Synthesis and antitrypanosomal activities of a series of 7-deaza-5'-noraristeromycin derivatives with variations in the cyclopentyl ring substituents

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Citation of Original Publication

Seley, K L, S W Schneller, D Rattendi, S Lane, and C J Bacchi. “Synthesis and Antitrypanosomal Activities of a Series of 7-Deaza-5’-Noraristeromycin Derivatives with Variations in the Cyclopentyl Ring Substituents.” Antimicrobial Agents and Chemotherapy 41, no. 8 (August 1997): 1658–61. https://doi.org/10.1128/aac.41.8.1658.

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Abstract

Previous work in our laboratories has suggested that (+)-5'-nor-7-deazaaristeromycin (compound 1) may represent a prototype structure for a series of compounds with significant antitrypanosomal activities. To test this possibility, a series of derivatives of compound 1 with changes in the cyclopentyl substituents (compounds 3 to 10) have been studied. Although some growth activity was obtained with the L-like compound 5, related compounds 3 and 7 had little or no activity below 100 microM. D-like compounds 4 and 6 showed some activity at or below 100 microM, but the most interesting finding was that both the D- and L-like compounds having a methyl substituent on the 4' position were most active.