Synthesis of potential inhibitors of hypoxanthine-guanine phosphoribosyltransferase for testing as antiprotozoal agents. 2. 1-Substituted hypoxanthines

JR Piper, AG Laseter, TP Johnston…

Index: Piper, James R.; Laseter, Anne G.; Johnston, Thomas P.; Montgomery, John A. Journal of Medicinal Chemistry, 1980 , vol. 23, # 10 p. 1136 - 1139

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Citation Number: 10

Abstract

Evidence indicating that effective in vivo inhibition of hypoxanthine guanine phosphoribosyltransferase (HGPRT, EC 2.4. 2.8) should produce antiprotozoal activity without significant toxic effects on mammalian hosts prompted syntheses of 1-substituted hypoxanthine5 bearing functionalized side chains whose groupings might interact with appropriate groupings of HGPRT to form covalent bonds or strong hydrophobic bonds. 3-( ...