resumÉ dr shakir ahamad · ahamad, a. k. gupta, r. kant, k. mohanan, org. biomol. chem. 2015, 13,...

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Department of Chemistry Aligarh Muslim University Aligarh, 202002, India shakirzaheer111 @gmail.com +91-8410487966 To work with a reputed institution as an assistant professor/research scientist, that will provide me a good platform to utilize my research, teaching and administration skills. AWARDS, DISTINCTIONS AND FELLOWSHIPS 2017: CSIR-CDRI Incentive award for publication-2017 2015: Senior research fellowship (SRF) from UGC, New Delhi 2013: Junior research fellowship (JRF) from UGC, New Delhi 2013: Qualified joint CSIR-UGC test for JRF and eligibility for lectureship (NET), AIR-34. 2013: Qualified GATE-2013, AIR-221 EDUCATION ALIGARH MUSLIM UNIVERSITY M.Sc Organic Chemistry 2013 75.00 % KURUKSHETRA UNIVERSITY B.Sc Chemistry 2011 70.00% HOBBIES CRICKET, BADMINTON, KABADDI, GYM INSTRUMENTATION & IT SKILLS MS OFFICE ADOBE PHOTOSHOP MestReNova TOPSPIN CHEM DRAW Mass spectrometery, NMR, HPLC, UPLC IR, UV, PXRD, X-Ray Crystallography, ITC, DSC RESEARCH DESCRIPTION Worked as research scholar (Ph. D.) under the supervision of Dr. Kishor Mohanan, (senior scientist at CSIR-central drug research institute, Lucknow) from July 2013 to April 2018 in the area of organic synthesis and medicinal chemistry. Ÿ Heterocyclic Chemistry Ÿ Development of metal-free domino multi-component reactions for the synthesis of structurally diverse N-, O-, F- and P-based heterocycles by employing diazo compounds. Ÿ Development of new synthetic methods. Ÿ Drug Discovery Ÿ Design, synthesis and biological evolution of pyrazole-based nucleoside as potential therapeutics for anti-HIV activity. Ÿ Design, synthesis and biological profiling (in vitro and in vivo) of aminopyridine derived PCSK-9 inhibitors as target drugs for anti- hyperlipidemic activity. Ÿ Design, synthesis and SAR study of 1-aminopropan-2-ole tethered aminoazabenzimidazoles for anti-malarial activity. RESUMÉ dr Shakir Ahamad Ÿ Doctor of Philosophy in Organic Chemistry: 20 December 2018 Ÿ Thesis entitled- “Domino reactions employing diazo compounds: an efficient access to novel N-heterocycles” (Under the supervision of Dr. Kishor Mohanan, Senior Scientist, Medicinal & Process Chemistry Division, Central Drug Research Institute, Lucknow, India) RESEARCH INTERESTS Organic Synthesis, Host-Guest chemistry, Chemical Biology and Medicinal Chemistry SCIFINDER OS - Windows, Linux CDRI LUCKNOW, INDIA Chemical Science 2013-18 Ph.D. Assistant Professor, Department of Chemistry, Aligarh Muslim University, Aligarh, 202002, India

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Department of Chemistry

Aligarh Muslim University

Aligarh, 202002, India

shakirzaheer111

@gmail.com

+91-8410487966

To work with a reputed institution as an assistant professor/research scientist,

that will provide me a good platform to utilize my research, teaching and

administration skills.

AWARDS, DISTINCTIONS AND FELLOWSHIPS

2017: CSIR-CDRI Incentive award for publication-2017

2015: Senior research fellowship (SRF) from UGC, New Delhi

2013: Junior research fellowship (JRF) from UGC, New Delhi

2013: Qualified joint CSIR-UGC test for JRF and eligibility for lectureship

(NET), A IR-34.

