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1.
Org Lett ; 24(43): 7924-7927, 2022 11 04.
Artigo em Inglês | MEDLINE | ID: mdl-36265082

RESUMO

A library of thiazoles and selenothiazoles were synthesized via Ir-catalyzed ylide insertion chemistry. This process is a functional group, particularly heterocycle-substituent tolerant. This was applied to the synthesis of fanetizole, an anti-inflammatory drug, and a thiazole-containing drug fragment that binds to the peptidyl-tRNA hydrolase (Pth) in Neisseria gonorrheae bacteria.


Assuntos
Irídio , Tiazóis , Bactérias , Catálise , Enxofre
2.
Microb Cell ; 9(4): 84-102, 2022 Apr 04.
Artigo em Inglês | MEDLINE | ID: mdl-35434122

RESUMO

Not all treasure is silver and gold; for pathogenic bacteria, iron is the most precious and the most pillaged of metallic elements. Iron is essential for the survival and growth of all life; however free iron is scarce for bacteria inside human hosts. As a mechanism of defence, humans have evolved ways to store iron so as to render it inaccessible for invading pathogens, such as keeping the metal bound to iron-carrying proteins. For bacteria to survive within humans, they must therefore evolve counters to this defence to compete with these proteins for iron binding, or directly steal iron from them. The most populous form of iron in humans is haem: a functionally significant coordination complex that is central to oxygen transport and predominantly bound by haemoglobin. Haemoglobin is therefore the largest source of iron in humans and, as a result, bacterial pathogens in critical need of iron have evolved complex and creative ways to acquire haem from haemoglobin. Bacteria of all cell wall types have the ability to bind haemoglobin at their cell surface, to accept the haem from it and transport this to the cytoplasm for downstream uses. This review describes the systems employed by various pathogenic bacteria to utilise haemoglobin as an iron source within human hosts and discusses their contribution to virulence.

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