8-(Dicyclopropylmethyl)-1, 3-dipropylxanthine: a potent and selective adenosine A1 antagonist with renal protective and diuretic activities

…, H Nonaka, A Karasawa, H Mizumoto…

Index: Shimada, Junichi; Suzuki, Fumio; Nonaka, Hiromi; Karasawa, Akira; Mizumoto, Hideaki; et al. Journal of Medicinal Chemistry, 1991 , vol. 34, # 1 p. 466 - 469

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Citation Number: 40

Abstract

1, 3-Dipropyl-8-(3-pentyl) xanthine (14), a open-chain analogue of 4, had about 63-fold higher affinity to the A, receptor than a parent compound (3) and moderate A, selectivity. But 14 was a less potent A, antagonist than 4. A further increase or decrease in the size of alkyl substitutent (R'or R2) caused a loss of affinity at the Al receptor (compare 9, 10, and 17 with 14). An amino or a phenoxy group reduced affinity to Al and A2 receptors (1 1 and 16). ...