75369-41-4Relevant articles and documents
Design, synthesis and biological activity of multifunctional α,β-unsaturated carbonyl scaffolds for Alzheimer's disease
Bag, Seema,Ghosh, Sanjukta,Tulsan, Rekha,Sood, Abha,Zhou, Weihong,Schifone, Christine,Foster, Michelle,Levine III, Harry,T?r?k, Béla,T?r?k, Marianna
, p. 2614 - 2618 (2013)
A series of compounds containing an α,β-unsaturated carbonyl moiety, such as chalcones and coumarins were designed, synthesized and tested in a variety of assays to assess their potential as anti-Alzheimer's disease (AD) agents. The investigations include
CHEMICAL COMPOUNDS
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Page/Page column 51; 52, (2018/10/19)
The present disclosure relates to compounds of Formula (I): and to their pharmaceutically acceptable salts, pharmaceutical compositions, methods of use, and methods for their preparation. The compounds disclosed herein inhibit the maturation of cytokines of the IL-1 family by inhibiting inflammasomes and may be used in the treatment of disorders in which inflammasome activity is implicated, such as inter alia autoinflammatory and autoimmune diseases and cancers.
Discovery of a Quinoline-4-carboxamide Derivative with a Novel Mechanism of Action, Multistage Antimalarial Activity, and Potent in Vivo Efficacy
Baragana, Beatriz,Norcross, Neil R.,Wilson, Caroline,Porzelle, Achim,Hallyburton, Irene,Grimaldi, Raffaella,Osuna-Cabello, Maria,Norval, Suzanne,Riley, Jennifer,Stojanovski, Laste,Simeons, Frederick R. C.,Wyatt, Paul G.,Delves, Michael J.,Meister, Stephan,Duffy, Sandra,Avery, Vicky M.,Winzeler, Elizabeth A.,Sinden, Robert E.,Wittlin, Sergio,Frearson, Julie A.,Gray, David W.,Fairlamb, Alan H.,Waterson, David,Campbell, Simon F.,Willis, Paul,Read, Kevin D.,Gilbert, Ian H.
supporting information, p. 9672 - 9685 (2016/11/19)
The antiplasmodial activity, DMPK properties, and efficacy of a series of quinoline-4-carboxamides are described. This series was identified from a phenotypic screen against the blood stage of Plasmodium falciparum (3D7) and displayed moderate potency but with suboptimal physicochemical properties and poor microsomal stability. The screening hit (1, EC50 = 120 nM) was optimized to lead molecules with low nanomolar in vitro potency. Improvement of the pharmacokinetic profile led to several compounds showing excellent oral efficacy in the P. berghei malaria mouse model with ED90 values below 1 mg/kg when dosed orally for 4 days. The favorable potency, selectivity, DMPK properties, and efficacy coupled with a novel mechanism of action, inhibition of translation elongation factor 2 (PfEF2), led to progression of 2 (DDD107498) to preclinical development.
