Graduate School and School of Pharmaceutical Sciences, The University of Osaka

Research

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Faculty Members

Drug Innovation Center Lead Exploration Unit

Kobayashi NaotakeSpecially Appointed Assosiate Professor

[Education]
1993 Department of Pharmacy, Faculty of Pharmaceutical Sciences, Tokyo University of Pharmacy and Life Science
1995 Department of Life Science and Technology, Graduate School of Life Science, Tokyo Institute of Technology
2022 Ph.D (Engineering, Kyoto University)
　“The discovery of orally effective thyrotropin-releasing hormone (TRH) mimetic: Rovatirelin Hydrate”
[Work Experience]
1995 Shionogi Pharmaceutical Company Ltd. Pharmaceutical Research Division
2021 Shionogi TechnoAdvance Research Co., Ltd.
2022 Lead Exploration Units, Graduate School of Pharmaceutical Science, Osaka University

Research theme

Drug discovery support based on academic seeds

In order to develop academia seeds into drug candidates, following supports using the knowledge and technology cultivated at pharmaceutical companies are provided:
1. Investigate the latest information on drug discovery targets and provide advice and proposals.
2. Evaluate hit compounds from the perspective of medicinal chemistry and ADME-T, and optimize their structures for drug candidates.
3. Provide advice and proposals for joint research and out-licensing with pharmaceutical companies.

Representative achievements

Revaluation of thyrotropin-releasing hormone and its mimetics as candidates for treating a wide range of neurological and psychiatric disorders.
Kobayashi, N.; Kihara, T.
Frontiers in Clinical Drug Research – CNS and Neurological Disorders Volume 9, Chapter 4, Atta-ur-Rahman, Zareen Amtul, Eds: Bentham Science Publishers: United Arab Emirates, Sharjah, 2021; pp 90-136.

URL:https://www.eurekaselect.com/chapter/15563

Discovery of orally effective thyrotropin-releasing hormone (TRH) mimetic: 1-{N-[(4S,5S)-(5-methyl-2-oxooxazolidine-4-yl)carbonyl]-3-(thiazol-4-yl)-L-alanyl}-(2R)-2-methylpyrrolidine trihydrate (Rovatirelin Hydrate).
Kobayashi, N.; Sato, N.; Fujimura, Y.; Kihara, T.; Sugita, K.; Takahashi, K; Koike, K.; Sugawara, T.; Tada, Y.; Nakai, H.; Yoshikawa, T.
ACS Omega 2018, 3(10), 13647–13666.

URL:https://pubs.acs.org/doi/10.1021/acsomega.8b01481

Synthesis and evaluation of in vivo anti-hypothermic effect of all stereoisomers of the thyrotropin-releasing hormone mimetic: Rovatirelin Hydrate.
Kobayashi, N.; Sato, N.; Sugita, K.; Takahashi, K.; Sugawara, T.; Tada, Y.; Yoshikawa, T.
Journal of Peptide Science 2019, 25(12), e3228.

URL:https://onlinelibrary.wiley.com/doi/10.1002/psc.3228

Synthesis and evaluation of in vivo anti-hypothermic effect of the N-and C-terminus modified thyrotropin-releasing hormone mimetic: [(4S,5S)-(5-methyl-2-oxooxazolidine-4-yl)carbonyl]-[3-(thiazol-4-yl)-L-alanyl]-L-prplinamide.
Kobayashi, N.; Sato, N.; Sugita, K.; Kihara, T.; Koike, K.; Sugawara, T.; Tada, Y.; Yoshikawa, T.
Chemical and Pharmaceutical Bulletin 2021, 69(4), 314-324.

URL:https://doi.org/10.1248/cpb.c20-00454

A novel method for the synthesis of macrocyclic peptides using arylsulfonyloxyacetic acids as N-terminus functional groups.
Kobayashi, N.; Nakamura, J.
Tetrahedron Letters 2024, 141(17), 155073.

URL:https://doi.org/10.1016/j.tetlet.2024.155073

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