857292-66-1Relevant articles and documents
INHIBITORS OF PLASMA KALLIKREIN AND USES THEREOF
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, (2019/09/30)
The present invention provides compounds and compositions thereof which are useful as inhibitors of plasma kallikrein and which exhibit desirable characteristics for the same.
Design, synthesis, and evaluation of new thiadiazole-based direct inhibitors of enoyl acyl carrier protein reductase (InhA) for the treatment of tuberculosis
?ink, Roman,Sosi?, Izidor,?ivec, Matej,Fernandez-Menendez, Raquel,Turk, Samo,Pajk, Stane,Alvarez-Gomez, Daniel,Lopez-Roman, Eva Maria,Gonzales-Cortez, Carolina,Rullas-Triconado, Joaquin,Angulo-Barturen, Inigo,Barros, David,Ballell-Pages, Lluís,Young, Robert J.,Encinas, Lourdes,Gobec, Stanislav
, p. 613 - 624 (2015/01/30)
Mycobacterial enoyl acyl carrier protein reductase (InhA) is a clinically validated target for the treatment of tuberculosis infections, a disease that still causes the death of at least a million people annually. A known class of potent, direct, and competitive InhA inhibitors based on a tetracyclic thiadiazole structure has been shown to have in vivo activity in murine models of tuberculosis infection. On the basis of this template, we have here explored the medicinal chemistry of truncated analogues that have only three aromatic rings. In particular, compounds 8b, 8d, 8f, 8l, and 8n show interesting features, including low nanomolar InhA IC50, submicromolar antimycobacterial potency, and improved physicochemical profiles in comparison with the tetracyclic analogues. From this series, 8d is identified as having the best balance of potency and properties, whereby the resolved 8d S-enatiomer shows encouraging in vivo efficacy.
Pyridines
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Page/Page column 29, (2008/06/13)
Compounds of formula as well as pharmaceutically acceptable salts and esters thereof, wherein R1 to R6 have the significance given in claim 1 can be used in the form of pharmaceutical compositions.