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Prof. Opa Vajragupta

Department of Pharmaceutical Chemistry


  opa.vaj@mahidol.ac.th

Education Background

B.Sc.(Honors), Pharmacy, Mahidol University, Thailand
Ph.D. (Medicinal Chemistry), Boston, USA
Cert. in Radiopharmacy, Boston, USA

Work Experience

Expertise

Award & Honor

Current Research


Publication

Year 2024

1.

Targeting Alpha7 Nicotinic Acetylcholine Receptors in Lung Cancer: Insights, Challenges, and Therapeutic Strategies

Arunrungvichian K; Vajragupta O; Hayakawa Y; Pongrakhananon V.
ACS Pharmacology and Translational Science 2023 Dec 21;7(1):28-41 , 2024.

Year 2023

2.

Selective α(3)β(4) Nicotinic Acetylcholine Receptor Ligand as a Potential Tracer for Drug Addiction

Kanasuwan A, Deuther-Conrad W, Chongruchiroj S, Sarasamkan J, Chotipanich C, Vajragupta O, Arunrungvichian K.
Int J Mol Sci 2023 Jan 19;15:13-26 , 2023.

Year 2021

3.

Synthesis, characterization and antimalarial activity of isoquinoline derivatives

Theeramunkong S*, Thiengsusuk A, Vajragupta O, Muhamad P..
Medicinal chemistry research 2021; 30(1): 109-119., 2021.

Year 2020

4.

α7-Nicotinic acetylcholine receptor antagonist QND7 suppresses non-small cell lung cancer cell proliferation and migration via inhibition of Akt/mTOR signaling.

Witayateeraporn W, Arunrungvichian K, Pothongsrisit S, Doungchawee J, Vajragupta O, Pongrakhananon V*..
Biochem biophys res commun 2020; 521(4): 977-983., 2020.

5.

In silico finding of key interaction mediated α3β4 and α7 nicotinic acetylcholine receptor ligand selectivity of quinuclidine-triazole chemotype

Arunrungvichian K, Chongruchiroj S, Sarasamkan J, Schüürmann G, Brust P, Vajragupta O*..
International journal of molecular sciences 2020; 21(17): 6189: 1-18., 2020.

6.

Lead discovery of a guanidinyl tryptophan derivative on amyloid cascade inhibition

Suwanttananuruk P, Jiaranaikulwanitch J*, Waiwut P, Vajragupta O..
Open chemistry 2020;18(1): 546-548., 2020.

Year 2017

7.

Design and synthesis of caffeic amides by structure-based approaches

Mudjupa C, Theeramunkong S, Vajragupta O*..
Chiang Mai Journal of Science 2017; 44(2): 617-629., 2017.

8.

Neuritogenic activity of bi-functional bis-tryptoline triazole

Jiaranaikulwanitch J*, Tadtong S, Govitrapong P, Fokin VV, Vajragupta O..
Bioorganic and Medicinal Chemistry 2017; 25(3): 1195-1201, 2017.

9.

Radiosynthesis of (S)-[18F]T1: The first PET radioligand for molecular imaging of α3β4 nicotinic acetylcholine receptors

Sarasamkan J, Fischer S, Deuther-Conrad W, Ludwig F-A, Scheunemann M, Arunrungvichian K, Vajragupta O, Brust P*..
Applied Radiation and Isotopes 2017; 124: 106-113., 2017.

Year 2016

10.

Antiangiogenic Effects of VH02, a Novel Urea Derivative: In Vitro and in Vivo Studies.

Phowichit S, Kobayashi M, Fujinoya Y, Sato Y, Sanphanya K, Vajragupta O, Chularojmontri L, Wattanapitayakul SK*..
Molecules. 2016; 21(9): E1258., 2016.

11.

Design and Synthesis of Nicotinic Acetylcholine Receptor Antagonists and their Effect on Cognitive Impairment

Jaikhan P, Boonyarat C, Arunrungvichian K, Taylor P, Vajragupta O*..
Chemical Biology & Drug Design 2016; 87(1): 39-56., 2016.

