1421314-64-8Relevant academic research and scientific papers
The synthesis of 5-functional 3-hydroxypyridin-4-ones and their impact on the chelating properties of the ligands
Chen, Yu-Lin,Chen, Jing,Ma, Yongmin,Hider, Robert C.
, p. 515 - 517 (2015)
The presence of the 5-functional group on 3-hydroxypyridin-4-ones (HPOs) can significantly change their chelating properties because the 5-position is adjacent to one of the chelating moieties. A 5-methoxy-substituted HPO has been successfully synthesized using a 5-bromo analogue with NaOMe in the presence of a copper(I) catalyst. The atomic charges and stability constants of the HPOs with either electron-donating or election-withdrawing groups on the 5-position were compared. The result showed that the 5-substituted HPOs possess lower stability constants, compared to those of the 5-unsubstituted analogue (deferiprone).
Carbamoyl pyridone HIV-1 integrase inhibitors. 2. Bi- and tricyclic derivatives result in superior antiviral and pharmacokinetic profiles
Kawasuji, Takashi,Johns, Brian A.,Yoshida, Hiroshi,Weatherhead, Jason G.,Akiyama, Toshiyuki,Taishi, Teruhiko,Taoda, Yoshiyuki,Mikamiyama-Iwata, Minako,Murai, Hitoshi,Kiyama, Ryuichi,Fuji, Masahiro,Tanimoto, Norihiko,Yoshinaga, Tomokazu,Seki, Takahiro,Kobayashi, Masanori,Sato, Akihiko,Garvey, Edward P.,Fujiwara, Tamio
, p. 1124 - 1135 (2013/03/28)
This work is a continuation of our initial discovery of a potent monocyclic carbamoyl pyridone human immunodeficiency virus type-1 (HIV-1) integrase inhibitor that displayed favorable antiviral and pharmacokinetic properties. We report herein a series of
TRICYCLIC COMPOUNDS AS mPGES-1 INHIBITORS
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, (2013/11/05)
The present disclosure is directed to compounds of formula (I), and pharmaceutically acceptable salts thereof, as m PGES-1 inhibitors. These compounds are inhibitors of the microsomal prostaglandin E synthase-1 (m PGES-1) enzyme and are therefore useful in the treatment of pain and/or inflammation from a variety of diseases or conditions, such as asthma, osteoarthritis, rheumatoid arthritis, acute or chronic pain and neurodegenerative diseases.
POLYCYCLIC CARBAMOYLPYRIDONE DERIVATIVE HAVING HIV INTEGRASE INHIBITORY ACTIVITY
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, (2010/11/24)
The present invention is to provide a novel compound (I), having the anti-virus activity, particularly the HIV integrase inhibitory activity, and a drug containing the same, particularly an anti-HIV drug, as well as a process and an intermediate thereof. Compound (I) wherein Z1 is NR4; R1 is hydrogen or lower alkyl; X is a single bond, a hetero atom group selected from O, S, SO, SO2 and NH, or lower alkylene or lower alkenylene in which the hetero atom group may intervene; R2 is optionally substituted aryl; R3 is hydrogen, a halogen, hydroxy, optionally substituted lower alkyl etc; and R4 and Z2 part taken together forms a ring, to form a polycyclic compound, including e.g., a tricyclic or tetracyclic compound.