2013: Qualified GATE-2013, AIR-221

EDUCATION

ALIGARH MUSLIMUNIVERSITY

M.ScOrganic Chemistry

2013

75.00 %

KURUKSHETRAUNIVERSITY

B.ScChemistry

2011

70.00%

HOBBIESCRICKET, BADMINTON, KABADDI, GYM

INSTRUMENTATION& IT SKILLS

MS OFFICE

ADOBE PHOTOSHOP

MestReNova

TOPSPIN

CHEM DRAW

Mass spectrometery, NMR, HPLC, UPLC

IR, UV, PXRD, X-Ray Crystallography, ITC,

DSC

RESEARCH DESCRIPTION

Worked as research scholar (Ph. D.) under the supervision of Dr. Kishor

Mohanan, (senior scientist at CSIR-central drug research institute, Lucknow)

from July 2013 to April 2018 in the area of organic synthesis and medicinal

chemistry.

Ÿ Heterocyclic Chemistry

Ÿ Development of metal-free domino multi-component reactions for the

synthesis of structurally diverse N-, O-, F- and P-based heterocycles by

employing diazo compounds.

Ÿ Development of new synthetic methods.

Ÿ Drug Discovery

Ÿ Design, synthesis and biological evolution of pyrazole-based nucleoside

as potential therapeutics for anti-HIV activity.

Ÿ Design, synthesis and biological profiling (in vitro and in vivo) of

aminopyridine derived PCSK-9 inhibitors as target drugs for anti-

hyperlipidemic activity.

Ÿ Design, synthesis and SAR study of 1-aminopropan-2-ole tethered

aminoazabenzimidazoles for anti-malarial activity.

RESUMÉ

dr Shakir Ahamad

Ÿ Doctor of Philosophy in Organic Chemistry: 20 December 2018

Ÿ Thesis entitled- “Domino reactions employing diazo compounds: an

efficient access to novel N-heterocycles” (Under the supervision of Dr.

Kishor Mohanan, Senior Scientist, Medicinal & Process Chemistry Division,

Central Drug Research Institute, Lucknow, India)

RESEARCH INTERESTS

Organic Synthesis, Host-Guest chemistry, Chemical Biology and Medicinal

Chemistry

SCIFINDER

OS - Windows, Linux

CDRILUCKNOW, INDIA

ChemicalScience

2013-18

Ph.D.

Assistant Pro fesso r, D epartm ent o f Ch em istry,

Ali garh M usli m U n iversity, Ali garh, 2020 02, I n d ia

RESEARCH APTITUDE

Ÿ Planning, organizing and implementation of research projects.

Ÿ Capable of performing both collaborative and independent research.

Ÿ Supervision of research work of graduate and post-graduate project trainees and junior Doctoral colleagues.

Ÿ Designing, synthesizing and lead optimization through SAR study for medicinal chemistry purpose.

RESEARCH AND TEACHING EXPERIENCE

Ÿ Junior Research Fellow: Medicinal & Process Chemistry Division, CSIR-Central Drug Research Institute Lucknow-226031,

Uttar Pradesh, India, 2013-2015.

Ÿ Senior Research Fellow: Medicinal & Process Chemistry Division, CSIR-Central Drug Research Institute, Lucknow-226031,

Uttar Pradesh, India, 2015-2018.

Ÿ Project Assistant: Molecular & Structural Biology division, CSIR - Central Drug Research Institute, Lucknow -

Ÿ 226031, India (2018-2019)

Ÿ Assistant Professor: Department of Chemistry, Aligarh Muslim University, Aligarh 202002, India

Ÿ (since 02-08-2019)

RESEARCH SKILLS

Ÿ Experienced in performing multi-step organic synthesis from milligram to gram scale.

Ÿ Experienced in handling light and moisture sensitive compounds and performing reactions under inert atmosphere and

their proper purification.

Ÿ Strong knowledge and experienced in designing and synthesizing organic molecules of biological interest.

Ÿ Capable to handle sugar and nucleoside based molecules.

Ÿ Efficient in handling spectroscopic techniques and data interpretation (Mass, IR, UV, HPLC, UPLC and NMR).

Ÿ Adept in using general techniques for separation and purification of organic compounds.

Ÿ Skilled in using online databases such as Reaxys, Scifinder, Science direct, Google Scholar and PubMed.

