Medicinal/Organic chemist

EDUCATION

National Institute of Pharmaceutical Education and Research (NIPER) Punjab, India

Ph.D. (Medicinal/Synthetic Chemistry)

(Thesis submitted) Degree expected in February 2011

Thesis: Design, synthesis and biological evaluation of quinoline and tricyclic guanidine compounds for anti-HIV activity.

PhD Advisor: Prof. K. K. Bhutani, Director and Head of Department, NIPER

National Institute of Pharmaceutical Education and Research (NIPER) Punjab, India

Master of Science (Pharm.) (Medicinal/Synthetic Chemistry)

GPA: 9.0/10, July 2003-June 2005

Thesis: Synthesis of O-alkylated phloroglucinol derivatives as potential anti-malarial compounds.

Research Advisor: Dr. Inder Pal Singh, Associate Professor, NIPER

University of Pune Maharashtra, India

Bachelor of Pharmacy. July1999-June 2003

N. D. M. V. P. Samaj College of Pharmacy, Nashik, Maharashtra. First Class with 68%.

FELLOWSHIPS AND AWARDS

• Senior Research Fellowship (Council of Scientific and Industrial Research, (CSIR), Ministry of Science and Technology, India), April 2010.

• Senior Research Fellowship (Department of Biotechnology, DBT, Ministry of Science and Technology, India), July 2008.

• Junior Research Fellowship (Department of Biotechnology, DBT, Ministry of Science and Technology, India), July 2006.

• National Eligibility Test (NET) conducted by UGC-CSIR, June 2006.

• Graduate Aptitude Test in Engineering (GATE) conducted by IIT Madras with the percentile core: 97.08 (February 2003).

SPECIALIZATION AND AREA OF RESEARCH INTEREST

• Design and Synthesis of New Chemical Entities (NCE’s) for biological evaluation.

• To explore the functions of biologically active lead structures by modifying them (lead optimization) and enhancing the biological or medical significance with simpler scaffolds designed for ease of synthesis.

• Development of new synthetic methodologies for construction of various heterocyclic ring systems present in natural products.

• Design and development of new reactions, methods, reagents, and strategies that introduce fundamentally novel ways of synthesizing complex molecules of biological or medicinal significance.

• Development of Greener techniques for synthesis.

• Study of Structure Activity Relationship (SAR) of synthesized derivatives for various biological activities.

• Intellectual Property Rights.

TECHNICAL EXPERTISE/SKILLS

• Expertise in setting up of any type of chemical reaction, including anhydrous reactions (e.g. reactions involving butyl lithium and Grignard reagents in large quantity).

• Trained to perform retrosynthetic analysis of natural products and design schemes for their total synthesis.

• Practical skill for designing new series of compounds for synthesis.

• Hands on practice of drying of various solvents for anhydrous reactions.

• Handled various hazardous inflammable chemicals (butyl lithium, Grignard reagents etc).

• Exposure to the various analytical instruments like GC, HPLC, UV, IR, MS, NMR, GC-MS, LC-MS, HRMS.

• Handling of various instruments like IR, UV, HPLC, NMR, LC-MS etc.

• Good experience of purification of synthesized compounds by crystallization, various chromatography techniques like CC, FC, VLC, and Preparative TLC etc.

• Able to search and understand various patents databases like EU, US and others.

• Good knowledge of GMPs, various guidelines like ICH.

• Good knowledge of Intellectual Property Rights (IPR) and practical experience of filing Indian patents.

• Well trained and developed skills to write research papers in peer reviewed journals.

• Performed extraction, isolation, and purification of natural products from plant extracts by column chromatography like VLC, FC, Preparative TLC, and HPLC etc.

• Practical skill for characterization of natural products using various spectroscopic techniques such as IR, UV, MS, 1D NMR, 2D NMR and elemental analysis.

RESEARCH EXPERIENCEWORK EXPERIENCE

NIPER, Department of Natural Products Chemistry (July 2006-present)

Advisor: Prof. K. K. Bhutani Punjab, India

• Achieved total synthesis of various natural products like batzelladine K (marine tricylic guanidine alkaloid), buchapine and related compounds (quinoline alkaloids), 8-hyroxy canthin-6-one and its derivatives (canthin-6-one alkaloids).

• Explored the tricyclic guanidinium core present in batzelladine alkaloids and synthesized various derivatives to evaluate for anti-HIV activity.

• Designed, synthesized and evaluated new series of quinoline 2,4-diol based on anti-HIV natural product buchapine leading to identification of three potent inhibitors of HIV-1.

• Designed, synthesized and evaluated new series of β-carboline derivatives based on anti-HIV natural product butyl harmine and canthinone leading to identification of 1-formyl β-carboline derivatives as potent inhibitor of HIV-1.

• Developed a method for efficient chemo-selective di-alkylation of quinoline 2,4-diol derivatives in water.

