Electron deficient heteroaromatic ammonioamidates. Part 25. N-(Quinazolin-3-io)amidates. Part 12. The synthesis of n-(6,7-dimethoxy-2-methylquinazolin-3-io)ethoxythioformamidate and of 2-(3,4-dimethoxyphenyl)-8,9-dimethoxy-5-methyl-10bH-[1,3,4]-thiadiazolo [3,2-c] quinazoline, the ring isomer of N-(6,7-dimethoxy-2-methylquinazolin-3-io)-3,4-dimethoxy(thiobenzamidate)

Lempert‐Sreter, M.; Lempert, K.; Møller, Jørgen

doi:10.1039/p19830002011

Cited by 10 publications

(1 citation statement)

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“…It was ascertained via the analysis of the published data [18, 19] that ring–chain tautomerism is typical of thiohydrazones. Cyclic tautomers (thiadiazolines II ) are easily oxidized by air oxygen, yielding inactive and toxic thiadiazoles III ( Fig.…”

Section: Resultsmentioning

confidence: 99%

Development of Chlamydial Type III Secretion System Inhibitors for Suppression of Acute and Chronic Forms of Chlamydial Infection

et al. 2012

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The Type III secretion system (T3SS) is currently considered to be one of the main pathogenicity factors in Gram-negative bacteria, which exhibit different types of parasitizing activity. The presence of this structure is essential for the development of an acute infection; the chronicity of the infection is fundamentally dependent upon its functioning. In this regard, T3TS is one of the most promising targets for the development of broad-spectrum antimicrobial drugs that do not develop resistance and are efficacious for the acute and chronic forms of infection. The mechanism of action in drug development is based on the specific inhibition of T3SS, which should interrupt the infectious process, thereby enabling the immune system to eliminate the pathogen. As a result of pilot screening using specific cellular and bacterial tests, followed by chemical optimization and detailed characterization of the biological activity, a new class of chlamydial T3SS inhibitors was obtained. The selected compounds have obvious advantages over the currently available inhibitors of T3SS pathogens thanks to the high inhibitory activity of these compounds with minimal damaging effects on eukaryotic cells. Preclinical trials of the selected inhibitors are currently under way.

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Section: Resultsmentioning

confidence: 99%