12.

Development and validation of high-performance liquid chromatography method for determination of miconazole, triamcinolone, methylparaben and propylparaben in cream

Ei ZZ, Pimthon J, Vajragupta O, Leanpolchareanchai J, Phechkrajang CM*..
Mahidol University Journal of Pharmaceutical Sciences 2016; 43 (4): 211-221, 2016.

13.

Role of scavenger receptors in peptide-based delivery of plasmid DNA across a blood-brain barrier model

Srimanee A*, Regberg J, Hällbrink M, Vajragupta O, Langel Ü..
International Journal of Pharmaceutics 2016; 500(1): 128-135., 2016.

14.

Synthesis and biological evaluation of simplified analogs of lophocladine B as potential antitumor agents

Theeramunkong S*, Vajragupta O, Mudjupa C..
Medicinal Chemistry Research 2016; 25(12): 2959-2964., 2016.

15.

Varying Chirality Across Nicotinic Acetylcholine Receptor Subtypes: Selective Binding of Quinuclidine Triazole Compounds.

Sarasamkan J, Scheunemann M, Apaijai N, Palee S, Parichatikanond W, Arunrungvichian K, Fischer S, Chattipakorn S, Deuther-Conrad W, Schüürmann G, Brust P, Vajragupta O..
ACS Medicinal Chemistry Letters 2016; 7(10): 890-895., 2016.

Year 2015

16.

Cognitive improvement in a mouse model with substituted 1,2,3-triazole agonists for nicotinic acetylcholine receptors.

Arunrungvichian K, Boonyarat C, Fokin VV, Taylor P, Vajragupta O*..
ACS Chemical Neuroscience 2015, 6(8):1331-40., 2015.

17.

Effect of N-terminal truncation on antibacterial activity, cytotoxicity and membrane perturbation activity of Cc-CATH3

Jittikoon J*, Ngamsaithong N, Pimthon J, Vajragupta O..
Archives of Pharmacal Research 2015; 38(10): 1839-1849, 2015.

18.

Lead compound bearing caffeic scaffold induces EGFR suppression in solid tumor cancer cells

Mudjupa C, Abdelhamed S, Refaat A, Yokoyama S, Saiki I, Vajragupta O*..
Journal of applied biomedicine 2015; 13(4): 305-317, 2015.

19.

Selectivity Optimization of Substituted 1,2,3-Triazoles as α7 Nicotinic Acetylcholine Receptor Agonists

Arunrungvichian K, Fokin VV, Vajragupta O*, Taylor P..
ACS Chemical Neuroscience 2015; 6(8): 1317-1330, 2015.

Year 2014

20.

Development of Chemometric Tool for Determination of Peptide Samples Comparing with High-Performance Liquid Chromatography

Phechkrajang C, Jarusintanakorn S, Vajragupta O..
Mahidol University Journal of Pharmaceutical Sciences 2014; 41 (4), 18-28, 2014.

21.

Heptaphylline induces apoptosis in human colon adenocarcinoma cells through bid and Akt/NF-kappaB (p65) pathways.

Boonyarat C, Yenjai C, Vajragupta O, Waiwut P*..
Asian Pacific Journal of Cancer Prevention 2014; 15(23): 10483-10487, 2014.

22.

Peptide-based delivery of oligonucleotides across blood-brain barrier model

Srimanee A*, Regberg J, Hallbrink M, Kurrikoff K, Veiman K.-L, Vajragupta O, Langel U..
International Journal of Peptide Research and Therapeutics 2014; 20(2): 169-178, 2014.

23.

Synthesis, biological evaluation and molecular modeling study of novel tacrine-carbazole hybrids as potential multifunctional agents for the treatment of Alzheimer’s disease

Thiratmatrakul S, Yenjai C, Waiwut P, Vajragupta O, Reubroycharoen P, Tohda M, Boonyarat C*..
European Journal of Medicinal Chemistry 2014; 75: 21-30, 2014.

Year 2013

24.

