Publication

Research Papers : 2004-2010

2010

• Design and synthesis of KNT-127, a δ-opioid receptor agonist effective by systemic administration
  Nagase, H.; Nemoto, T.; Matsubara, A.; Saito, M.; Yamamoto, N.; Osa, Y.; Hirayama, S.; Nakajima, M.; Nakao K.; Mochizuki, H.; Fujii, H.
  Bioorg. Med. Chem. Lett., 2010, 20, 6302-6305.
• Synthesis of pyrrolomorphinan derivatives as κ opioid agonists
  Fujii, H.; Ida, Y.; Hanamura, S.; Osa, Y.; Nemoto, T.; Nakajima, M.; Hasebe, K.; Nakao K.; Mochizuki, H.; Nagase, H.
  Bioorg. Med. Chem. Lett., 2010, 20, 5035-5038.
• Investigation of Beckett-Casy model 3: Synthesis of novel naltrexone derivatives with contracted and expanded D–rings and their pharmacology
  Nagase, H.; Imaide, S.; Tomatsu, M.; Hirayama, S.; Nemoto, T.; Sato, N.; Nakajima, M.; Nakao K.; Mochizuki, H.; Gouda, H.; Hirono, S.; Fujii, H.
  Bioorg. Med. Chem. Lett., 2010, 20, 3801–3804.
• Investigation of Beckett-Casy model 2: Synthesis of novel 15–16 nornaltrexone derivatives and their pharmacology
  Nagase, H.; Imaide, S.; Tomatsu, M.; Nemoto, T.; Nakajima, M.; Nakao, K.; Mochizuki, H.; Fujii, H.
  Bioorg. Med. Chem. Lett., 2010, 20, 3726–3729.
• Identification of the three-dimensional pharmacophore of κ-opioid receptor agonists
  Yamaotsu, N.; Fujii, H.; Nagase, H.; Hirono, S.
  Bioorg. Med. Chem., 2010, 18, 4446.
• A Double Decarboxylation Reaction of an Oxazolidinone and Carboxylic Acid: Its Application to the Synthesis of a New Opioid Lead Compound.
  Fujii, H.; Imaide, S.; Watanabe, A.; Yoza, K.; Nakajima, M.; Nakao, K.; Mochizuki, H.; Sato, N.; Nemoto, T.; Nagase, H.
  J. Org. Chem., 2010, 75, 995-998.
• Investigation of Beckett–Casy model 1: Synthesis of novel 16,17-seco-naltrexone derivatives and their pharmacology.
  Imaide, S.; Fujii, H.; Watanabe, A.; Nemoto, T.; Nakajima, M.; Nakao, K.; Mochizuki, H.; Nagase, H.
  Bioorg. Med. Chem. Lett., 2010, 20, 1055-1058.
• Drug design and synthesis of a novel opioid receptor agonist with an oxabicyclo[2.2.2]octane skeleton and its pharmacology
  Nagase, H.; Watanabe, A.; Nemoto, T.; Yamaotsu, N.; Hayashida, K.; Nakajima, M.; Hasebe, K.; Nakao, K.; Mochizuki, H.; Hirono S.; Fujii, H.
  Bioorg. Med. Chem. Lett., 2010, 20, 121-124.

