50488-44-3Relevant academic research and scientific papers
CARBOXY SUBSTITUTED (HETERO) AROMATIC RING DERIVATIVES AND PREPARATION METHOD AND USES THEREOF
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, (2017/03/21)
Carboxy-substituted (hetero)aryl derivatives, pharmaceutical compositions comprising these compounds, and methods of preparing such compounds and compositions are provided. The compounds or compositions are useful in inhibiting xanthine oxidase and urate anion transporter 1, and also can be used in the treatment or prevention of diseases associated with high blood uric acid level in mammals, especially humans.
A highly practical and convenient halogenation of fused heterocyclic N-oxides
Wang, Dong,Wang, Yuxi,Zhao, Junjie,Li, Linna,Miao, Longfei,Wang, Dong,Sun, Hua,Yu, Peng
, p. 5762 - 5768 (2016/08/30)
A novel, simple and practical method for the regioselective halogenation of fused heterocyclic N-oxides has been developed. It employs Vilsmeier reagent, generated in situ by POX3and DMF, as both the activating agent and the nucleophilic halide source. The method is amenable across a broad range of substrates, including quinolines, isoquinolines and the diazine N-oxides, possessing a variety of substitution patterns. Furthermore, all of the reagents associated are cheap and easy to obtain. The potential extension of this method to a one-pot oxidation/halogenation sequence that obviates the need for isolation of the N-oxide intermediates is also presented.
Design, synthesis and biological evaluation of 2-substituted quinolines as potential antileishmanial agents
Gopinath, Vadiraj S.,Pinjari, Jakir,Dere, Ravindra T.,Verma, Aditya,Vishwakarma, Preeti,Shivahare, Rahul,Moger, Manjunath,Kumar Goud, Palusa Sanath,Ramanathan, Vikram,Bose, Prosenjit,Rao,Gupta, Suman,Puri, Sunil K.,Launay, Delphine,Martin, Denis
, p. 527 - 536 (2013/10/22)
An analogous library of 2-substituted quinoline compounds was synthesized with the aim to identify a potential drug candidate to treat visceral leishmaniasis. These molecules were tested for their in vitro and in vivo biological activity against Leishmania donovani. Metabolic stability of these compounds was also improved through the introduction of halogen substituents. Compound (26g), found to be the most active; exhibited an IC50 value of 0.2 μM and >180 fold selectivity. The hydrochloride salt of (26g) showed 84.26 ± 4.44 percent inhibition at 50 mg/kg × 5 days (twice daily, oral route) dose in L. donovani/hamster model. The efficacy was well correlated with the PK data observed which indicating that the compound is well distributed.
A new 4-(2-methylquinolin-4-ylmethyl)phenyl P1′ group for the β-amino hydroxamic acid derived TACE inhibitors
Chen, Xiao-Tao,Ghavimi, Bahman,Corbett, Ronald L.,Xue, Chu-Biao,Liu, Rui-Qin,Covington, Maryanne B.,Qian, Mingxin,Vaddi, Krishna G.,Christ, David D.,Hartman, Karl D.,Ribadeneira, Maria D.,Trzaskos, James M.,Newton, Robert C.,Decicco, Carl P.,Duan, James J.-W.
, p. 1865 - 1870 (2007/10/03)
A new P1′ group for TACE inhibitors was identified by eliminating the oxygen atom in the linker of the original 4-(2-methylquinolin-4-ylmethoxy)phenyl P1′ group. Incorporation of this 4-(2-methylquinolin-4-ylmethyl)phenyl group onto different β-aminohydro
Hydantoins and related heterocycles as inhibitors of matrix metalloproteinases and/or TNF-alpha converting enzyme (TACE)
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, (2008/06/13)
The present application describes novel hydantoin derivatives of formula (I): or pharmaceutically acceptable salt or prodrug forms thereof, wherein A, B, R1, R2, R3, R4, R5, R6, R7, R11, and n are defined in the present specification, which are useful as inhibitors of matrix metalloproteinases (MMP), TNF-α converting enzyme (TACE), aggrecanase, or a combination thereof.
Spiro-cyclic beta-amino acid derivatives as inhibitors of matrix metalloproteases and TNF-alpha converting enzyme (TACE)
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, (2008/06/13)
The present application describes novel spiro-cyclic β-amino acid derivatives of formula I: or pharmaceutically acceptable salt forms thereof, wherein ring B is a 3-13 membered carbocycle or heterocycle, ring C forms a 3-11 membered spiro-carbocycle or spiro-heterocycleon ring B, and the other variables are defined in the present specification, which are useful as as matrix metalloproteinases (MMP), TNF-α converting enzyme (TACE), and/or aggrecanase inhibitors.
Barbituric acid derivatives as inhibitors of TNF-alpha converting enzyme (TACE) and/or matrix metalloproteinases
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Page/Page column 33, (2008/06/13)
The present application describes novel barbituric acid derivatives of formula I: or pharmaceutically acceptable salt or prodrug forms thereof, wherein A, B, L, R1, R2, R3, R4, R5, n, W, U, X, Y, Z, U