Novel VEGFR-2 kinase inhibitors identified by the back-to-front approach

Sanphanya K, Wattanapitayakul SK, Phowichit S, Fokin VV, Vajragupta O*..
Bioorganic and Medicinal Chemistry Letters 2013; 23(10): 2962-2967, 2013.

25.

Synthesis, Topoisomerase I Inhibitory and Cytotoxic Activities of Chromone Derivatives

Maicheen C, Jittikoon J, Vajragupta O, Ungwitayatorn J*..
Medicinal Chemistry 2013; 9(3): 329-339, 2013.

Year 2012

26.

Antibacterial Activity of Cc-CATH3 Peptide and its N-terminally Truncated Analogues against Gram-positive and Gram-negative Bacteria.

Ngamsaithong N, Pimthon J, Vajragupta O, Jittikoon J*..
Mahidol University Journal of Pharmaceutical Sciences 2012; 39(2): 1-6, 2012.

27.

From BACE1 Inhibitor to Multifunctionality of Tryptoline and Tryptamine Triazole Derivatives for Alzheimer’s Disease

Jiaranaikulwanitch J, Govitrapong P, Fokin VV, Vajragupta O*..
Molecules 2012; 17(7): 8312-8333, 2012.

28.

Molecular Dynamics and Experimental Investigations of Membrane Perturbation by Ceragenin CSA-13

Jueati R, Jittikoon J, Vajragupta O, Pimthon J*..
Mahidol University Journal of Pharmaceutical Sciences 2012; 40(2): 25-32, 2012.

29.

Synthesis and evaluation of 1-(substituted)-3-prop-2-ynylureas as antiangiogenic agents

Sanphanya K, Wattanapitayakul SK, Prangsaengtong O, Jo M, Koizumi K, Shibahara N, Priprem A, Fokin VV, Vajragupta O*..
Bioorganic and Medicinal Chemistry Letters 2012; 22(8): 3001-3005, 2012.

30.

The effect of crebanine on memory and cognition impairment via the alpha-7 nicotinic acetylcholine receptor

Rojsanga P, Boonyarat C, Utsintong M, Nemecz A, Yamauchi JG, Talley TT, Olson AJ, Matsumoto K, Vajragupta O*..
Life Sciences 2012; 91(3 มิ.ย.): 107-114, 2012.

31.

Virtual screening against acetylcholine binding protein

Utsintong M, Rojsanga P, Ho K-Y, Talley TT, Olson AJ, Matsumoto K, Vajragupta O*..
Journal of Biomolecular Screening 2012; 17(2): 204-215, 2012.

Year 2011

32.

Antifungal, cytotoxic activities and docking studies of 2,5-dimercapto-1,3,4-thiadiazole derivatives

Samee W*, Vajragupta O..
African Journal of Pharmacy and Pharmacology 2011; 5(4): 477-485, 2011.

Year 2010

33.

Authentication of coscinium fenestratum among the other menispermaceae plants prescribed in Thai folk medicines.

Watthanachaiyingcharoen R, Komatsu K, Zhu S, Vajragupta O, Leelamanit W*..
Biol Pharm Bull 2010; 33(1): 91-94., 2010.

34.

Triazolyl tryptoline derivatives as β-secretase inhibitors

Jiaranaikulwanitch J, Boonyarat C, Fokin VV, Vajragupta O*..
Bioorg Med Chem Lett. 2010: 20(22): 6572-6576., 2010.

Year 2009

35.

5-substituted pyrido[2,3-d]pyrimidine, an inhibitor against three receptor

Kammasud N, Boonyarat C, Sanphanya K, Utsintong M, Tsunoda S, Sakurai H, Saiki I, André I, Grierson DS, Vajragupta O*..
Bioorg Med Chem lett 2009 ;19(3):745-50., 2009.

36.

Rediocides A and G as potential antitoxins against cobra venom

Utsintong M, Kaewnoi A, Leelamanit W, Olson AJ, Vajragupta O*..
Chem Biodivers 2009; 6(9): 1404-1414., 2009.

37.

