I. PERSONAL DETAILS
Name: Ganesh N Y Pujarayya
Father Name: Yallappa N H Pujar
Mother Name: Basamma N Y
Qualification: M.Sc., Ph.D. (ORGANIC CHEMISTRY)
I have 01 Year experience in Anthem Biosciences Pvt. Ltd. in Bangalore, Karnataka, India as a “Research Assistant”.
I have 04 Yrs experience worked as Research Scholar in National Research Institute of Visvesvarayya Technological University, Belagaum-590018, Karnataka, India. I have 04 Teaching experience (Guest Lecturer) for UG and PG courses in Govt. Science College, Chitraurga-577 501, Karnataka, India. Residential Address: Ganesh N Y S/O Yallappa N H,
Chikkanahalli New Ext., Pujar
Nituvalli, Davangere-577004, Karnataka, India
Official Address: Ganesh N Y, Ph.D.
Scholar, Dept. of
Govt. Science College,
Chitradurga-577501, Karnataka, India.
I am an expert in the synthesis of Heterocyclic drugs & their biological screening test mainly on anticancer activity, antibacterial and antimicrobial and so on..
Well knowledge in Name Reactions of Organic Chemistry, Reagents role, Stereochemistry & so on.
Research Literature Survey
Research Schemes Planning
Data Collection for Research
Elucidation of Compounds by Spectroscopy such as FT-IR, H-NMR, C NMR, Elemental Analysis, LC-MS
In Vitro studies for Synthesized Compounds
Handling the instruments such as Rota-Vapor, Magnetic Stirrer, Microwave Oven, Ultrasonicator, Muffle Furnace, FT-IR, 1HNMR, HPLC, LC-MS.
Handling of In-vitro study instruments.
IV. RESEARCH ACHIEVEMENTS:
I have been guiding M.Sc students for their Academic projects since from 3 years in Synthetic Organic Chemistry and Biological activity of synthesized compounds.
My Research Paper has presented by me in an International Conference held at Atlanta of USA in 2018.
I have been guiding the students on Scientific dissertation writing skills
Trainee in Anthem Biosciences Pvt. Lt, Bangalore.-Synthesis of Pyrazolo-Pyrimidines & its Characterization, Handling of required instruments on that occasion. (2 months, 2014).
Nominated for Young Scientist Award by INSA in 2015- “Synthesis of Dry Ice & Its application for Reducing CO2 in environment”.
Ph.D work on the Title:
“STUDIES ON THE SYNTHESIS, CHARACTERIZATION AND BIOLOGICAL EVALUATION OF PYRAZOLE DERIVATIVES AND PYRAZOLO-PYRIMIDINES”. Synthesis of Quinolines and Thiophenes are undergoing project under my leadership Currently, I am working on the project entitled “DESIGN AND SYNTHESIS OF PYRAZOLE DERIVATIVES AND IN-VITRO SCREENING TO
PROTECT ACE2 HUMAN CELLS” AGAINST COVID-19.
“DESIGN, SYNTHESIS OF DOPED PYRAZOLO [3,4-
d]PYRIMIDINES BY A SPECIFIC METHOD FOR IN-VITRO AND IN-VIVO SCREENING AGAINST NOVEL COVID-19 AS ACE2
HUMAN CELL RECEPTORS”. This project work to be completed yet
Published ‘ 06’ Research papers in peer review International journals as a main Author & Co- responding Author (journals name & Title mentioned in separate)
Another ‘04’ papers are communicating in peer review international journals.
Participated in many International conferences & National Conferences.
Presented in International & National Conferences. PAPERS/PUBLICATIONS OUT OF THE RESEARCH WORK
1. Ganesh N Yallappa1* D. Nagaraja1 & U. Chandrashekhar2. “Base Catalyzed Microwave Assisted Synthesis, Characterization of 6-Bromo-Pyrazolo-[1,5-a]Pyrimidine-3-Ethyl- Carboxylate & Its Biological Evaluation as CDKs Inhibitor”; Asian J. Chem.; Vol. 30, No. 8
2. D. Nagaraja1, Ganesh N Yallappa1* & U. Chandrashekhar2; “AN EFFICIENT NANO- CATALYSED SYNTHESIS, CHARACTERIZATION & STUDY OF FLUORESCENCE PROPERTY OF SUBSTITUTED PYRAZOLE”; Heterocyclic Letters, Vol. 8 No.1 79-83 Nov- Jan 2018; ISSN: (print) 2231–3087 / (online) 2230-9632; CODEN: HLEEAI http://heteroletters.org.
