moiety of 1.8) We have also reported novel methodology for the synthesis of the amide analog of 19) and non-ornithinecontaining macrocyclic lactones.10) Herein, we describe the synthesis and evaluation of a newseries of amidine analogs of the ornithine moiety of FR901469, and the discovery of pyrazolium derivative 8 with reduced hemolytic activity and comparable efficacy to 1 in a murine model ...

A practical and highly stereoselective approach to access 2,6-disubstituted piperidines using an amidine auxiliary is reported. Following the diastereoselective addition of Grignard reagents at the 2-position of an activated pyridinium salt, the amidine group directs a regioselective metalation at the 6-position, enabling further functionalization. A subsequent electrophilic quench or a Negishi...

The total synthesis of two key analogues of vancomycin containing single-atom exchanges in the binding pocket (residue 4 amidine and thioamide) are disclosed as well as their peripherally modified (4-chlorobiphenyl)methyl (CBP) derivatives. Their assessment indicates that combined pocket amidine and CBP peripherally modified analogues exhibit a remarkable spectrum of antimicrobial activity (VSS...

Citation: Fetz AE, Neeli I, Buddington KK, Read RW, Smeltzer MP, Radic MZ and Bowlin GL (2018) Localized Delivery of Cl-Amidine From Electrospun Polydioxanone Templates to Regulate Acute Neutrophil NETosis: A Preliminary Evaluation of the PAD4 Inhibitor for Tissue Engineering. Front. Pharmacol. 9:289. doi: 10.3389/fphar.2018.00289 Localized Delivery of Cl-Amidine From Electrospun Polydioxanone ...

An electrochemical investigation of novel electrolytes based on amidine salts for aluminium batteries.

The parallel solid phase synthesis of an 18-member library of 2-substituted pyrimidines is described using a chlorogermane-functionalised resin. The success of the key Pinner-type condensations between a resin-bound enaminone and an array of amidine hydrochlorides highlights the stability of arylgermane linkers (cf. arylsilanes) towards strongly basic/nucleophilic conditions.