Studies on Griseolic Acid Derivatives X. Synthesis and Phosphodiesterase Inhibitory Activity of 2-Substituted Derivatives of Griseolic Acid

Masakatsu Kaneko Bioscience, New Lead, Research Laboratories, SANKYO CO., LTD., 2-58 Hiromachi 1-chome Shinagawa-ku, Tokyo, 140

Misako Kimura Bioscience, New Lead, Research Laboratories, SANKYO CO., LTD., 2-58 Hiromachi 1-chome Shinagawa-ku, Tokyo, 140

Yoshinobu Murofushi Bioscience, New Lead, Research Laboratories, SANKYO CO., LTD., 2-58 Hiromachi 1-chome Shinagawa-ku, Tokyo, 140

Takashi Yasumoto Bioscience, New Lead, Research Laboratories, SANKYO CO., LTD., 2-58 Hiromachi 1-chome Shinagawa-ku, Tokyo, 140

Yasuteru Iijima Bioscience, New Lead, Research Laboratories, SANKYO CO., LTD., 2-58 Hiromachi 1-chome Shinagawa-ku, Tokyo, 140

Mitsuo Yamazaki Fermentation, Research Laboratories, SANKYO CO., LTD., 2-58 Hiromachi 1-chome Shinagawa-ku, Tokyo, 140

Abstract

Griseolic acid derivatives which were modified at the 2-and/or 6-positions were first synthesized from griseolic acid by a ring opening—reclosure reaction of the adenine ring. Among these derivatives, the 2-amino-6-deamino-6-hydroxyl (guanine) derivative showed 3.3 and 45 times stronger inhibitory activity against cAMP and cGMP PDE, respectively, than those of griseolic acid. Structure-activity relationships among these derivatives are also discussed.

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Studies on Griseolic Acid Derivatives X. Synthesis and Phosphodiesterase Inhibitory Activity of 2-Substituted Derivatives of Griseolic Acid

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Studies on Griseolic Acid Derivatives X. Synthesis and Phosphodiesterase Inhibitory Activity of 2-Substituted Derivatives of Griseolic Acid

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