✦ LIBER ✦

Solution phase combinatorial chemistry. Discovery of 13- and 15-membered polyazapyridinocyclophane libraries with antibacterial activity

✍ Scribed by Haoyun An; Tingmin Wang; Venkatraman Mohan; Richard H. Griffey; P.Dan Cook

Book ID: 104208492
Publisher: Elsevier Science
Year: 1998
Tongue: French
Weight: 921 KB
Volume: 54
Category: Article
ISSN: 0040-4020
DOI: 10.1016/s0040-4020(98)00131-8

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✦ Synopsis

A solution phase simultaneous addition of functionalities (SPSAF) combinatorial a~oa~ was utilized to synthesize 40 polyazacyclophane lilraries (total complexity of 4275). Eighteen different functionality sets, utilizing 42 functionalities, were designed to disrupt RNA-pmtein interactions. Guanidine functionality sets with a greater potential to form positive charges iwovided the most active libraries. Differences in antibacterial activity m'e clearly related to different ring sizes with the more rigid 13-membered scaffold afftrding more active libraries compared with libraries from the 15-membeted scaffold. Molecular modeling estabfished a significant difference in the shapes of 13-and 15-membered pytidinophanes. Several fibraries exhibited potent antibacterial activity.

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