2009

• Hydrogenolysis of the cyclopropyl group into an isopropyl group in the presence of a platinum catalyst and hydrobromic acid.
  Fujii, H.; Okada. K; Ishihara, M.; Hanamura, S.; Osa, Y.; Nemoto, T; Nagase, H.
  Tetrahedron, 2009, 65, 10623-10630.
• Aerobic oxidation of indolomorphinan without the 4,5-epoxy bridge and subsequent rearrangement of the oxidation product to spiroindolinonyl-C-normorphinan derivative.
  Fujii, H.; Ogawa. R; Ohata, K.; Nemoto, T.; Nakajima, M.; Hasebe, K.; Mochizuki, H.; Nagase, H.
  Bioorg. Med. Chem., 2009, 17, 5983-5988.
• Novel Oxidation Reaction of Tertiary Amines with Osmium Tetroxide.
  Fujii, H.; Ogawa, R.; Jinbo, E.; Tsumura, S.; Nemoto, T.; Nagase, H.
  Synlett, 2009, 14, 2341-2345.
• Novel rearrangement reaction of a 6,14-endoethanomorphinan derivative to a benzomorphan derivative.
  Fujii, H.; Watanabe, Y.; Osa, Y.; Nemoto, T.; Sato, N.; Nagase, H.
  Tetrahedron, 2009, 65, 4808-4813.
• Design and synthesis of novel delta opioid receptor agonists and their pharmacologies.
  Nagase, H.; Osa, Y.; Nemoto, T.; Fujii, Hl.; Imai, M.; Nakamura, T.; Kanemasa, T.; Kato, A.; Gouda, H.; Hirono, S.
  Bioorg. Med. Chem. Lett., 2009, 19, 2792–2795.
• Synthesis of a new opioid ligand having the oxabicyclo[3.2.1]octane skeleton using a new rearrangement reaction.
  Watanabe, A.; Fujii, H.; Nakajima, M.; Hasebe, K.; Mochizuki, H.; Nagase, H.
  Bioorg. Med. Chem. Lett., 2009, 19, 2416-2419.
• Novel Synthesis of a 1,3,5-Trioxazatriquinane Skeleton Using a Nitrogen Clamp.
  Nagase, H.; Watanabe, A.; Harada, M.; Nakajima, M.; Hasebe, K.; Mochizuki, H.; Yoza, K.; Fujii, H.
  Org. Lett., 2009, 11, 539-542.
• Synthesis of novel twin drug consisting of 8-oxaendoethanotetrahydromorphides with a 1,4-dioxane spacer and its pharmacological activities: μ, κ, and putative ε opioid receptor antagonists.
  Fujii, H.; Watanabe, A.; Nemoto, T.; Narita, M.; Miyoshi, K.; Nakamura, A.; Suzuki, T.; Nagase, H.
  Bioorg. Med. Chem. Lett., 2009, 19, 438-441.

2008

• Synthesis of a novel 6, 14-epoxymorphinan derivative and its pharmacology.
  Nemoto, T.; Fujii, H.; Narita, M.; Miyoshi, K.; Nakamura, A.; Suzuki, T.; Nagase, H.
  Bioorg. Med. Chem. Lett., 2008, 18, 6398-6401.
• (3R)-3-Amino-4-(2,4,5-trifluorophenyl)-N-{4-[6-(2-methoxyethoxy)benzothiazol-2-yl]tetrahydropyran-4-yl} butanamide as a Potent Dipeptidyl Peptidase IV Inhibitor for the Treatment of Type 2 Diabetes.
  Nitta, A.; Fujii, H.; Sakami, S.; Nishimura, Y.; Ohyama, T.; Satoh, M.; Nakaki, J.; Satoh, S.; Inada, C.; Kozono, H.; Kumagai, H.; Shimamura, M.; Fukazawa, T.; Kawai, H.
  Bioorg. Med. Chem. Lett., 2008, 18, 5435-5438.
• Design, Synthesis, and Structure-Activity Relationship of Novel Opioid κ-Agonists.
  Kawai, K.; Hayakawa, J.; Miyamoto, T.; Imamura, Y.; Yamane, S.; Wakita, H.; Fujii, H.; Kawamura, K.; Matsuura, H.; Izumimoto, N.; Kobayashi, R.; Endo, T.; Nagase, H.
  Bioorg. Med. Chem., 2008, 16, 9188-9201.
• Synthesis of a Stable Iminium Salt and Propellane Derivatives.
  Nagase, H.; Yamamoto, N.; Nemoto, T.; Yoza, K.; Kamiya, K.; Hirono, S.; Momen, S.; Izumimoto, N.; Hasebe, K.; Mochizuki, H.; Fujii, H.
  J. Org. Chem., 2008, 73, 8093-8096.
• Novel cleavage reaction of the C16-N17 bond in naltrexone derivatives.
  Fujii, H.; Imaide, S.; Watanabe, A.; Nemoto, T.; Nagase, H.
  Tetrahedron Lett., 2008, 49, 6293-6296.
• Synthesis of N-isobutylnoroxymorphone from naltrexone by a selective cyclopropane ring opening reaction.
  Fujii, H.; Osa, Y.; Ishihara, M.; Hanamura, S.; Nemoto, T.; Nakajima, M.; Hasebe, K.; Mochizuki, H.; Nagase, H.
  Bioorg. Med. Chem. Lett., 2008, 18, 4978-4981.
• Design and synthesis of a metabolically stable and potent antitussive agent, a novel δ opioid receptor antagonist, TRK-851.
  Sakami, S.; Kawai, K.; Maeda, M.; Aoki, T.; Fujii, H.; Ohno, H.; Ito, T.; Saitoh, A.; Nakao, K.; Izumimoto, N.; Mastuura, H.; Endo, T.; Ueno, S.; Nastume, K.; Nagase, H.
  Bioorg. Med. Chem., 2008, 16, 7956-7967.
• Structure-Antitussive Activity Relationships of Naltrindole Derivatives. Identification of Novel and Potent Antitussive Agents.
  Sakami, S.; Maeda, M.; Kawai, K.; Aoki, T.; Kawamura, K.; Fujii, H.; Hasebe, K.; Nakajima, M.; Endo, T.; Ueno, S.; Ito, T.; Kamei, J.; Nagase, H.
  J. Med. Chem., 2008, 51, 4404-4411.
• Syntheses of 4,6'-epoxymorphinan derivatives and their pharmacologies.
  Nemoto, T.; Fujii, H.; Narita, M.; Miyoshi, K.; Nakamura, A.; Suzuki, T.; Nagase, H.
  Bioorg. Med. Chem., 2008, 16, 4304-4312.
• 非ペプチド性GLP-1作動薬/経口糖尿病治療薬への可能性
  藤井秀明
  ファルマシア, 2008, 44, 79-80.

