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Dr. Rajshekhar Karpoormath

Person

Dr. Rajshekhar Karpoormath

Telephone

 +27(0)31 260 7179

Email

 karpoormath@ukzn.ac.za  

Campus

Westville

Research Interests

Target based Drug design and Synthesis. 
Organic Synthesis and Methodology development Biosensors.

Designation

Senior Lecturer

 Biosketch

Dr. Rajshekhar Karpoormath is currently a senior lecturer in the Discipline of Pharmaceutical Sciences, College of Health Sciences, University of KwaZulu-Natal, Durban, South Africa.
Education and Appointments 
Dr. Rajshekhar Karpoormath was born in Hubli (Karnataka, India) on 02 November, 1975.  He joined the faculty of Pharmaceutical Chemistry, University of KwaZulu-Natal in July 2010.
  • After his secondary education, Rajshekhar was awarded Bachelor of Pharmacy degree from K.L.E. Society’s College of Pharmacy, Belgaum affiliated with Karnataka University, Dharwad, India. 
  • He obtained his M.Pharma degree from Rajiv Gandhi University, Bangalore, India.  
  • In March 2004, he was appointed as lecturer in the Department of Pharmaceutical Chemistry in Dayanand Sagar College of Pharmacy, Bangalore, India.
  • In 2005, he joined National Chemical Laboratory, CSIR, Pune, India as a Senior Research Fellow (June 2005 - July 2006).  
  • From Aug 2006, he joined the School of Chemistry and Physics at the University of KwaZulu-Natal, South Africa for his Doctoral studies. 
  • In July 2010, he joined Department of Pharmaceutical Chemistry, College of Health Sciences, University of KwaZulu-Natal, Durban, as a Faculty.
 
Research Area 
Our current organic/medicinal chemistry work focusses on the design and synthesis of anti-HIV, anti-cancer, anti-tubercular and anti-microbial compounds. SMCRG’s main research areas are:
  • Computer-aided drug design techniques like structure-based and ligand-based design methods.
  • Rational molecular modeling areas starting from virtual screening of ligands, identification of hits and their further optimization to lead compound.
  • Synthesis and evaluation of target-directed anti-HIV, anti-cancer, anti-tubercular and anti-microbial agents.
  • Synthetic Methodology development 
  • Developing electroanalytical sensors to improve current limits of detection, and investigate the analysis of completely new analytes, using a range of novel nanoparticles based electrodes.
 
