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Structure of HIV-1 protease with KNI-272, a tight-binding transition-state analog containing allophenylnorstatine.
Pharmacokinetic study of a tripeptide HIV‐1 protease inhibitor, KNI‐174, in rats after intravenous and intraduodenal administrations
- A. Kiriyama, T. Mimoto, Y. Kiso, K. Takada
- Biology, ChemistryBiopharmaceutics & drug disposition
- 1 April 1993
An HPLC assay system is developed and examined the pharmacokinetics of KNI‐174 in rats using this assay method after both intravenous and intraduodenal administrations to obtain the disposition characteristics and bioavailability of this new anti‐AIDS drug.
Synthesis of di- and tripeptide analogues containing alpha-ketoamide as a new core structure for inhibition of HIV-1 protease.
Comparison of a new orally potent tripeptide HIV‐1 protease inhibitor (anti‐aids drug) based on pharmacokinetic characteristics in rats after intravenous and intraduodenal administrations
- A. Kiriyama, T. Mimoto, S. Kisanuki, Y. Kiso, K. Takada
- Medicine, BiologyBiopharmaceutics & drug disposition
- 1 November 1993
Although the anti‐AIDS virus activity of these two drugs has not been investigated in vivo, KNI‐272 is expected to be a better candidate for oral anti-AIDS therapies.
Synthesis and in vivo evaluation of N-13 labeled opioid peptide analogue for PET opiate receptor studies
Synthesis and biological evaluation of a 13N-labeled opioid peptide.
A synthetic method suitable for the rapid preparation of 13N-labeled dermorphin analogue, H-Tyr-D-Met(O)-Phe-Gly-NH2 (SD-62).
- Y. Kiso, S. Iinuma, T. Mimoto, H. Saji, A. Yokoyama, K. Akaji
- Chemistry, BiologyChemical & pharmaceutical bulletin
- 25 October 1991
A synthetic method suitable for the preparation of 13N-labeled dermorphin analogue, H-Tyr-D-Met(O)-Phe-Gly-NH2 (SD-62), was established and the time profile of the radioactivity accumulation in the brain paralleled well that of the analgesic activity.