AMIDATION OF HYALURONIC ACID WITH A METHOTREXATE-DERIVED AMINE: OPTIMIZATION OF THE KEY REACTION FOR THE SYNTHESIS OF A CANDIDATE DRUG FOR THE TREATMENT OF OSTEOARTHRITIS

作者：Homma Akie^*; Ishizawa Takenori; Sato Haruhiko; Okamachi Akira; Emura Takashi; Kato Tatsuya; Matsuura Tetsu; Sato Shigeo; Ikemi Masahisa; Kitagawa Hironoshin; Morikawa Tadashi; Ikeya Hitoshi; Takahashi Koichi

来源：Heterocycles, 2010, 82(1): 273-279.

DOI：10.3987/COM-10-S(E)41

• High Molecular Weight HA
• Degradation of HA
• Gel Permeation Chromatography
• Acetyltryptophan

Optimal amidation conditions between hyaluronic acid (HA) and a methotrexate (MTX)-derived amine that gave rise to a HA-MTX conjugate having a molecular weight of similar to 2000 kDa have been established based on a model experiment using a tryptophan-derived amine in aqueous THF. This method is robust and provides a conjugate with properties of primary importance for efficacy-MW and amine binding ratio-that satisfy the criteria for a HA-MTX conjugate to be a good candidate.

• 出版日期2010-12-31