Publications 
  1. Design and synthesis of VEGFR-2 tyrosine kinase inhibitors as potential anticancer agents by virtual based screening, Harun M. Patel, Pankaj Bari, Rajshekhar Karpoormath, Malleshappa Noolvi, Neeta Thapliyal, Sanjay Surana, Pritam Jain, RSC Advances, (2015), 5, 56724-56771.
  2. AgNO3 catalyzed regio-selective synthesis of 3-Alkyl/Aryl-idene-3,4-dihydro-4-tosyl-2H-1,4-benzoxazine: Novel anti-tubercular scaffolds, Sivanandhan Karunanidhi, Rajshekhar Karpoormath, Milan Bera, Rajesh A. Rane, Mahesh B. Palkar, Journal of Heterocyclic Chemistry (2015), Ahead of Print. (DOI 10.1002/jhet.2472).
  3. Editorial (Thematic Issue: "Discovery and development of new anticancer drugs inspired from natural product leads" Part 1), Rajesh Rane, Rajshekhar Karpoormath, Anticancer Agents in Medicinal Chemistry (2015), 15, 536.
  4. Novel synthetic organic compounds inspired from antifeedant marine alkaloids as potent bacterial biofilm inhibitors, Rajesh A. Rane, Rajshekhar Karpoormath, Shital S. Naphade, Pavan K. Bangalore, Mahamadhanif Shaikh, Girish Hampannavar, Bioorganic Chemistry (2015), 61, 66.
  5. Novel series of coumarinyl substituted-thiazolidin-2,4-dione analogs as anticancer agents: Design, synthesis, spectral studies and cytotoxicity evaluation, Mahesh B. Palkar, Sunil S. Jalalpure, Rajesh A. Rane, Harun M. Patel, Mahamadhanif S. Shaikh, Girish A. Hampannavar, Wesam S. Alwan, Girish S. Bolakatti and Rajshekhar Karpoormath, Anti-cancer agents in medicinal chemistry (2015), Ahead of Print. (DOI: 10.2174/1871520615666150424110339).
  6. A categorical review on electroanalytical determination of non-narcotic over-the-counter abused antitussive drugs, Neeta Thapliyal, Harun Patel, Rajshekhar Karpoormath, Rajendra N. Goyal, Rajkumar Patel, Talanta (2015), 142, 157-163. 
  7. Stereo-selective synthesis, structural and antibacterial studies of novel glycosylated β2,3-amino acid analogues, Pramod Kadam, Rajshekhar Karpoormath, Bernard Omondi, Hafizah Chenia, Deresh Ramjugernath, Neil A. Koorbanally, Medicinal Chemistry Research (2015) (Accepted manuscript).
  8. Synthesis and characterization of Ba0.5Co0.5Fe2O4 nanoparticle ferrites: application as electrochemical sensor for ciprofloxacin, Nadir S. E. Osman, Neeta Thapliyal, Wesam S. Alwan,  Rajshekhar Karpoormath,  Thomas Moyo, Journal of Materials Science: Materials in Electronics (2015), Ahead of Print.( DOI: 10.1007/s10854-015-3036-x).
  9. Epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors from the natural origin: A recent perspective, Harun M. Patel, Rajesh Rane, Neeta Thapliyal, Mahesh Palkar, Mahamadhanif Shaikh, Rajshekhar Karpoormath, Anti-Cancer Agents in Medicinal Chemistry (2015), Ahead of Print. (DOI: 10.2174/1871520615666150312100259). 
  10. Structural insight of glitazone for hepato-toxicity: Resolving mystery by PASS, Harun Patel, Yogesh Sonawane, Rakesh Jagtap, Kiran Dhangar, Neeta Thapliyal, Sanjay Surana, Malleshappa Noolvi, Mahamadhanif S. Shaikh, Rajesh A. Rane, Rajshekhar Karpoormath, Bioorganic & Medicinal Chemistry Letters (2015), 25, 1938-1946.
  11. Design, synthesis and evaluation of small molecule imidazo[2,1-b][1,3,4]thiadiazoles as inhibitors of transforming growth factor-β type-I receptor kinase (ALK5), Harun M. Patel, Baljeet Sing, Varun Bhardwaj, Mahesh Palkar, Mahamadhanif S. Shaikh,  Rajesh Rane, Wesam S. Alwan, Andanappa K. Gadad, Malleshappa N. Noolvi, Rajshekhar Karpoormath, European Journal of Medicinal Chemistry (2015), 93, 599-613. 
  12. Novel imidazo[2,1-b]-1,3,4-thiadiazoles as promising antifungal agents against clinical isolate of Cryptococcus neoformans, Wesam S. Alwan, Rajshekhar Karpoormath, Mahesh B. Palkar, Harun M. Patel, Rajesh A. Rane,  Mahamadhanif S. Shaikh, Afsana Kajee, Koleka P. Mlisana, European Journal of Medicinal Chemistry (2015), 95, 514-525.
  13. Current perspective of natural alkaloid carbazole and its derivatives as antitumor agents, Mahamadhanif S Shaikh, Rajshekhar Karpoormath, Neeta Thapliyal , Rajesh A Rane, Mahesh B Palkar, A M Faya, Harun M Patel , Wesam S Alwan , Kavita Jain , Girish A Hampannavar , Anti-cancer agents in medicinal chemistry (2015), Ahead of Print. (DOI: 10.2174/1871520615666150113105405).