Virtual screening against {alpha}-cobratoxin

Utsintong M, Talley TT, Taylor PW, Olson AJ, Vajragupta O*..
J Biomol Screen 2009; 14(9): 1109-1118., 2009.

Year 2007

38.

Effects of manganese complexes of curcumin and diacetylcurcumin on kainic acid-induced neurotoxic responses in the rat hippocampus

Sumanont Y, Murakami Y,Tohda M , Vajragupta O, Watanabe H, Matsumoto K*..
Biol Pharm Bull 2007;30(9) Sep: 1732—1739, 2007.

Year 2006

39.

A novel neuroprotective agent with antioxidant and nitric oxide synthase inhibitory action

Vajragupta O*, Boonyarat C, Olson AJ, Murakami Y, Tohda M, Matsumoto K, Watanabe H..
Free Radic Res 2006; 40(7): 685-95., 2006.

40.

Prevention of kainic acid-induced changes in nitric oxide level and neuronal cell damage in the rat hippocampus by manganese complexes of curcumin and diacetylcurcumin.

Sumanont Y, Murakami Y, Tohda M, Vajragupta O, Watanabe H, Matsumoto K*..
Life Sci 2006; 78(16): 1844-1849., 2006.

Year 2005

41.

Active site binding modes of curcumin in HIV-1 protease And integrase

Vajragupta O*, Boonchoong P, Morris MG, and Olson JA..
Bioorganic & Medicinal Chemistry letters 2005; 15(14): 3364-3368, 2005.

Year 2004

42.

Antoixidant activity of Limnophila aromatica Merr

Sribusarakum A, Bunyapraphatsara N, Vajragupta O, Watanabe H.
Thai J Phytopharm 2004;11(2):11-17, 2004.

43.

Evaluation of the nitric oxide radical scavenging activity of manganese complexes of curcumin and its derivative

Sumanont Y, Murakami Y, Tohda M, Vajragupta O, Matsumoto K, Watanabe H*..
Biol Pharm Bull 2004;27(2):170-3., 2004.

Year 2003

45.

Amides from natural acids against oxidative Stress.

Vajragupta O, Utsintong M, Peungvicha P, Watanabe H.
Mahidol J Pharm Sci 2003;30(2):27-36, 2003.

46.

Cytoprotective and cytotoxic effects of curcumin: Dual action on H2O2-induced oxidative cell damage in NG108-15 cells.

Mahakunakorn P, Tohda M, Murakami Y, Matsumoto K, Watanabe H*, Vajragupta O..
Biol Pharm Bull 2003; 26(5): 725-8, 2003.

47.

Effect of pH, buffer concentration ionic strength and temperature on ketoconazole stability in acidic solutions.

Junyaprasert VB, Techowanich S, Vajragupta O, Mitrevej A..
Mahidol J Pharm Sci 2003;30(2):17-36, 2003.

48.

Maganese complexes of curcumin: Radical scavenger and neuroprotective agents.

Vajragupta O,Boonchoong P, Watanabe H, Tohda M, Kummasud N, Sumanont Y..
Free Radic Res 2003; 37: 49 (suppl 1), 2003.

49.

Manganese complexes of curcumin analogues: Evalution of hydroxyl radical scavenging ability, superoxide dismutase activity and stability towards hydrolysis

Boonchoong P, Vajragupta O, Berliner LJ..
Free Radic Res 2003; 37: 51 (suppl 1), 2003.

50.

Manganese complexes pf curcumin and its derivatives: evaluation for the radical scavenging ability and neuroprotective activity.

Vajragupta O*, Boonchoong P, Watanabe H, Tohda M, Kummasud N, Sumanont Y..
Free Radic Biol Med35(12):1632-44, 2003; 35(12): 1632-1644, 2003.

51.

Manganese-Based Complexs of Radical Scavengers as Neuroprotective Agents.

Vajragupta O*, Boonchong P, Yaowared S,Hiroshi W, Wongkrajang Y, Kammasud N..
Bioorganic & Medicinal Chemistry 2003;11:2329-2337, 2003.