Ÿ Softwares: ChemDraw, MS Word, MS Excel, MS PowerPoint, Adobe Photoshop, TOPSPIN, MestReNova, etc.

Ÿ Experienced in writing research articles and reviews.

PUBLICATIONS

Papers Published in International Journals

Organic Chemistry

1. Solubility enhancement of Ribociclib through host–guest interactions with cucurbiturils, D. Katiyar, T. S. S. Ahamad,

Thakur (Manuscript under preparation)

2. Bioavailability improvement of Tenofovir through inclusion with CB7. , D. Katiyar, T. S. Thakur (Manuscript S. Ahamad

under preparation)

3. ''Metal-catalysed regioselective synthesis of donor−acceptor CF3-containing cyclopropanes, and its nucleophilic ring

opening reactions.'' A. Kumar, , R. Kant, K. Mohanan. (Manuscript under preparation) S. Ahamad

4. ''Metal-catalyzed domino three-component reaction using trifluorodiazoethane: An approach towards the synthesis

of trifluoromethylpyrazoles.'' A. Kumar, S. Mathew, , R. Kant, K. Mohanan. (Manuscript under preparation) S. Ahamad

5. 'Silver-Catalyzed Three-Component Route to Trifluoromethylated 1,2,3-Triazolines Using Aldehydes, Amines, and

Trifluorodiazoethane.'' A. Kumar, , R. Kant, K. Mohanan. 2019, 21, 2962. S. Ahamad Org. Lett.,

6. Base-mediated 1,6-conjugate addition reaction of Seyferth-Gilbert reagent to para-quinone methides A. K. Gupta, S.

Ahamad, R. Kant, K. Mohanan 2018, 16, 4623. Org. Biomol. Chem.

7. Metal-Free three-component assembly of fully-substituted 1,2,3-triazoles .; K.; Kumar A.; Kant, R.; Mohanan, Ahamad, S

K. Asian J. , 2018, 7, 1698. Org. Chem

8. Three-component synthesis of 3,4-disubstituted pyrazoles using diazosulfone as a diazomethane surrogate. , S. Ahamad

R. K. Patidar, A. Kumar, R. Kant, K. Mohanan, 2017, 2, 11995. ChemistrySelect

9. Metal-Free three-component domino approach to phosphonylated triazolines and triazoles. , R. Kant, K. S. Ahamad

Mohanan, 2016, 18, 280. Org. Lett.

10. Three-component domino HWE olefination/1,3-dipolar cycloaddition/oxidation strategy for the rapid synthesis of

trisubstituted pyrazoles. , R. Kant, K. Mohanan, 2016, 1, 5276. S. Ahamad ChemistrySelect

11. Substrate-controlled product-selectivity in the reaction of the Bestmann–Ohira reagent with N-unprotected isatin-

derived olefins. A. K. Gupta, , E. Gupta, R. Kant, K. Mohanan, 2015, 13, 9783. S. Ahamad Org. Biomol. Chem.

12. Domino reaction involving the Bestmann–Ohira reagent and a,b-unsaturated aldehydes: efficient synthesis of

functionalized pyrazoles. , A. K. Gupta, R. Kant, K. Mohanan, 2015, 13, 1492. S. Ahamad Org. Biomol. Chem.

Medicinal Chemistry

Publications from medicinal chemistry part are awaited as further studies under process.

ORAL AND POSTERS PRESENTATION, AND PARTICIPATION IN CONFERENCES/ SYMPOSIA / WORKSHOP

1. Participated and delivered an oral talk in at CSIR-CDRI, Lucknow, “XII J-NOST Conference for Research Scholars”

th th24 to 27 November, 2016.

2. Participated and delivered an oral talk in at “International Conference on Recent Advances in Chemical Science”

th thAligarh Muslim Univetsity, 29 to 30 March, 2016

3. Participated and presented poster in One Day Symposium on “Drug Discovery in India: Past, Present and Future”

st at CSIR-Central Drug Research Institute, Lucknow, 1 January 2015.

th th4. Volunteered in , at CSIR-CDRI Lucknow, 15 -16 September, 2017.“The First CDRI and NRDC-Industry Conclave”

5. Volunteered in (CTDDR-2016) th“6 International Symposium On Current Trends In Drug Discovery And Research”

th thheld at CSIR-Central Drug Research Institute, 25 – 28 February, 2016, Lucknow.