3. Ganesh N Yallappa1, D Nagaraja1* & U. Chandrashekhar1, “An Efficient Nano-Catalyzed Green Synthesis, Characterization of Substituted Pyrazoles& Study of Their Fluorescence Characteristics”. Journal on Material science (accepted). 4. D Nagaraja1*, Ganesh N Yallappa1 & U. Chandrashekhar1; Green Synthesis of Pyrazolo
[3,4]-Pyrimidine-thiones by using Ionic liquid 2-methyl-Imidazolium-Oxalate as Potent EAC receptor antagonists; Asian J. of Pharmaceutical and Clinical Research, 2019; 12(9): 276-280.
5. Ganesh N Yallappa1, D. Nagaraja1*, U. Chandrashekhar2
. NANO-CATALYZED GREEN
SYNTHESIS OF PYRAZOLE DERIVATIVES & ITS BIOLOGICAL ACTIVITY AS EAC RECEPTOR ANTAGONISTS. Pharmacophore, 2019; 28(3): 28-32. 6. Ganesh N Yallappa1, D. Nagaraja1* and Chandrashekhar U2 and Joy Hosakere3; “One Pot Multi-component Microwave assisted Synthesis, Characterization of Pyrazolo
[3,4-d]- Pyrimidines by using 2-Methyl-imidazolium-thiocyanate as MCF-7 Breast cancer cell inhibitors ".; Communicated in Med. Chem. Res. (MCRE-D-19-00752). 7. D. Nagaraja1, Ganesh N Yallappa1* & U. Chandrashekhar2. DESIGN AND SYNTHESIS OF PYRAZOLO-PYRIMIDINE DERIVATIVES BY USING NANO-ZnO CATALYST AND STUDY OF THEIR ANTIBACTERIAL ACTIVITY. (Communicated in Med. Chem. Res.)
8. Ganesh N Yallappa1, D. Nagaraja1* and Chandrashekhar U2; “One Pot Multicomponent Microwave assisted synthesis of Pyrano [2,3-c]pyrazoles and its biological activity against Prostate cancer cell lines”. Abstract has been accepted for International conference on “Natural Products and Synthetic Chemistry” to be conducted in New York, USA. 9. D. Nagaraja1*, Ganesh N Yallappa1 & U. Chandrashekhar2: “ONE-POT MULTI COMPONENT SYNTHESIS OF 4H-PYRANO [2,3- c] PYRAZOLES IN METHANOL AT ROOM TEMPERATURE BY MW AND THEIR ANTI-BACTERIAL SCREENING”
(Communicated in Synthetic Communications).
10. Ganesh N Yallappa1, D. Nagaraja1* and Chandrashekhar U2. “DESIGN AND SYNTHESIS OF PYRAZOLO-PYRIMIDINE DERIVATIVES BY USING NANO-ZnO CATALYST AND STUDY OF THEIR ANTIBACTERIAL ACTIVITY”. (Manuscript is communicated). 11. Ganesh N Yallappa1* and D Nagaraja. DESIGN AND SYNTHESIS OF PYRAZOLE DERIVATIVES AND IN-VITRO SCREENING TO PROTECT ACE2 HUMAN CELLS AGAINST COVID-19. (Communicated in Asian J Pharmaceuticals) 12. Suresha Kumara T H1, Rajendra Prasad S1’, Ganesh N Yallappa1* and Suresh Kumar H M1. “Microwave Assisted Synthesis of Pyrazolone derivatives by using Nano-CoO and Study of their Anti-bacterial activity” (Manuscript under Preparation). CONFERENCES/WORKSHOPS/SYMPOSIUMS
1. Oral Presentation of Research Paper in Indian Science Congress which was held in Bangalore on January 3rd and 4th 2020.
