Synthesis and molecular design of fused deazaflavin-steroid derivatives for biological and pharmacological activities

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This research is synthesis of the fused compounds that include two different existent physiological or pharmacological activities structurally at the same time. As a new trial in the active molecular design for drugs, I have made the plan for synthesis of such hybrid compounds like 5-deazaflavins and steroids, by expecting the bioactive potentiation or new bioactivities in the new hybrid compounds, and further I have done the search for the bioactivity of those new hybrid compounds. I describe the above research result that I got in the research period.We succeeded in the synthesis of the hybrid compounds that build in deazaflavin and steroid structures structurally at the same time. In these syntheses, we established the two kinds of simple synthetic methods. Namely the first method was the condensation of 3-morpholinoandrostene with appropriate 6-amino-5-formylpyrimidines in the presence of p-toluenesulfonic acid. The second method was the similar condensation of 2-hydroxymethylenean … More drostanolone with appropriate 6-aminopyrimidine derivatives. We tried the condensation reaction with the pyrimidine derivative and not only androstanolone but also testosterone or cholesterol derivative. The reaction has consequently been useful for the preparation of the desired hybrid compounds such as deazaflavin-androstanes and deazaflavin-cholestenes.We succeeded in the synthesis of the hybrid compounds that build in deazaflavin and steroid structures structurally at the same time. In these syntheses, we established the two kinds of simple synthetic methods. Namely the first method was the condensation of 3-morpholinoandrostene with appropriate 6-amino-5-formylpyrimidines in the presence of p-toluenesulfonic acid. The second method was the similar condensation of 2-hydroxymethyleneandrostanolone with appropriate 6-aminopyrimidine derivatives. We tried the condensation reaction with the pyrimidine derivative and not only androstanolone but also testosterone or cholesterol derivative. The reaction has consequently been useful for the preparation of the desired hybrid compounds such as deazaflavin-androstanes and deazaflavin-cholestenes.We examined the anti-coccidiosis activity for the hybrid compounds prepared here as one of search for the biological activities. Thus, some of the hybrid compounds showed more potent anti-coccidiosis activity than that of robenidine that was used as the positive control. Hereafter, the good result of the biological and pharmacological activities for these hybrid compounds will be expected. Less