Synthesis and antiviral evaluation of N-carboxamidine-substituted analogs of 1-. beta.-D-ribofuranosyl-1, 2, 4-triazole-3-carboxamidine hydrochloride.

B Gabrielsen, MJ Phelan, L Barthel-Rosa…

Index: Gabrielsen, Bjarne; Phelan, Michael J.; Barthel-Rosa, Luis; See, Cathy; Huggins, John W.; et al. Journal of Medicinal Chemistry, 1992 , vol. 35, # 17 p. 3231 - 3238

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Citation Number: 38

Abstract

Ten, hitherto unreported, analcguea of l-~-~ nbo~ anosyl-l, 2, 4-triazole3-carbo~ dine hydrochloride (2a, ribamidine) and methyl carboximidate 5 have been synthesized. These include the N-cyano (2b), N-alkyl (2c-e), N-amino acid (2f-h), N,"-disubstituted (6, 7a, b), and the N-methylated carboxamide (If) analogues of ribavirin. In addition, a new facile synthesis of carboxamidine 2a was also developed. All compounds were evaluated for biological ...

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