6. Participated in organized by Waters India (p) Ltd., at SAIF, CSIR-CDRI, Lucknow, “HPLC/UPLC training programme”

th th 5 -6 September 2017.

7. Participated in Workshop on “The Application of MS and LC-MS/MS Instrument for Identification and

Characterization of Small Molecules” th st at SAIF, CSIR-CDRI, Lucknow 29 September to 1 October, 2015.

UNDERGRADUATE TRAININGS AND PROJECTS

Ÿ One month project on the “production of ethanol from sugarcane molasses'' at department of biotechnology, GNKC,

Yamuna nagar-135001, Haryana, India, 2011.

Ÿ One month training in pathology at city pathology lab, Saharanpur-247001, Uttar Pradesh, India 2010.

Ÿ One month industrial training on fermentation technology at Pilkhani Distillery & Chemical Works, Saharanpur-

247001, Uttar Pradesh, India, 2009.

EXTA-CURRICULAR

Ÿ Won gold medals in marathon, kabaddi, cricket and silver medal in badminton mixed doubles held at CSIR-CDRI

in the “Annual Sports 2018”.

Ÿ Won gold medal in cricket and silver medal in kabaddi held at CSIR-CDRI in the “annual sports 2017”.

Ÿ Won gold medal in kabaddi and silver medal in cricket held at CSIR-CDRI in the “annual sports 2016”.

Ÿ Won several prizes in competitions held at the school level.

Ÿ First (2007) and second (2008) level training certificates from ''Hindustan Scouts & guides'' Utter Pradesh, India.

PERSONAL DETAILS

Ÿ Father’s Name : Zaheer Ahamad

ŸthDate of Birth : 20 July 1991

Ÿ Nationality/Sex/Marital Status : Indian/Male/ Single

Ÿ Languages known : Hindi/Urdu/English

ACADEMIC REFEREES

Dr. Tejender S. Thakur

Senior Scientist

Molecular & Structural Biology

CSIR - Central Drug Research Institute, Lucknow - 226031, India

[email protected]

0522-2772450 EPABX-4481, Fax No.- +91-522-2771941

DECLARATION

I hereby declare that the

information given above is true

and I hold the responsibility of

its authenticity.

Date:

Place:

Shakir Ahamad

वैज्ञानिकऔरिवीकृतअिुसंधािअकादमी ACADEMY OF SCIENTIFIC AND INNOVATIVE RESEARCH

Summary of the Research Work

Organic Synthesis and Medicinal Chemistry

2

Synthetic Organic Chemistry

1. Silver-Catalyzed Three-Component Route to Trifluoromethylated 1,2,3-Triazolines Using

Aldehydes, Amines, and Trifluorodiazoethane

A. Kumar, S. Ahamad, R. Kant, K. Mohanan. Org. Lett., 2019, 21, 2962.

2. Base-mediated 1,6-conjugate addition reaction of Seyferth-Gilbert reagent to para-quinone

methides

A. K. Gupta, S. Ahamad, R. Kant, K. Mohanan Org. Biomol. Chem. 2018, DOI: 10.1039/C8OB01017J

3. Metal-Free three-component assembly of fully-substituted 1,2,3-triazoles

Ahamad, S.; K.; Kumar A.; Kant, R.; Mohanan, K. Asian J. Org. Chem, 2018, DOI: 10.1002/ajoc.201800340

3

4. Three-component synthesis of 3,4-disubstituted pyrazoles using diazosulfone as a diazomethane

surrogate

Ahamad, S.; Patidar R. K.; Kumar A.; Kant, R.; Mohanan, K. ChemistrySelect 2017, 2, 11995.

