344-39-8Relevant articles and documents
Activation and stabilization of aldimines by an ortho-trifluoromethyl substituent in direct vinylogous Mannich-type reactions
Lautens, Mark,Tayama, Eiji,Nguyen, Duy
, p. 5131 - 5133 (2004)
Lewis acid catalyzed direct vinylogous Mannich-type reaction with a weak nucleophile dienol, generated in situ by ring-opening and rearrangement of vinyloxiranes, could be demonstrated in excellent yields under mild conditions using benzylidene(4-methoxy-2-trifluoromethyl)aniline (MTMA) as an electrophile. The o-trifluoromethyl substituent can stabilize imines by a steric effect and activate by an electron-withdrawing effect. It proved to be an easily deprotectable protecting group for direct Mannich-type reactions.
TRICYCLIC COMPOUNDS AS mPGES-1 INHIBITORS
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Page/Page column 46, (2012/09/10)
The present invention relates to tricyclic compounds of formula (I) or pharmaceutically acceptable salt thereof as mPGES-1 inhibitors. These compounds are inhibitors of the microsomal prostaglandin E synthase-1 (mPGES-1) enzyme and are therefore useful in the treatment of pain and/or inflammation from a variety of diseases or conditions, such as asthama, osteoarthritis, rheumatoid arthritis, acute or chronic pain and neurodegenerative diseases. (I)
Structure-Activity relationships for a series of quinoline-based compounds active against replicating and nonreplicating mycobacterium tuberculosis
Lilienkampf, Annamaria,Jialin, Mao,Baojie, Wan,Yuehong, Wang,Franzblau, Scott G.,Kozikowski, Alan P.
supporting information; experimental part, p. 2109 - 2118 (2009/12/31)
Tuberculosis (TB) remains as a global pandemic that is aggravated by a lack of health care, the spread of HIV, and the emergence of multidrug-resistant TB (MDR-TB) and extensively drug-resistant TB (XDRTB) strains. New anti-TB drugs are urgently required to shorten the long 6-12 month treatment regimen and to battle drug-resistant Mtb strains. We have identified several potent quinoline-based anti-TB compounds, bearing an isoxazole containing side-chain. The most potent compounds, 7g and 13, exhibited submicromolar activity against the replicating bacteria (R-TB), with minimum inhibitory concentrations (MICs) of 0.77 and 0.95 μM, respectively. In general, these compounds also had micromolar activity against the nonreplicating persistent bacteria (NRP-TB) and did not show toxicity on Vero cells up to 128 μM concentration. Compounds 7g and 13 were shown to retain their anti-TB activity against rifampin, isoniazid, and streptomycin resistant Mtb strains. The results suggest that quinoline-isoxazole-based anti-TB compounds are promising leads for new TB drug development.