Studies on Griseolic Acid Derivatives X. Synthesis and Phosphodiesterase Inhibitory Activity of 2-Substituted Derivatives of Griseolic Acid |
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| Authors: | Masakatsu Kaneko Misako Kimura Yoshinobu Murofushi Takashi Yasumoto Yasuteru Iijima Mitsuo Yamazaki |
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| Institution: | 1. Bioscience, New Lead , Research Laboratories, SANKYO CO., LTD. , 2-58 Hiromachi 1-chome Shinagawa-ku, Tokyo, 140;2. Fermentation , Research Laboratories, SANKYO CO., LTD. , 2-58 Hiromachi 1-chome Shinagawa-ku, Tokyo, 140 |
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| Abstract: | 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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