Year 2002

52.

Neuroprotection of Hydroxynicotinyl Amide 18 against Lipid Peroxidation and Memory Impairment.

Vajragupta O, Monthakantirat O, Boonchong P, Watanabe H, Peungvicha P..
Mahidol J Pharm Sci 2002; 29: 33-43, 2002.

53.

New leads of HIV-1 Integrase Inhibitors

Vajragupta O,Boonchoong P.
Mahidol J Pharm Sci 2002; 29(3-4), 2002.

Year 2000

54.

Chromanamide 12 : inhibition of lipid peroxidation and protection against learning and memory impairment.

Vajragupta O*, Monthakanrat O, Wongkrajang, Y, Watanabe H, Peungvicha P.
Life Sci 2000; 67(14): 1725-1734, 2000.

55.

Chromanamide and nicotinyl amide derivatives : inhibition of lipid peroxidation and protection against head trauma

Vajragupta O*, Toasaksiri S, Boonyarat C, Wongkrajang Y, Peungvicha P.
Free Radic Res 2000; 32(2): 145-155, 2000.

56.

Comparative quantitative structure-activity study of radical scavengers.

Vajragupta O*, Boonchoong P, Wongkrajang Y..
Bioorg Med Chem 2000; 8(11): 2617-2628, 2000.

Year 1997

57.

Differential scanning colorimeter in purity determination on pharmaceutical raw material.

Vajragupta O, Silapakalpradit W, Pitijomwong W, La-ong S..
J Ind Pharm 1997; 2(2): 29-37, 1997.

Year 1996

58.

Betacarotene serum profile after single dose adminstration of betacarotene capsule v.s. carrot.

Chindavijak B, Sornsuvit C, Vajragupta O, Pattamakom V..
Thai J Phytopharm 1996; 3:7-15, 1996.

59.

Synthesis and antihypertensive activity of N-(Alkyl/alkenyl/aryl)-N-heterocyclic ureas and thioureas.

Vajragupta O, Pathomsakul A, Matayatsuk C, Rungreuangyingyod L, Wongkrajang Y, Foye OW..
Journal of Pharmaceutical Sciences 1996; 85 (3): 258-61, 1996.

Year 1995

60.

24 hour serum level after a single dose administration of beta-carotene capsule.

Chindavijak B, Soontornpass C, Vajragupta O.
Mahidol J Pharm Sci 1995; 22:92-100, 1995.

Year 1993

61.

Synthesis and skin permeation study of lidocaine organic salts.

Vajragupta O, La-ong S..
Drug Dev Ind Pharm 1993;20:2671-84, 1993.


Presentation

Year 2017

1.

Development of (S)-[18F]T1 as first PET tracer for imaging the α3β4 nicotinic acetylcholing receptor

Sarasamkan J, Fischer s, Deuther-Conrad W, Ludwig FA, Scheunemann M, Vajragupta O*, Brust P..
22nd International Symposium on Radiopharmaceutical Scinces 2017;, 2017.

Year 2014

2.

Drug discovery and pre-clinical development of small molecule therapeutics for cancer and neurodegenerative disorders

Vajragupta O*..
การประชุมสุดยอดมหาวิทยาลัยวิจัยแห่งชาติ ครั้งที่ 3 (31 ก.ค. -1 ส.ค.57) ณ บางกอกคอนเวนชั่นเซ็นเตอร์ ชั้น 22 โรงแรมเซ็นทาราแกรนด์ เซ็นทรัลเวิลด์ กรุงเทพฯ , 2014.

Year 2012

3.

Structural modifications of virtual lead active on alpha 7 nicotinic acetylcholine as anticancer agents. .

Jaikhan P, Boonyarat C,Vajragupta O. The 15th Hellenic Symposium on Medicinal Chemistry,Athens .
Frontiers in Plant Science 2012; May 25-27, , 2012.

Year 2011

4.

Multifunctional of tryptoline and tryptamine triazole derivatives for Alzheimer’s disease.