  14. An insight into purine, tyrosine and tryptophan derived marine antineoplastic alkaloids, Mahesh B Palkar, Rajesh A Rane, Neeta Thapliyal , Mahamadhanif S Shaikh , Wesam S Alwan, Kavita S Jain , Sivanandhan Karunanidhi, Harun M Patel , Girish A Hampannavar, Rajshekhar Karpoormath, Anti-cancer agents in medicinal chemistry (2015), Ahead of Print. (DOI:  10.2174/1871520615666150101143520).
  15. Electroanalysis of antitubercular drugs in pharmaceutical dosage forms and biological fluids: A review, Neeta Thapliyal, Rajshekhar V. Karpoormath, Rajendra N. Goyal, Analytica Chimica Acta (2015), 853, 59-76.
  16. Acridone-based antitumor agent: A mini-review, Wesam S. Alwan , Anand A Mahajan, Rajesh A. Rane, Anish A. Amritkar, Shital S. Naphade, Mayur C. Yerigiri, Rajshekhar Karpoormath, Anti-cancer agents in medicinal chemistry (2015), Ahead of Print. (DOI: 10.2174/1871520615666150113104457).
  17. Design and synthesis of novel carbazolo-thiazoles as potential anti-mycobacterial agents using a molecular hybridization approach, Mahamadhanif S. Shaikh, Mahesh B. Palkar, Harun M. Patel, Rajesh A. Rane, Wesam S. Alwan, Mahidansha M. Shaikh, Iqbal M. Shaikh, Girish A. Hampannavar, Rajshekhar Karpoormath, RSC Advances (2014), 4(107), 62308-62320. 
  18. Synthesis and evaluation of novel marine bromopyrrole alkaloid-based derivatives as potential antidepressant agents, Rajesh A. Rane, Shital Napahde, Pavan K. Bangalore, Niteshkumar U. Sahu, Nishant Shah, Yogesh A. Kulkarni, Kalyani Barve, Leena Lokare, Rajshekhar Karpoormath, Chemical Biology & Drug Design (2014), 84(5), 593-602.
  19. Design and synthesis of novel antineoplastic agents inspired from marine bromopyrrole alkaloids, Rajesh A. Rane, Pavan K. Bangalore, Shital S Naphade, Harun M. Patel , Mahesh B. Palkar, Rajshekhar Karpoormath, Anti-cancer agents in medicinal chemistry (2014), Ahead of Print. (DOI: 10.2174/1871520614666141203124745).
  20. Novel series of phenylalanine analogs endowed with promising anti-inflammatory activity: synthesis, pharmacological evaluation, and computational insights, Mahesh B. Palkar, D. M. Praveen, Pradeepkumar M. Ronad, A. H. M. Viswanathswamy, Rajesh A. Rane, Harun M. Patel, Mahamadhanif S. Shaikh, Girish A. Hampannavar, Kavita S. Jain,  Rajshekhar Karpoormath, Medicinal Chemistry Research (2014), Ahead of Print. (DOI: 10.1007/s00044-014-1272-x).
  21. Synthesis of novel amides based on acridone scaffold with interesting antineoplastic activity, Anand A Mahajan, Rajesh A Rane, Anish A Amritkar, Shital S Naphade, Pankaj B Miniyar, Pavan K. Bangalore, Rajshekhar Karpoormath, Anti-cancer agents in medicinal chemistry (2014), Ahead of Print. (DOI: 10.2174/1871520614666141130130130)
  22. Synthesis of novel hybrids inspired from bromopyrrole alkaloids inhibiting MMP-2 and -12 as antineoplastic agents, Rajesh A Rane, Shital S Naphade, Pavan K. Bangalore, Mahesh B Palkar, Harun M Patel, Mahamadhanif S Shaikh, Wesam S Alwan , Rajshekhar Karpoormath, Chemical biology & drug design (2014), Ahead of Print (DOI: 10.1111/cbdd.12481).
  23. Synthesis, in vitro evaluation, and molecular docking studies of azetidinones and thiazolidinones of 2-amino-5-cyclopropyl-1,3,4-thiadiazole as antibacterial agents Harun Patel, Lishu Mishra, Malleshappa Noolvi, Rajshekhar Karpoormath, Swaranjit S. Cameotra, Archiv der Pharmazie (Weinheim, Germany) (2014), 347(9), 668-684.
  24. Synthesis, pharmacological screening and in silico studies of new class of Diclofenac analogues as a promising anti-inflammatory agents, Mahesh B Palkar, Anuj S Singhai, Pradeepkumar M Ronad, A H M Vishwanathswamy, Thippeswamy S Boreddy, Veeresh P Veerapur, Mahamadhanif S Shaikh , Rajesh A Rane, Rajshekhar Karpoormath, Bioorganic & medicinal chemistry (2014), 22(10), 2855-66.
  25. Synthesis of novel 4-nitropyrrole-based semicarbazide and thiosemicarbazide hybrids with antimicrobial and anti-tubercular activity, Rajesh A Rane, Mahesh B Palkar, Mahamadhanif S Shaikh , Shital S Naphade, Pavan K. Bangalore, Rajshekhar Karpoormath, Bioorganic & medicinal chemistry letters (2014), 24(14), 3079-83.
