Biologically Active Compounds

We had predicted in our 1-hydroxyindole hypothesis that the introduction of a hydroxy or an alkoxy group onto the 1-position of biologically inactive indole compounds makes them become biologically active compounds [1-7]. In addition, the application of the idea to the known biologically active indoles has their original activities improved or modified for the discovery of new drugs [1-7].

With these basic concepts, we have given birth to various biologically active compounds thus far and some examples are shown in our previous re views [1-7]. Notably, we have shown that simple 1-hydroxytryptamines are fundamentally inhibitors of blood platelet aggregation (for our new lead compounds for cerebral infarction and myocardial infarction see [43,44]). New compounds with potent activity are in preparation for patent application. Excluding these, we would like to introduce some of our biologically active compounds in this section.

Yohimbine ( 192a, Fig. 7) is a widely known a2-blocker effective in treating erectile dysfunction (ED). They have been used all over the world. A slight modification of its mother skeleton and the introduction of an alkyl group onto its N(1) position are shown to change its biological activity [45]. Therefore, we are interested in the preparation of 1-hydroxyyohimbine (192b) and its derivatives. As expected, 192b and some derivatives (192c-f) are a2-blockers as potent as yohimbine [46,47].

Compounds (193a,b-199a,b) have also been discovered to be a2-block-ers [46,47]. When the activity of yohimbine is made a standard for 100, those of 193a and 194a are 87.7 ± 8.53 and 17.8, respectively. The activity of compound (195a, 100.0 ± 0.00) is found to be equal to or more potent than yohimbine (192a) [46,47]. The 1-hydroxy compounds (193a and 195a) are stronger than the corresponding N(1)H compounds (193b and 195b), while 194a is weaker than 194b. In a series of Nb-acyltryptamines (196-199), differences in activities are small between 1-hydroxy and N(1)H compounds.

Pregnancy And Childbirth

Pregnancy And Childbirth

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