Jiaranaikulwanitch J, Utsintong M, Fokin VV, Vajragupta O. The 4th International Symposium on Advances in Synthetic and Medicinal Chemistry (ASMC2011). .
Frontiers in Plant Science August 21-25, 2011. St. Petersburg, Russia., 2011.

5.

Synthesis and molecular docking studies of DPP IV inhibitors bearing chromone scaffold.

33. Theeramunkong S, Swainoi W, Prasertchareonsuk W, Keawnoi A, Vajragupta O. The 4th International Symposium on Advances in Synthetic and Medicinal Chemistry (ASMC2011). .
Frontiers in Plant Science August 21-25, 2011. St. Petersburg, Russia., 2011.

Year 2009

6.

Enhancing internationalisation though collaborative research in PhD programmes: a case study from the Faculty of Pharmacy, Mahidol University

Vajragupta O.*.
The 5th QS-APPLE Annual Conference, Kuala Lumpur Conference Centre (KLCC), November 24-26, 2009, Kuala Lumpur, Malaysia 2009, 2009.

7.

Virtual Screening against Vascular Endothelial Growth Factor Receptor 2

Mudjupa C, Boonyarat C, Vajragupta O* .
12th MipTec Conference –The Leading European Event for Drug Discovery, Congress Center Basel, Switzerland, October 13 - 15, 2009 2009, 2009.

Year 2008

8.

Dipeptidylpeptidase IV inhibitors from structure-based design using scaffold derived from herbal active components

Theeramunkong S, Vajragupta O. .
Drug of the Future / XXth Int Symp Med Chem (Aug 31-Sept 4, Vienna) 2008; 33(Suppl. A): 212-213, 2008.

9.

Virtual screening against cobra venom.

Utsintong1 M, Taylor PW, Olson AJ, Vajragupta O. .
Drugs of the Future/XXth Int Symp Med Chem (Aug 31-Sept 4, Vienna) 2008; 33(Suppl. A): 204-205., 2008.

Year 2007

10.

Detoxification Mechanism of Rediocides against Cobra Venom

Vajragupta O, Utsintong M, Leelamanit W, Kaewnoi A, Olson AJ..
Screening & MedChem Europe 2007, February 20-21 2007, Barcelona, Spain , 2007.

Year 2006

11.

A novel neuroprotective agent with antioxidant and nitric oxide synthase inhibitory action.

Boonyarat C, Vajragupta O, MurakamiY, Tohda Y, Musatmoto K, Olson AJ, Watanabe H..
Drug of the Future, 2006; 31 (Suppl. A):120/. International Symposium on Medicinal Chemistry (ISMC - 2006) 120, 2006.

Year 2005

12.

Neuronal Nitric Oxide Template: useful for Virtual Screening.

Vajragupta O, Boonyarat C, Morris GM, Huey R, Li C, Olson AJ..
30th FEBS Congress - 9th IUBMB Conference, July 2-7, 2005, Budapest, Hungary. FEBS 2005;272(Suppl. 1):431, 2005.

13.

Structure-based design of novel inhibitors of FGFr and VEGFr as anti-angiogenesis agents

Kammasuda,N, André I, Grierson DS, Vajragupta O. .
The 7th International Conference on Chemical Structures (ICCS 2004), Noordwijkerhout, The Netherlands. 2005, 2005.

Year 2004

14.

A novel neuroprotective agent : a dual action of radical scavenger and nitric oxide synthase inhibitor

Vajragupta O, Watanabe H, Boonyarat C..
Drug of the Future 2004;29(Suppl. A):231, 2004.

เกี่ยวกับภาควิชา

The ultimate success of a pharmacist's practice relies on applying expertise to minimize the consumer's risk of harm from medication while maximizing the positive outcomes in disease prevention and treatment.

The ultimate success of a pharmacist's practice relies on applying expertise to minimize the consumer's risk of harm from medication while maximizing the positive outcomes in disease prevention and treatment.
Pradit Hutangura
The First Dean of Faculty of Pharmacy, Mahidol University
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