• Constructed various heterocyclic ring systems like substituted 3,4-dihydro-β-carboline, β-carboline, quinoline 2,4-diol derivatives etc. present in natural products.

• Established a method for aromatization of 1-methyl-3,4-dihydro-β-carboline-3-carboxylic acid and derivatives accompanied by N-9 alkylation in one-pot.

• Developed a new route for direct synthesis of 3-substituted 3,4-dihydro-β-carboline-3-carboxylic acid derivatives.

• Identified the pharmacophore and established the Structure Activity Relationship (SAR) of quinoline, batzelladines and β-carboline derivatives for anti-HIV activity.

• Wrote and filed two patents of research work in India

• Collected plant materials from the field and prepared various extracts of Piper longum, Asparagus racemosus, Papaver somniferum.

• Assisted in isolation and characterization of various natural products from various parts of plants.

• Supervised and guided master students for designing experiments and conducting their research work.

NIPER, Department of Natural Products Chemistry (July 2003-June 2005)

Advisor: Dr. Inder Pal Singh Punjab, India

• Achieved total synthesis of anti-malarial natural product containing phloroglucinol nucleus (1-(prenyloxy)-4-(3-methyl-butyryl)-2-methyl-3,5-dihydroxybenzene)

• Designed and synthesized various series of phloroglucinol derivatives for anti-microbial activity.

• Developed a method for selective alkylation on phloroglucinol nucleus.

• Identified the pharmacophore essential for anti-microbial activity and established Structure Activity Relationship (SAR).

TEACHING EXPERIENCE

S.N.J.B’s Shriman Sureshdada Jain College of Pharmacy, Nashik, Maharashtra, India.

Department of Medicinal Chemistry. Lecturer (August 2005-July 2006)

Organic chemistry

• Taught the basic and advanced courses of organic chemistry including reaction mechanism, name reactions and rearrangements.

• Prepared teaching materials including problem sets and exams.

• Assisted students individually with homework problems or material they found difficult to understand.

• Evaluated the project work and thesis of undergraduate and master students.

• Supervised and instructed students in organic chemistry techniques. Emphasized keeping complete and accurate scientific notes.

• Supervised and assisted students with multi-step syntheses of compounds designed to teach general laboratory techniques.

• Demonstrated various techniques of organic chemistry practical like crystallization, distillation, filtration etc. to undergraduate students.

• Motivated and guided students to appear for competitive exam.

Medicinal Chemistry

• Lectured the advanced courses of medicinal chemistry including the structure, nomenclature, SAR studies, mechanism of actions, drug interactions of drugs etc.

• Assisted in development of lab curriculum. Updated and revised existing lab assignments.

• Guided students with multi-step syntheses of drugs designed to teach general laboratory techniques.

PUBLICATIONS

1. “Antiprotozoal and antimicrobial activities of O-alkylated and formylated acylphloroglucinols.” S. B. Bharate, S. I. Khan, Nafees. A. M. Y, S. K. Chauthe, M. R. Jacob, B. L. Tekwani, I. A. Khan, I. P. Singh. Bioorg. Med. Chem. 2007, 15, 87–96.

2. “Aromatization and chemoselective alkylation of 1-methyl-3,4-dihydro-β-carboline-3-carboxylic acid and its derivatives.” K. G. Brahmbhatt, N. Ahmed, I. P. Singh, K. K. Bhutani. Tetrahedron Lett. 2009, 50, 5501–5504.

3. “Efficient chemoselective alkylation of quinoline 2,4-diol derivatives in water.” N. Ahmed, K. G. Brahmbhatt, I. P. Singh, K. K. Bhutani. J. Heterocyl. Chem. 2010, DOI: 10.1002/jhet.364.

4. “Synthesis and Anti-HIV Activity of Alkylated Quinoline 2,4-diols.” N. Ahmed, K. G. Brahmbhatt, S. Sabde, D. Mitra, I. P. Singh, K. K. Bhutani. Bioorg. Med. Chem. 2010, 18, 2872-2879. (Among Top 25 most downloadable research papers)

5. “Total Synthesis of ( ) Batzelladine K: A Biomimetic Approach.” N. Ahmed, K. G. Brahmbhatt, I. P. Singh, K. K. Bhutani. Synthesis 2010, 15, 2567-2570.

6. “Synthesis and evaluation of β–carboline derivatives as inhibitors of human immunodeficiency virus.” K. G. Brahmbhatt, N. Ahmed, S. Sabde, D. Mitra, I. P. Singh, K. K. Bhutani. Bioorg. Med. Chem. Lett. 2010, 20, 4416-4419.

7. “Synthesis and evaluation of tricyclic batzelladine K analogues as HIV-1 inhibitors.” N. Ahmed, K. G. Brahmbhatt, S. Sabde, D. Mitra, I. P. Singh, K. K. Bhutani. (Manuscript under preparation).