2. E-Poster presentation of an abstract in International Conference held in USA, Atlanta on the title “Green Synthesis of Pyrazolo-Pyrimidines by using Ionic liquids as an EAC receptor antagonist” (17th to 18th July 2018).
3. Oral Presentation in two day National Conference (RANST) held in Govt. Science College, Chitradurga on the title “Base Catalysed Microwave assisted Synthesis, Characterization of 6-Bromo-Pyrazolo-[1,5-a]-Pyrimidine-3-Ethyl-Carboxylate & its Biological Evaluation as CDKs inhibitor” (April 2017). 4. Oral Presentation in National Symposium ‘CHEMEXCEL’ in BIET college, Davangere on the title “An Efficient Nano-Catalyzed Green Synthesis, Characterization of Substituted Pyrazoles & Study of Their Fluorescence Characteristics” (March 2018). 5. Poster Presentation in Nat ional Level Conference on “Recent Advances in Material Science” held on 5th February 2019 organised by the Department of Chemistry, Field Marshal K.M. Cariappa College, Madikeri.
6. Poster Presentation in Two day National Conference on “Exploring Innovative Research and Developments in Chemical Sciences” (EIRDCS-2019) organised by the Department of PG Studies and Research in Chemistry, Kuvempu University, Shivamogga held during 1 st & 2nd March-2019.
7. Oral Presentation in National “14th Conference of Society of Cytologist and Geneticists and Bio Entrepreneurship Summit” held at the Department of Biotechnology and Research Centre, Bapuji Institute of Engineering and Technology, Davangere during 6th to 8th March 2019.
8. Poster Presentation in International Conference on “Advanced Functional materials and Health Care” (AFMAHC) organised by Dept. of Chemistry, Mysore University, Mysore.
(18th to 20th March).
9. E-poster to be presented in International conference on “Emerging trends in Organic Synthesis and Drug discovery” organised by held at New York, USA (June 24th and 25th 2019).
10. Participated in International conference held on “Recent advances in Chemical Science” at Kadur, Shivamogga (Kuvempu University).
11. Participated in one day National Conference held at Davangere University on “Recent Trends & Future Applications of Chemical Sciences” (RTFACS-2016). 1 2 . Participated in IIT Indore-RSC Symposium on “Advances in Chemical Sciences”, held at IIT Indore, India on 30th January 2018.
13. Participated in Workshop Organized by Maharani’s Science College for Women, Bangalore- DBT star college Scheme Sponsored “ Hands on training on Science Laboratory Equipment & Instrumentation” (September 2017).
14. Participated in 3 day Workshop at Vivekananda College of Engineering & Technology, Puttur organized by VTU on “Research Methodologies & Latex” (September 2017).
V. COMPUTER SKILLS:
I am expertise in MS-Word, MS-Excel, MS-Power Point & other basic knowledge.
Chemsketch & ISIS Draw.
VI. COMMUNICATION SKILLS:
Languages expert in- English, Kannada & Hindi.
Good English writing skills.
Mothiveerappa High School,
D R M Science College, Davangere-
(Karnataka PU Board), Karnataka,
S J V P Autonomous College,
M.Sc. (General Chemistry)
Govt. Science College,
Ph.D. (Organic Chemistry/
Title: “Studies on the
and Biological Evaluation
of Pyrazoles and Pyrazolo-
Govt. Science College, VTU-RRC,
(Affiliated to VTU, Belagavi)
VII. EDUCATIONAL DETAILS:
VIII. RESEARCH STATEMENT
Heterocyclic compounds are very widely distributed in nature and are essential to life. They play a vital role in the metabolism of all living cells. Nitrogen containing heterocycles are the compounds placed at the topmost in the field of pharmaceuticals and agrochemical industries. The biological importance of Nitrogen containing heterocycles have made them scope for synthesis. Their importance as precursors to many biologically active compounds has made attention on developing methods to functionalize these systems.