5. Metal-Free three-component domino approach to phosphonylated triazolines and triazoles

Ahamad, S.; Kant, R.; Mohanan, K. Org. Lett. 2016, 18, 280

6. Three-component domino HWE olefination/1,3-dipolar cycloaddition/oxidation strategy for the

rapid synthesis of trisubstituted pyrazoles

Ahamad, S.; Kant, R.; Mohanan, K. ChemistrySelect 2016, 1, 5276

4

7. Domino reaction involving the Bestmann–Ohira reagent and α,β-unsaturated aldehydes: efficient

synthesis of functionalized pyrazoles

Ahamad, S.; Gupta, A. K.; Kant, R.; Mohanan, K. Org. Biomol. Chem. 2015, 13, 1492.

8. Substrate-controlled product-selectivity in the reaction of the Bestmann–Ohira reagent with N-

unprotected isatin-derived olefins

A. K. Gupta, S. Ahamad, E. Gupta, R. Kant, K. Mohanan, Org. Biomol. Chem. 2015, 13, 9783.

9. Metal-catalyzed regioselective synthesis of donor−acceptor CF3-containing cyclopropanes, and its

nucleophilic ring opening reactions

A. Kumar, S. Ahamad, R. Kant, K. Mohanan. (Manuscript Communicated)

5

10. Metal-catalyzed domino three-component reaction using trifluorodiazoethane: An approach

towards the synthesis of trifluoromethylpyrazoles

A. Kumar, S. Mathew, S. Ahamad, R. Kant, K. Mohanan. (Manuscript Communicated)

Medicinal Chemistry

11. Design, Synthesis and Biological Evaluation of a Novel Class of Pyrazole Nucleosides as Antiviral

Agents

S. Ahamad, S. verma, R. Patidar, R. Kant, K. Mohanan. (Further studies are going on)

6

12. Design, synthesis and biological profiling of aminopyridine derived PCSK-9 inhibitors as

target drugs for anti-hyperlipidemic activity (liver LDL clearance)

S. Ahamad, A. Burman, K. Mohanan. (Further studies are going on)

PARAMETERS S-017-0594

Aqueous buffer solubility

(by Kinetic Method)

≥ 60µg/mL

SGF Stability (pH1.2)

(% remaining, 1 h)

90.86%

(Stable)

SIF Stability (pH7.4)

(% remaining, 2 h)

89.17%

(Stable)

Plasma Stability

(% remaining, 1.5 h)

83.34 ± 2.85%

(Stable)

Microsomal stability

(% remaining, 1h ) 54.96 ± 9.02%

K(1/min) 0.010 ± 0.002667

Half-Life (min) 81.4 ± 17.60

Intrinsic clearance

(mL/min×mg) 0.010 ± 0.002667

Hepatic clearance(L/h/kg) 16.965 ± 4.68

7

13. Design, synthesis and SAR study of 1-aminopropan-2-ole tethered aminoazabenzimidazoles for

anti-malarial activity

S. Ahamad, S. Mathew, K. Mohanan. (LEAD optimizationis going on)

8

14. Molecular Encapsulation of cyclin-dependent kinase 4/6 inhibitors by Cucurbit[7]Uril: An

Experimental and Computational Study

S. Ahamad, Tejender S. Thakur (Manuscript Communicated)

Supramolecular

Formulation

9

15. Bioavailability improvement of Tenofovir through inclusion with CB7.

S. Ahamad, D. Katiyar, T. S. Thakur (Manuscript under preparation)

10

16. Inclusion of Anti-bacterial drugs (Levofloxacin and ciprofloxacin) in Cucurbit[7]uril

S. Ahamad, D. Katiyar, T. S. Thakur (Manuscript under preparation)

17. Study to improve the thermal stability and aqueous solubility of CDRI developmental compound

S011-1599 (potent Anti Breast Cancer Lead)

We have prepared a new crystalline salt form of the S011-1559. The new crystalline phase possess high

thermal stability than the parent compound S011-1559, a low melting solid which exists as liquid at RT.

Further, we were also able to address the poor aqueous solubility the compound S011-1559 (practically

insoluble in water) by crystal engineering. The new salt for is highly soluble in water (~1-2 mg/mL).