Clark Norman Eid

Design, syntheses and potentiating activities against methicillin resistant Staphylococcus aureus of cyclic analogs of LY301621

Abstract Previous SAR studies of the diastereomers of LY301621 suggested the importance of a β-turn conformation for biological activity. In the present study, cyclic analogs were designed and synthesized that possess Type II and II β-turns. Their biological activity will be discussed.

Synthesis of new 3-thiosubstituted carbacephem antibiotics and their activity against penicillin resistant Streptococcus pneumoniae

The synthesis of a series of 3-thiosubstituted carbacephem derivatives is described. The compounds were assayed against penicillin susceptible, intermediate and resistant strains of Streptococcus pneumoniae. Several analogs displayed potent in vitro activity against these organisms.

Synthesis of a radioiodinated park nucleotide analog: a new tool for antibacterial screen development

The Park nucleotide is an important biological building block used in the construction of bacterial cell walls. Herein, we describe the synthesis of a radiolabeled Park nucleotide analog, p-iodophenoxyacyl-Ala-(d)-iso-Glu-Lys-(d)-Ala-(d)-Ala-OH-[123I], using electrophilic destannylation. Anti-Park nucleotide antibody binding assays using a scintillation proximity assay (SPA) system showed good recognition of the radiolabeled surrogate. This methodology could be used for establishing a screen to identify inhibitors of peptidoglycan biosynthesis.