The synthesis of nitrogen Heterocycles and their derivatives occupy an important place in the realm of natural and synthetic organic chemistry due to their therapeutic and pharmacological properties. They have emerged as integral backbones of over seven thousand existing drugs. In addition to these important biological applications nitrogen Heterocycles are ideal scaffolds for making libraries of drug like compounds and to generate libraries of inhibitors of HIV-1 protease. A large number of nitrogen containing heterocyclic building blocks have several applications in pharmaceutical research and drug discovery. Most of the organic compounds containing nitrogen show better biological activity than non- nitrogen compounds [1-5].
Upon reviewing literature, we became interested in the synthesis of some nitrogen containing Heterocycles like, pyridine, pyrimidine and fused pyrimidine Heterocycles. Although a numerous modified methods under improved conditions have been reported for the synthesis of these classes of compounds, most of the methods are generally carried out in organic solvents, longer reaction time, high temperature and expensive catalysts are used. Moreover disadvantages of most of the existing methods are that catalyst is destroyed in the work-up and cannot be recovered or reused. Due to the immense biological activities of nitrogen containing heterocyclic compounds, we have become interested in the synthesis of various nitrogen heterocyclic and evaluate their biological activity associated with them [6-9]. PROBLEM STATEMENT:
During our research work, we planned to sort out many challenges in the field of synthetic organic chemistry. We worked our plan very successful. However, we are unsatisfied with some compounds which yield quantitatively less by our methodology. In biological evaluation, some compounds showed less anticancer activity.
OBJECTIVE OF THE PROPOSED RESEARCH:
In the part of Synthetic organic chemistry, we have main objectives of the proposed research.
Design the synthesis of Pyrazoles and Pyrazolo-pyrimidine derivatives: To design the desired derivatives by using starting materials which are inexpensive and reaction favor.
Pyrano-pyrazoles and Pyrazolo-Pyrimidines from four component starting materials: We planned to use four components which lead to moment reaction.
Green Chemistry approach: The use of solvents and catalysts should be eco-friendly.
Microwave Irradiation and Ultrasonic method:
Use of Ionic Liquids: Preparation of Ionic liquids. These act as catalysts for the reaction.
Nano catalyst: The use of Nano-catalysts to accelerate the reaction.
Biological activity (Anticancer and Antimicrobial): In vitro screening of all compounds against MCF-7 human breast cancer cell line by MTT assay based cytotoxicity study was done. We have studied in vitro antibacterial screening for Pyrano-pyrazoles. Cancer is still continuing to be a major health problem worldwide. The treatment of cancer is associated with various side effects.
Bone marrow depression
Hepatotoxicity and many more.
Because of the need & value of anticancer drugs, many laboratories are intensively investigating the chemistry & biology of novel anticancer agents. SUMMARY:
Cancer is still continuing to be a major health problem worldwide. The development of new anticancer therapeutic agents is one of the fundamental goals in medicinal chemistry as cancer causes about 15% of all the death. Surpassing cardiovascular diseases, it is taking the position number one killer due to various factors. Also the treatment of cancer is associated with various side effects which include bone marrow depression, alopecia, drug-induced cancer, hepatotoxicity and many more. Because of the need and value of anticancer drugs, many laboratories are intensively investigating the chemistry and biology of novel anticancer agents. Also the development of resistance against the existing anticancer drugs and cytotoxicity and genotoxicity of anticancer drugs to the normal cells are other major problems in cancer therapy, keeping research window open in search for newer anticancer molecules. But the window passage has become narrower because it is rather hard to search a molecule that can selectively inhibit the proliferation of abnormal cells only with least or no effect on normal cells. In the last decade, several Pyrazolo-Pyrimidines proved to have anticancer activity. The