Synthetic chemist

PREETPAL SINGH SIDHU

Department of Medicinal Chemistry and Institute for Structural Biology and Drug Discovery

Virginia Commonwealth University, Richmond, VA

Ph. 804-***-****

E-mail *******@***.***

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

EDUCATION

Bachelor of Pharmacy (2006) Rajiv Gandhi University of Health Science, India

Doctor of Philosophy (2011) Dept. of Medicinal Chemistry, Virginia Commonwealth University

Thesis title: Designing Allosteric Inhibitors of Thrombin

Advisor: Dr. Umesh Desai

Post Doctoral Fellow (Present) Dept. of Medicinal Chemistry, Virginia Commonwealth University

Advisor: Dr. Umesh Desai

CERTIFICATION

• Industry Diploma in Contract Research & Clinical Trial (2006)

• Certificate in Pharmaceutical Patents (2006)

• Lean Six Sigma (Present)

AWARDS AND HONORS

• AAiPS 2009 Student Scholar Award Recognition of excellence in graduate research and education by American Association of Indian Pharmaceutical Scientists

• 2010 Graduate School Mentorship Award Recognition for mentorship in graduate school mentorship program at Virginia Commonwealth University

WORK EXPERIENCE

Department of Medicinal Chemistry, Virginia Commonwealth University, Richmond

• Post Doctoral Fellow Nov 2011 - Present

• Graduate Research Assistant Aug 2011 - Nov 2011

• Graduate Teaching Assistant Aug 2008 - Aug 2011

• Graduate Research Assistant Jan 2008 - Jun 2008

INVENTION DISCLOSURE

• Sulfated benzofurans as anticoagulants. UR Desai, Q Zhou, PS Sidhu; VCU Invention (Nov, 2011).

PUBLICATIONS

1. Rational Design of Potent, Small, Synthetic Allosteric Inhibitors of Thrombin. Preetpal S. Sidhu, Aiye Liang, Akul Y. Mehta, May A. Hamdy, Qibing Zhou and Umesh R. Desai. J. Med. Chem. 2011, 54(15), 5522-5531.

2. First Step in Synthetic, Allosteric, Direct Inhibitors of Thrombin and Factor Xa. Jenson Verghese, Aiye Liang, Preetpal S. Sidhu, Qibing Zhou, Michael Hindle, and Umesh R. Desai. Bioorg. Med. Chem. Letters, 2009, 19(15), 4126.

3. Identification of Novel Binding Site for Allosteric Regulation of Thrombin. Preetpal S. Sidhu, May A. Hamdy Aiye Liang, Philip D. Mosier, Qibing Zhou, David H. Farrell and Umesh R. Desai. Submitted to J. Med. Chem.

MANUSCRIPT IN PROGRESS

1. Exploring Larger Chemical Space to Design Small, Aromatic, Sulfated Allosteric Modulators of Thrombin. Preetpal S. Sidhu, Aiye Liang, Qibing Zhou and Umesh Desai. Manuscript ready for submission to Bioorg. Med. Chem. Letters

2. An Efficient Synthesis of Highly Functionalized Benzofuran Ring in One Step. Preetpal S. Sidhu, Qibing Zhou and Umesh R. Desai. Manuscript ready for submission to Tetrahedron Letters

3. Synthesis and Biochemical Studies of 2nd Generation Benzofuran Based Allosteric Modulator of Thrombin.Preetpal S. Sidhu, May A. Hamdy, Akul Y. Mehta, Qibing Zhou and Umesh R. Desai. Manuscript ready for submission to J. Med. Chem

POSTER AND ORAL PRESENTATIONS

1. SERMAC-2011, Design & Synthesis of Allosteric Inhibitors of Thrombin, ACS Regional Meeting, Richmond, VA.

2. Virginia Academy of Science-2011, Design, Synthesis and Interaction Studies of Sulfated Allosteric Modulator of Thrombin, VAS Annual Meeting, Richmond, VA.

3. SERMAC/SWRM-2010, Synthesis and Interaction Studies of Benzofuran Based Allosteric Modulator of Thrombin, ACS regional meeting, New Orleans, LA.

4. SERMAC/SWRM-2010, Exploring Larger Chemical Space to Design Small, Aromatic, Sulfated Allosteric Modulators Of Thrombin, ACS regional meeting, New Orleans, LA.

5. The Twenty Seventh Annual Daniel T. Watts Research Poster Symposiums 2010, Structure Based Design Of Allosteric Inhibitors Of Thrombin, Virginia Commonwealth University, Richmond, VA.

6. School of Pharmacy's Research and Career Day 2010, Exploring Larger Chemical Space to Design Small, Aromatic, Sulfated Allosteric Modulators of Thrombin, Virginia Commonwealth University, Richmond, VA.

7. Graduate Student Association Twelfth Annual Research Symposium and Exhibit 2010, Structure Based Design Of Allosteric Inhibitors Of Thrombin, Virginia Commonwealth University, Richmond, VA.

8. School of Pharmacy's Research and Career Day 2009, Design, Synthesis and Interaction Studies Of Dual, Direct Non-saccharide Allosteric Modulators Of Thrombin And Factor Xa, Virginia Commonwealth University, Richmond, VA.

