Optimized 5-membered heterocycle-linked pterins for the inhibition of Ricin Toxin A.
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ABSTRACT:
SUBMITTER: Pruet JM
PROVIDER: S-EPMC3462456 | biostudies-literature | 2012 Jul
REPOSITORIES: biostudies-literature
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Optimized 5-membered heterocycle-linked pterins for the inhibition of Ricin Toxin A.
Pruet Jeff M JM Saito Ryota R Manzano Lawrence A LA Jasheway Karl R KR Wiget Paul A PA Kamat Ishan I Anslyn Eric V EV Robertus Jon D JD
ACS medicinal chemistry letters 20120529 7
The optimization of a series of pterin amides for use as Ricin Toxin A (RTA) inhibitors is reported. Based upon crystallographic data of a previous furan-linked pterin, various expanded furans were synthesized, linked to the pterin and tested for inhibition. Concurrently, hetero-analogs of furan were explored, leading to the discovery of more potent triazol-linked pterins. Additionally, we discuss a dramatic improvement in the synthesis of these pterin amides via a dual role by diazabicycloundec ...[more]
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