Dr. Parthasarathi Das

Medicinal Chemistry Division
CSIR - Indian Institute of Integrative Medicine,Canal Road, Jammu – 180001
Email: partha@iiim.ac.in

Positions Held  
Position Held Date Organization
Principal Scientist Since 2012 CSIR-IIIM
Scientist Fellow 2011- 2012 CSIR-IIIM
Research Investigator 2007-2011 Aurigene Discovery Technologies Ltd
Principal Scientist 2004-2007 Dr. Reddy’s Laboratories Ltd
Postdoctoral Fellow 2002-2003 Chemistry and Chemical Biology, Harvard University,  USA.  
Researcher 2000-2002 Graduate School of Science, Tohoku University, Japan
Postdoctoral Fellow 1999-2000 Inst. of Organische Chemie der RWTH Aachen, Germany.

Awards and Fellowships

  • Harvard  University Postdoctoral Fellowship , USA.

  • CREST-Japan Science  & Technology  Postdoctoral Fellowship, Japan

  • Graduiertenkollegs- DFG Fellowship, Germany

  • CSIR Research Fellowship, India .

  • GATE-1993, India

Membership
  • Chemical Research Society of India (CRSI), Bangalore, India

  • Indian Society of Chemists and Biologist (ISCB), Lucknow, India.

Research Area

Catalysis

Our research is focused on the discovery of new catalytic, systems for organic synthesis that utilize the power of transition metal catalysts. Our goal is to enable greater efficiency and novel bond constructions in the synthesis of medicinally important heteroaromatics, with applications that extend to natural product synthesis, drug discovery and process chemistry. The development of these methods also provides a platform for mechanistic investigations, which will enable insight into questions of fundamental reactivity and catalyst design.

 

Total Synthesis

While complex architecture and dense functionality draw our attention to select natural products, with interesting biological activities. Pharmaceutical companies waning interest in natural products reflects the difficulties and costs associated with their synthesis and subsequent structure-activity relationship (SAR) studies. This offers academics the opportunity to develop novel chemical strategies in the context of various therapeutic areas.

Medicinal Chemistry

Infections caused by Gram negative bacteria constitute a major unmet medical need, particularly in the hospital setting, where Gram negative pathogens account for 61% of the infections. Gram-negative bacteria possess an additional outer membrane decorated with lipopolysaccharide (LPS). LPS is composed of three distinct units. The outermost unit is the O-antigen, which is a glycan polymer. This is linked to a sugar-containing core domain which is appended to the membrane anchoring group, lipid A (endotoxin). This outer membrane provides a substantial protective barrier, and Gram-negative bacteria lacking lipid A are either not viable or are highly susceptible to a range of anti-infective drugs, suggesting that enzymes involved in lipid A production could represent new drug targets. Nine unique enzymes catalyze the synthesis of lipid A and UDP-3-O-(R-3-hydroxymyristol)-N-acetylglucosamine deacetylase (LpxC) is a cytosolic zincmetalloamidase responsible for carrying out the second biosynthetic step. The essential role LpxC plays in the biosynthesis of lipid A, coupled with a lack of homology with mammalian proteins, has catalyzed efforts to identify small molecule LpxC inhibitors for the treatment of serious Gram-negative infections.

Publications
  • Rao, D. N.; Rasheed, S.k.; Das, P. Palladium/ Silver Synergistic Catalysis in Direct Aerobic Carbonylation of C(sp2)−H Bonds Using DMF as a Carbon Source: Synthesis of Pyrido-Fused Quinazolinones and Phenanthridinones Org. Lett. (2016); (DOI: 10.1021/acs.orglett.6b01292).
  • Kannaboina, P.; Kumar, K. A. ; Das, P. Site-Selective Intermolecular Oxidative C-3 Alkenylation of 7-Azaindoles at Room Temperature . Org. Lett.(2016) 18, 900-903 (DOI: 10.1021/ol4027478).

