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Communication | Regular issue | Vol 63, No. 1, 2004, pp.9-16
Published online, 10th November, 2003
DOI: 10.3987/COM-03-9925
New Synthesis and Biologically Active Molecular Design of Deazapteridine-Steroid Hybrid Compounds

Tomohisa Nagamatsu,* Hiroki Yamada, and Kazuyuki Shiromoto

*Faculty of Pharmaceutical Science, Okayama University, 1-1-1 Tsushima-naka, Okayama 700-8530, Japan

Abstract

This paper describes a facile and general synthesis of a new class of the hybrid compounds (4, 5 and 16), possessing 5-deazapteridine and steroid in the same ring system, by condensation of 6-(monosubstituted amino)uracils (9) or 6-(monosubstituted amino)-2-phenylpyrimidin-4(3H)-ones (14) with 2-hydroxy-methyleneandrostanolone (10) or 2-hydroxymethylenetestosterone (15) under heating in the presence of p-toluenesulfonic acid monohydrate and their potential unti-coccidiosis activities.