8. “Total synthesis of 8-hydroxy canthinone and its derivatives.” K. G. Brahmbhatt, N. Ahmed, I. P. Singh, K. K. Bhutani. (Manuscript under preparation).

PATENTS

1. “Novel anti-HIV compounds.” K. K. Bhutani, N. Ahmed, K. G. Brahmbhatt, I. P. Singh, D. Mitra, S. Sabede. Application No.1556/DEL/200*-**-**-****.

2. “Novel alkylated derivatives of quinoline 2,4-diol with anti-HIV activity.” K. K. Bhutani, N. Ahmed, K. G. Brahmbhatt, I. P. Singh, D. Mitra, S. Sabede. Application No.1557/DEL/200*-**-**-****.

PRESENTATIONS

1. “Design and synthesis of canthin-6-one amino acid conjugates for anti-HIV activity.” K. G. Brahmbhatt, V. M. Gohil, N. Ahmed, I. P. Singh, K. K. Bhutani. New Developments on Drug Discovery in Natural Products and Traditional Medicines II (DDNPTM) 20-24 November 2010, NIPER, Mohali, India. (1st Poster Prize Award).

2. “Synthesis of tricyclic guanidine analogues of batzelladine K for anti-HIV activity.” N. Ahmed, K. G. Brahmbhatt, I. P. Singh, K. K. Bhutani. New Developments on Drug Discovery in Natural Products and Traditional Medicines II (DDNPTM) 20-24 November 2010, NIPER, Mohali, India.

3. “Total synthesis of ( ) Batzelladine K and its derivatives for anti-HIV activity.” N. Ahmed, K. G. Brahmbhatt, K. K. Bhutani. ESF-COST High-Level Research Conference on Natural Products Chemistry, Biology and Medicine III, Acquafredda di Maratea, Italy, 5-10 September 2010.

4. “Synthesis of 1-methyl-3,4-dihydro-β-carboline-3-carboxylic acid and 1-methyl-β-carboline-3-carboxylic acid derivatives for anti-HIV activity.” K. G. Brambhatt, N. Ahmed, K. K. Bhutani. Tenth Tetrahedron Symposium, 22-25 June 2010, Peking University, Beijing, China.

5. “Synthesis and Anti-HIV Activity of C-3 Dialkylated derivatives of Quinoline 2,4-diols.” N. Ahmed, K. G. Brahmbhatt, S. Sabde, D. Mitra, I. P. Singh, K. K. Bhutani. Drug Discovery in Natural Products and Traditional Medicines (DDNPTM) Nov. 2008, NIPER, S.A.S. Nagar, Mohali, India.

6. “Design and synthesis of β-carboline derivatives for anti-HIV activity.” K. G. Brahmbhatt, N. Ahmed, S. Sabde, D. Mitra, I. P. Singh, K. K. Bhutani. Drug Discovery in Natural Products and Traditional Medicines (DDNPTM) Nov. 2008, NIPER, S.A.S. Nagar, Mohali, India.

COMPUTER PROFICIENCY

Well trained in using various computer software such as Windows, MS office, Chemistry Softwares such as Chemdraw, Chem3D, Reference management software (End note Plus), Data retrieval from various databases such as SciFinder, Chemical Abstracts, Pubmed, Highwire, STN search, Sciencedirect, Patents databases etc.

ACTIVITIESACTIVITIES

• Registered Pharmacist in Maharashtra state pharmacy council.

• One of the organizer and active participant in the national workshop on “Curriculum development in natural products at postgraduate level” held at NIPER, Mohali (November 2003).

• Successfully completed “General course on Intellectual Property (Distance learning)” conducted by Wipo Worldwide Academy, Geneva, Switzerland (October-November 2006)

• One of the active participants in the international conference on “Drug Discovery in Natural Products and Traditional Medicines (DDNPTM-2008)” held at NIPER, Mohali (November 2008).

• One of the active participants in the 2nd biennial international conference on “Drug Discovery in Natural Products and Traditional Medicines (DDNPTM-2010)” held at NIPER, Mohali (November 2010).

REFERENCES

1. Prof. Kamlesh K. Bhutani

Director and Head of Department of Natural Products, National Institute of Pharmaceutical Education and Research (NIPER), Sector 67, S.A.S. Nagar, Mohali-160062, Punjab, India.

+91-941*******; +91-172*******

*********@*****.**.**

2. Prof. K. P. R. Kartha

Department of Medicinal Chemistry, National Institute of Pharmaceutical Education and Research (NIPER), Sector 67, S.A.S. Nagar, Mohali-160062, Punjab, India.

+91-931*******; +91-172*******

*******@*****.**.**

3. Dr. Inder Pal Singh

Associate Professor, Department of Natural Products, National Institute of Pharmaceutical Education and Research (NIPER), Sector 67, S.A.S. Nagar, Mohali-160062, Punjab, India.

+91-981*******; +91-172*******

*******@*****.**.**

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