  26. Synthesis and pharmacological evaluation of marine bromopyrrole alkaloid-based hybrids with anti-inflammatory activity, Rajesh A. Rane, Mukesh Nandave, Suresh Nayak, Anushri Naik, Dhwani Shah, Wesam S Alwan, Niteshkumar U Sahu, Shital S. Naphade, Mahesh B Palkar, Sivanandhan Karunanidhi, Neeta Thapliyal, Rajshekhar Karpoormath, Arabian Journal of Chemistry (2014), Ahead of Print. (DOI:10.1016/j.arabjc.2014.06.004).
  27. Synthesis of novel 4-nitropyrrole-based semicarbazide and thiosemicarbazide hybrids with antimicrobial and anti-tubercular activity, Rajesh A. Rane, Shital S. Naphade, Pavan K. Bangalore, Mahesh B Palkar, Mahamadhanif S Shaikh, Rajshekhar Karpoormath, Bioorganic & Medicinal Chemistry Letters (2014), 24(14), 3079-3083. 
  28. Marine bromopyrrole alkaloids: Synthesis and diverse medicinal applications Rajesh Rane, Niteshkumar Sahu, Chetan Shah, Rajshekhar Karpoormath, Current Topics in Medicinal Chemistry (Sharjah, United Arab Emirates) (2014), 14(2), 253-273.
  29. Synthesis and NMR elucidation of pentacycloundecane-derived hydroxy acid peptides as potential anti-HIV-1 agents, Rajshekhar Karpoormath, Fernando Albericio, Thavendran Govender, Glenn E. M. Maguire, Hendrik G. Kruger, Structural Chemistry (2013), 24(5), 1461-1471.
  30. Novel PCU cage diol peptides as potential targets against wild-type CSA HIV-1 protease: synthesis, biological screening and molecular modelling studies, Rajshekhar Karpoormath, Yasien Sayed, Thavendran Govender, Hendrik G. Kruger, Mahmoud E. S. Soliman, Glenn E. M. Maguire, Medicinal Chemistry Research (2013), 22(8), 3918-3933.
  31. Synthesis and NMR elucidation of novel pentacycloundecane-derived peptides Rajshekhar Karpoormath, Oluseye K. Onajole, Tricia Naicker, Thavendran Govender, Glenn E. M. Maguire, Hendrik G. Kruger, South African Journal of Chemistry (2012), 65, 108-114.  
  32. Pentacycloundecane derived hydroxy acid peptides: A new class of irreversible non-scissile ether bridged type isostere as potential HIV-1 wild type C-SA protease inhibitors, Rajshekhar Karpoormath, Yasien Sayed, Patrick Govender, Thavendran Govender, Hendrik G. Kruger, Mahmoud E. S. Soliman, Glenn E. M. Maguire, Bioorganic Chemistry (2012), 40, 19-29.
  33. Benzyl 5-hydroxy-4-oxapentacyclo[5.4.1.02,6.03,10.08,11]dodecane-3-carboxylate Rajshekhar Karpoormath, Tricia Naicker, Thavendran Govender, Hendrik G. Kruger, Glenn E. M. Maguire, Acta Crystallographica, Section E: Structure Reports Online (2011), 67(4), o877.
  34. endo-11-(Dibenzylamino)tetracyclo[5.4.0.03,10.05,9]undecane-8-one, Rajshekhar Karpoormath, Patrick Govender, Thavendran Govender, Hendrik G. Kruger, Glenn E. M. Maguire, Acta Crystallographica, Section E: Structure Reports Online (2011), 67(3), o619, So619-So619/8. 
  35. tert-ButylN-[(11-exo-benzyloxycarbonyl-8 oxopentacyclo[5.4.0.02,6.03,10.05,9] undecane-11-endo-yloxy)carbonylmethyl]carbamate, Rajshekhar Karpoormath, Thavendran Govender, Patrick Govender, Hendrik G. Kruger, Glenn E. M. Maguire, Acta Crystallographica, Section E: Structure Reports Online (2010), 66(10), o2607-o2608.
  36. N,N'-[(8-endo,11-endo-Dihydroxypentacyclo[5.4.0.02,6.03,10.05,9]undecane-8,11-diyl)bis(methylenecarbonyl)]di-L-phenylalanine, Rajshekhar Karpoormath, Patrick Govender, Hendrik G. Kruger, Thavendran Govender, Glenn E. M. Maguire, Acta Crystallographica, Section E: Structure Reports Online (2010), 66(10), o2537-o2538.
  37. exo-8,exo-11-Diallylpentacyclo[5.4.0.02,6.03,10.05,9]undecane-endo-8,endo-11-diol, Grant A. Boyle, Thavendran Govender, Rajshekhar Karpoormath, Hendrik G. Kruger, Acta Crystallographica, Section E: Structure Reports Online (2007), 63(12), o4797, o4797/1-o4797/22. 
  38. exo-8,exo-11-Divinylpentacyclo[5.4.0.02,6.03,10.05,6]undecane-endo-8,endo-11-diol Grant A. Boyle, Thavendran Govender, Rajshekhar Karpoormath, Hendrik G. Kruger, Acta Crystallographica, Section E: Structure Reports Online (2007), 63(10), o3977, So3977/1-So3977/8. 
  39. Synthesis and anti-tubercular activity of a series of 2-sulfonamido/trifluoromethyl-6-substituted imidazo[2,1-b]-1,3,4-thiadiazole derivatives, Andanappa K. Gadad, Malleshappa N. Noolvi, Rajshekhar V. Karpoormath, Bioorganic & Medicinal Chemistry (2004), 12(21), 5651-5659.

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