9. The Twenty Sixth Annual Daniel T. Watts Research Poster Symposium 2009, Design, Synthesis and Interaction Studies Of Dual, Direct Non-saccharide Allosteric Modulators Of Thrombin and Factor Xa, Virginia Commonwealth University, Richmond, VA.

Laboratory Skills

Synthesis

Organic synthesis including anhydrous reaction, Microwave-based reactions, transition metal catalyzed reactions, polymer synthesis and characterization.

Molecular Modeling Software: Sybyl, legion, HINT, GOLD, MDL, Virtual Screening.

Analytical Techniques

NMR (Proton, Carbon and 2D), Mass Spectroscopy, Chromatography Techniques (Flash System, Cation Exchange, Size Exclusion), HPLC (Quantitative and Preparative), Enzyme Assay, Plasma and Blood Studies.

RESEARCH PROJECTS

• Synthesis of 2nd Generation Benzofuran-Based Sulfated Allosteric Inhibitors of Thrombin (Sept 2010 – Oct 2011).

The project involves the synthesis of pilot library of novel sulfated benzofuran based trimer and biological evaluation for inhibition of thrombin. These molecules were found to be potent allosteric inhibitors of thrombin. The library was also screened against the panel of other proteases involved in coagulation cascade and indentified the lead structures for designing the inhibitors for Factors VIIa, IXa, Xa and XIa. The manuscript is ready for submission to J. Med. Chem.

• Design Synthesis and Interaction Study of novel Allosteric Modulators of Thrombin (Jan 2008 - Sept 2010).

The project involves the design and synthesis of library of novel sulfated monomers and dimer as inhibitors of thrombin. The enzyme assay and mechanistic studies suggested as potent allosteric inhibitors of thrombin. This work is published in J. Med. Chem.

• Structure Based Virtual Screening to Explore Larger Chemical Space (Jan 2010 - Jul 2010).

The pharmacophore was generated from the library of sulfated benzofuran dimers to identify the new lead molecules. Using virtual screening, the vast chemical space in ZINC database was explored to find the new core structures as allosteric inhibitors of thrombin. In silico study was combination of ligand-based and docking-based approach using GOLD docking suite. The hit was evaluated experimentally. The manuscript is ready for submission to Bioorg. Med. Chem. Letters.

• QSAR Model of Direct Factor Xa Inhibitors (Sep 2009 - Dec 2009).

The QSAR studies were carried out for direct factor Xa inhibitors using MDL QSAR software to find relationship between enzyme inhibition activity and various physical descriptors.

• In silico Designing of Factor Xa and Thrombin Inhibitors (Mar 2008 - Jun 2008).

The project involves the designing of in silico library of molecules and docking it on the target protein using GOLD docking software. The virtual library was docked on crystal structure of thrombin and factor Xa and GOLDScore function was used to identify molecules having high binding affinity.

TEACHING

Teaching assistant for following courses:

• PHAR 524 (Foundation II)

• PHAR 534 (Foundation III)

• PHAR 640 (Foundation V)

• MEDC 543 (Clinical Chemistry for Pharmacists)

• MEDC 310 ( Medicinal Chemistry and Drug Design)

• MEDC 541 (Survey of Molecular Modeling Methods)

• MEDC 670 (Advanced Molecular Modeling)

MENTORSHIP

• Miten Patel (June 2010- Dec 2010) – Undergraduate Student

• Swathi Bobbity (Aug 2010-May 2011) – Graduate Mentorship Program

• Susana Ayad (June 2011- Present) – Undergraduate Student

• Amal Shanker ( Nov 2011 – Present) – Graduate Student

EXTRACURRICULAR LEADERSHIP INVOLVEMENT

• Student Advisor and Member of VCU Honor System, Office of Judicial Affairs & Academic Integrity, Virginia Commonwealth University, 2010 – 2011.

• Graduate Mentor, VCU Graduate School Mentorship Program, Virginia Commonwealth University, 2010 – 2011.

• Vice President, TIRANGA-Indian Nationals at VCU, Virginia Commonwealth University, 2009 – 2010.

• Treasurer, TIRANGA-Indian Nationals at VCU, Virginia Commonwealth University, 2010 – 2011.

MEMBERSHIPS

American Association of Pharmaceutical Scientists (AAPS)

American Chemical Society (ACS)

American Association of Indian Pharmaceutical Scientists (AAiPS)

REFERENCES

1. Dr. Umesh R. Desai

Professor

Department of Medicinal Chemistry/ Institute of Structural Biology and Drug Discovery

Virginia Commonwealth University, Richmond, USA.

Email: *******@***.***

2. Dr. Qibing Zhou

Professor and Scientific Director

National Engineering Research Center for Nanomedicine

Institute of MateriaMedica

Huazhong University of Science and Technology

Wuhan, China

Email: *****@***.***

3. Dr. Frank Gupton

Research Professor and Interim Chair

Department of Chemical and Life Sciences

Virginia Commonwealth University, Richmond, USA.

Email: ********@***.***

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