophosphorano)methandiide complex: Insertion of heteroallenes into aluminum-carbon bonds. K. Aparna, R. McDonald, R.G. Cavell, J. Am. Chem. Soc .,122,2000, 9314-9315
10. A Monomeric Samarium Bis(Iminophosphorano) Chelate Complex with a Sm=C bond. K. Aparna, M. Ferguson, R. McDonald, R.G. Cavell, J. Am. Chem. Soc .,122, 2000, 726-727.
11. Novel alkyl aluminum complexes of bis(iminophosphorano)methanide and methanediide. K. Aparna, M. Ferguson, R. McDonald, R.G. Cavell, Organometallics ,18, 1999, 4241-4243.
12. Chromium bis(phosphoranimine) complexes; bridging carbenes with no CO or Cp supporting ligands. K. Aparna, R. McDonald, R.G. Cavell, J. Chem. Soc., Chem. Commun., 1999, 1993-1994.
13. Structure and Reactivity of a Methyl Zinc Bis(iminophosphorano)methanide Chelate Complex. K. Aparna, R. McDonald, R.G. Cavell, Organometallics ,18, 1999, 3775-3777.
14. Novel Metal-Carbon Multiply-bonded twelve electron complexes of Titanium and Zirconium supported by a bis(phosphoranimine) chelate. R. G. Cavell, R. P. Kamalesh Babu, K. Aparna and R. McDonald, J. Am. Chem. Soc .,121, 1999, 5805-5806.
15. [Ph2P=NSiMe3]2CLi2: A dilithium dianionic methanide salt with an unusual Li4C2cluster structure. K. Aparna, R. P. Kamalesh Babu, R. McDonald and R. G. Cavell, Angew. Chem., Int. Ed. Engl .,38, 1999, 1483-1484.
16. Synthesis and characterization of manganese amidinate complexes and their reactions with dioxygen. K. Aparna, R. P. Kamalesh Babu, S. Gambarotta and G. Yap, Chem. Eur. J .,5, 1999, 577-586.
17. The reactions of di- and trivalent chromium amides with dioxygen. R. P. Kamalesh Babu, K. Feghali, I. Kovacs, K. Aparna, S. Gambarotta and G. Yap, J. Chem. Soc., Dalton Trans., 1998 , 1595-1605.
18. The reduction of Nb2Cl6(TMEDA)2by R2NLi, formation of diamagnetic niobium(II) cluster with short Nb-Nb triple bond and amide C-N bond cleavage. M. Tayebani, K. Aparna, K. Feghali, S. Gambarotta and C. Bensimon, J. Chem. Soc., Chem. Commun ., 1997, 2001-2002.
19. Zirconium alkyl and borohydride complexes stabilized by [3,5-Me2PhN(Ad)Li.Et2O] ( L ) ligation - crystal structures of ZrMe L 3 and Zr(BH4) L 3. K. Aparna, S. Gambarotta and C. Bensimon.Can.J. Chem., 75, 1997, 1494-1499.
20. Amino acid-lanthanide interactions:Crystalstructures of lanthanide and Calcium complexes of Acc6. K. Aparna, S. S. Krishnamurthy, M. Nethaji and P. Balaram. Polyhedron, 16, 1997, 507-512.
21. Synthetic, spectroscopic and structural studies on uranium and thorium complexes of diphosphazane dioxide ligands. K. Aparna, S. S. Krishnamurthy and M. Nethaji, J. Chem. Soc.,DaltonTrans., 1995, 2991-2997
22. Synthetic spectroscopic and structural studies on lanthanide complexes of diphosphazane dioxide ligands. K. Aparna, S. S. Krishnamurthy and M. Nethaji, Z. Anorg. Allg. Chem., 621, 1995, 1913-1921.
23. Diphenylantimony(V) oxo/chloro carboxylate and phosphinates, crystal structures of [SbPh2Cl{O2P(C6H11)2}]2O and [SbPh2(O2CPh)2]2O. Musa A. Said, K. C. Kumara Swamy, R. P. Kamalesh Babu, K. Aparna and M. Nethaji, J. Chem. Soc.,DaltonTrans., 1995, 2151-2157.
24. Synthetic, spectroscopic and crystallographic studies of heterofunctional diphosphazane ligands. R. P. Kamalesh Babu, K. Aparna, S. S. Krishnamurthy, M. Nethaji, Phosphorus, Sulfur and Silicon, 103, 1995, 39-53.
25. Peptide-lanthanide interactions:Crystalstructure of a europium(III)-tryglycine complex. K. Aparna, S. S. Krishnamurthy, M. Nethaji and P. Balaram, Int. J. Peptide Protein Res., 43, 1994, 19-22.
26. Amino acid-lanthanide interactions: Crystal structures of lanthanide complexes of a-amino isobutyric acid (Aib), [La2(Aib)4(H2O)8](ClO4)6and [Pr2(Aib)4(H2O)8]Cl6.H2O. K. Aparna, S. S. Krishnamurthy, M. Nethaji and P. Balaram, Polyhedron , 13, 1994, 2993-2997.
PATENTS
1. Novel Aluminum complexes for olefin polymerization. K. Aparna, R. G. Cavell and Q. Wang. US Patent (Application filed, 2000).
2. Phosphorus supported carbene transition metal complexes. R. P. Kamalesh Babu, K. Aparna, R. G. Cavell and Q. Wang US Patent (Application Serial No.09/174782 October 22, 1998).
3. Phosphineimine complexes of transition metals and Catalysis. R. G. Cavell, Q. Wang, R. P. Kamalesh Babu, K. Aparna, US Patent , 6,313,331 B1, Issued Nov 6, 2001.
4. Aluminum complexes for olefin polymerization. R. G. Cavell, Q. Wang, R. P. Kamalesh Babu, K. Aparna,US Patent 6,235,919 B1, Issued May 22, 2001.
5. Carbene Transition Metal Catalysts, R. G. Cavell, Q. Wang, R. P. Kamalesh Babu, K. Aparna, US Patent, 6,060, 568 Issued May 9, 2000.
CONFERENCE PRESENTATIONS/PARTICIPATIONS
1. 91st Canadian Chemistry Conference & Exhibition at Shaw Conference Center, Edmonton, May 28, 2008
2. Chemistry of Novel Alkyl Aluminum Bis(iminophosphorano)-methanide and -methanediide Complexes, K. Aparna and R. G. Cavell, oral presentation,Canadian Society of Chemistry (CSC2000), May2000, Calgary, Canada.
3. New early metal complexes of anionic bis(iminophosphorano)methane ligands: Metal-nitrogen and novel metal-carbon interactions,219thACS National Meeting,San Francisco, March 26-30, 2000
4. Novel Aluminum and Zinc Bis(iminophorphorano)methanide complexes. K. Aparna and R. G. Cavell, oral presentation,218thACS National Meeting,New Orleans, August 22-26, 1999 .
5. New dilithium methanide reagent and new group 4 (Ti, Hf, Zr) heterocarbenes supposted by bis(iminophosphorano) ligands, R.G. Cavell, R. P. Kamalesh Babu, K. Aparna,217th ACS National Meeting,Anaheim, March 21-25,1999
6. K. Aparna, XIVth International Conference on Phosphorus Chemistry, July 1998, Cincinnati, Ohio, USA.
7. K. Aparna , S. Gambarotta, Chromium amide/aryloxide complexes and their oxidative addition reactions,Inorganic Discussion Weekend, October 1997, University of Toronto, Canada.
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