2007

• Synthesis of a novel 4,6'-epoxymorphinan derivative and a highly strained novel conjugated ketone.
  Nemoto, T.; Fujii, H.; Sato, N.; Nagase, H.
  Tetrahedron Lett., 2007, 48, 7413-7417.
• Catalytic Aerobic Oxidation of nor-Binaltorphimine (nor-BNI) Analogs without 4,5-Epoxy Bridge Affords a More Selective Ligand for kappa Opioid Receptor than the Representative kappa Antagonist nor-BNI.
  Osa, Y.; Ida, Y.; Fujii, H.; Nemoto, T.; Hasebe, K.; Momen, S.; Mochizuki, H.; Nagase, H.
  Chem. Pharm. Bull., 2007, 55, 1489-1493.
• Synthesis of Opioid Ligands Having Oxabicyclo[2.2.2]octane and Oxabicyclo[2.2.1]heptanes Skeletons.
  Nagase, H.; Watanabe, A.; Nemoto, T.; Yamamoto, N.; Osa, Y.; Sato, N.; Yoza, K.; Kai, T.
  Tetrahedron Lett., 2007, 48, 2547-2553.

2004

• The First Example of the Stereoselective Synthesis of 7β-Carbamoyl-4,5α-epoxymorphinan via a Nobel and Reactive γ-Lactone.
  Fujii, H.; Hirano, N.; Uchiro, H.; Kawamura, K.; Nagase, H.
  Chem. Pharm. Bull., 2004, 52, 747-750.
• Drug design and synthesis ofε-opioid receptor agonist: 17-(cyclopropylmethyl)-4,5α-epoxy-3,6,β-dihydroxy-6,14-endoethenomorphinan-7α-(N-methyl-N-phenethyl)carboxamide (TAN-821) inducing antinociception mediated by putative ε-opioid receptor.
  Fujii, H.; Narita, M.; Mizoguchi, H.; Murachi, M.; Tanaka, T.; Kawai, K.; Tseng, L. F.; Nagase, H.
  Bioorg. Med. Chem. Lett., 2004, 12, 4133-4145.
• Rational Drug Design and Synthesis of a Selective ε-Opioid Receptor Antagonist on the Basis of the Accessory Site Concept.
  Fujii, H.; Narita, M.; Mizoguchi, H.; Hirokawa, J.; Kawai, K.; Tanaka, T.; Tseng, L. F.; Nagase, H.
  Bioorg. Med. Chem. Lett., 2004, 14, 4241-4243.