  • Rao, D.N.; Rasheed, S.k.; Kumar, K. A.; Reddy, A. S.; Das,P. Copper-Catalyzed CNH2 Arylation of 2-Aminobenzimidazoles and Related C-Amino-NH-azoles. Adv. Synth. Catal. (2016). (DOI: 10.1002/adsc.201600035).
  • Rasheed, Sk. ; Rao, D. N.; Das, P. Copper-Catalyzed Inter- and Intramolecular C−N Bond Formation: Synthesis of Benzimidazole-Fused Heterocycles. J. Org. Chem. (2015), 80, 9321−9327 (DOI: 10.1021/acs.joc.5b01396)
  • Kumar, K.A .; Kannaboina, P.; Dhaked, D. K. ; Vishwakarma, R.A.; Bharatam, P.V. ; Das, P. Cu-catalyzed arylation of the amino group in the indazole ring: regioselective synthesis of pyrazolo-carbazoles. Org. Biomol. Chem. ( 2015), 13, 1481-1491 (DOI: 10.1039/c4ob02044h) K.
  • Reddy, K. R.; Reddy, A. S.; Dhaked, D. K.; Rasheed, S. K.; Pathania, A.S.; Shankar, R. ; Malik, F.; Das,P. Palladium-catalyzed arylation of 2H-chromene: a new entry to pyrano[2,3-c]carbazoles. Org. Biomol. Chem.(2015), 13, 9285-9293 (DOI: 10.1039/c5ob01295c.).
  • Reddy, K. R. ; Reddy, A. S.; Shankar, R.; Kant, R.; Das, P . Copper-Catalyzed Oxidative C-H Amination: Synthesis of Imidazo[1,2-a]-N-Heterocycles from N-Heteroaryl Enaminones. Asian J. Org. Chem. (2015), 4, 573-583 (DOI: 10.1002/ajoc.201500052).
  • Khajuria, R.; Kannaboina, P.; Kapoor, K. K. ; Gupta, A.; Raina, G .; Jassal, A. K.; Rana, L. K.; Maninder , H. S.; Das, P. Divergent synthesis of 4, 6-diarylated pyridin-2(1H)-ones from chalcones: novel  access to 2,4,6-triaryl pyridines. Org. Biomol. Chem. (2015), 13, 5944-5954 (DOI: 10.1039/c5ob00545k).
  • Rao, D. N.; Rasheed, S.k. ;Vishwakarma, R.A.; Das, P. Copper-catalyzed sequential N-arylation of C-amino-NH-azoles. Chem. Commun. (2014), 50, 12911-12914 (DOI: 10.1039/c4cc05628k).
  • Kannaboina, P.; Kumar, K.A.; Aravinda, S.; Vishwakarma, Ram A. ; Das, P. Direct C‑2 Arylation of 7‑Azaindoles: Chemoselective Access to Multiarylated Derivatives. Org. Lett. (2013), 15, 5718-5721 (DOI: 10.1021/ol4027478).

Research Group

Sno.
Student Name
Research Area
1
D. Nageshwar Rao

Cu-catalyzed N-arylation strategies for the synthesis of Medicinally important novel nitrogenated heterocyles Synthesis of novel heterocyclic scaffolds via Transition-metal catalyzed and/or metal free C-H activation/functionalization of C(sp2)-H bonds
Multi step synthesis of bio-active compounds

2
SK. Rasheed

Cu-catalyzed N-arylation and synthesis of heterocycles Transition-metal catalyzed cross-coupling reaction to synthesis of bioactive scaffolds
Total synthesis of natural product

3
Prakash Kannaboina

Transition-metal catalyzed C-H activation/functionalization of azaindole system
Transition-metal catalyzed C-F bond formation and late stage SAR

4
K. Ranjith Reddy

Cu-catalyzed C-H amination and synthesis of novel heterocycles
Synthesis of heteroaromatics under metal-free conditions
Medicinal Chemistry
Total synthesis of natural product

5
K. Anil Kumar

Transition metal-catalyzed N-arylation of various multinucleophilic sites containing heterocycles and synthesis of medicinally important heterocycles
Transition-metal catalyzed C-H activation/functionalization of heteroaromatics

6
A. Siva Reddy

Cu-catalyzed N-arylation of multiple nucleophilic centres
Total synthesis of marine natural products
Medicinal Chemistry

7
Gaurav Raina

Transition-metal catalyzed C-H activation/functionalization
Synthesis of bio-active novel heterocycles via transition-metal catalyzed N-arylation