other activities reported for Pyrazole nucleus include antitubercular, anticonvulsant, anticancer, antimicrobial, anti-HIV, antihepatotoxic, anti-inflammatory and analgesic. Also Curcumin, a major yellow pigment and active component of turmeric, has been shown to possess anti-inflammatory and anticancer activities. In some countries, Curcumin was consumed in the diet upto 4g/adult/day, which appeared to lower the incident rate of colorectal cancer. In the study, Curcumin showed autophagic and apoptotic death of K562 cell line (Leukemia). The cytotoxicity studies in different cells indicated that the toxicity of Curcumin was significantly higher in tumor cells if compared to the normal cells. Curcumin and its derivatives possess a wide variety of pharmacological activities such as antibacterial, anti-HIV, anti- inflammatory, antimalarial, anticancer, and many more. Considering these recent discoveries, curcumin can be considered as an ideal lead compound for anticancer drug development. Earlier, we have reported the anticancer activity of Pyrazoles and Pyrazolo-pyrimidine derivatives analogues. On owing to these negative aspects of treatment, we have synthesized different derivatives of Pyrazolo- Pyrimidines which can show less toxic to the human body. We employed green chemistry so that use of environmental benign starting materials could have been used. Also, less expensive chemicals and solvent-free synthesis have been done. Microwave method, Conventional method and Ultrasonic method could have been implemented. In these, microwave method proved to be an excellent method with respect to green chemistry. Multicomponent synthesis could have been achieved. This afforded quick reactions as well as good yield of the desired products. Rather than using Nano-catalysts, we planned to use Ionic liquids which have been emerged good positive results for the Organic Synthesis. Biological activity (Antiviral activity): We have planned to screen all our synthesized compounds for biological evaluation, in particular anticancer activity. We will do both in-vivo and in-vitro study of Pyrazolo-Pyrimidines as CDKs inhibitor, as agonists for Ehlirich Ascites Carcinoma cell lines and agonists for MCF-7 Breast cancer cell lines. Also, plan to do Docking studies and cytotoxic activity. Literature survey reveals that, the importance of Pyrazolo-Pyrimidines, in therapy and other applications, herewith we are presumed to synthesize some novel Pyrazolo- Pyrimidine derivatives using simple and inexpensive starting materials by both conventional and microwave assisted synthesis, characterization
13CNMR, HPLC, MS and elemental analysis) and their biological evaluation will be taken up. REFERENCES:
. Chen Q, Zhu X-L, Jiang L-L, Liu Z-M, Yang G-F. Synthesis, antifungal activity and Co-MFA analysis of Novel 1,2,4- Triazolo [1,5-a] pyrimidine derivatives. Eur. J Med. Chem., 2008, 43 (3): 595-603.
. Amir M, Javed S.A, Harish K. Synthesis of some 1,3,4-oxadiazole derivatives as potential anti-inflammatory agents. Indian J. Chem, 2007, 46B: 1014-1019.
. Trilok C, Neha G, Suman L, Saxena S. S. Synthesis of substituted acridinyl pyrazoline derivatives and their evaluation for anti-inflammatory activity. Eur. J. Med Chem, 2010, 45: 1772-1776.
. Mohammed Asif. Biological Significances of Nitrogen Hetero Atom Containing Heterocyclic Compounds. International Journal of Bioorganic Chemistry, 2017, 2(3): 146-152.
. Monika Chauhan and Raj Kumar. Medicinal attributes of Pyrazolo [3,4-d]pyrimidines: A review. Bioorganic & Medicinal Chemistry, 2013, 21: 5657–5668.
. Xin Jiang Song, Yu Shao and Xing Gao Dong. Microwave-assisted synthesis of some novel fluorinated Pyrazolo [3,4-d]pyrimidine derivatives containing 1,3,4-thiadiazole as potential antitumor agents. Chinese Chem. Lett., 2011, 22: 1036-1038.
. Isao Takeuchi, Makoto Ushida, Yoshiki Hamada, Tomaoki Yuzuri, Hiroko Suezawa and Minoro Heuroto. Studies on nitrogen-containing heterocyclic compounds: Syntheses and reactions of Benzo[g]quinoline. Heterocycles, 1995, 41(10): 2221-2231.
. Devprakash, AB Udaykumar, J. of Pharm. Res., 2011, 4(7): 2436-2440.
. Abbas Al-Mulla, A Review: Biological Importance of Heterocyclic Compounds. Der Pharma Chemica, 2017, 9(13): 141-147.
I hereby declaring you that all the statements made in the above application are true and is correct to the best of my knowledge
(Ganesh N Y Pujarayya)