- PYRIDAZINE DERIVATIVES AS RORC MODULATORS
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Compounds of formula (I): (I) or pharmaceutical salts thereof, wherein m, n,, p, q A, B, Ri, R2, R3, R4, R5, R6and R7are as defined herein. Also disclosed are methods of making the compounds and using the compounds as RORs modulators for treatment of inflammatory diseases such as arthritis.
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Page/Page column 167; 168
(2018/05/24)
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- Chemical differentiation of three DMSP lyases from the marine: Roseobacter group
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Dimethylsulfoniopropionate (DMSP) catabolism of marine bacteria plays an important role in marine and global ecology. The genome of Ruegeria pomeroyi DSS-3, a model organism from the Roseobacter group, harbours no less than three genes for different DMSP lyases (DddW, DddP and DddQ) that catalyse the degradation of DMSP to dimethyl sulfide (DMS) and acrylate. Despite their apparent similar function these enzymes show no significant overall sequence identity. In this work DddQ and DddW from R. pomeroyi and the DddP homolog from Phaeobacter inhibens DSM 17395 were functionally characterised and their substrate scope was tested using several synthetic DMSP analogues. Comparative kinetic assays revealed differences in the conversion of DMSP and its analogues in terms of selectivity and overall velocity, giving additional insights into the molecular mechanisms of DMSP lyases and into their putatively different biological functions.
- Burkhardt, Immo,Lauterbach, Lukas,Brock, Nelson L.,Dickschat, Jeroen S.
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supporting information
p. 4432 - 4439
(2017/07/10)
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- Synthesis and antiallergic activity of dimethyl-2- (phenylcarbamoyl)ethylsulfonium p-toluenesulfonate derivatives
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The derivatives of dimethyl-2-(phenylcarbamoyl)ethylsulfonium p- toluenesulfonates were synthesized and evaluated for antiallergic activity. The 2,3-dihydroxyethoxy group was introduced to the phenyl ring from the standpoint of lipophilicity and electronic effects of substituent. The IgE- induced rat passive cutaneous anaphylaxis (PCA) was inhibited by oral administration of several substituted 2-[(4- propoxyphenyl)carbamoyl]ethyldimethylsulfonium p-toluenesulfonate derivatives. Among them (±)-2-[N-[4-(3-ethoxy-2- hydroxypropoxy)phenyl]carbamoyl]ethyldimethylsulfonium p-toluenesulfonate (1a, IPD-1151T) was found to possess considerable activity in the PCA test, and it was launched as Suplatast tosilate in Japan.
- Tada, Yukio,Yamawaki, Ichiro,Ueda, Shuichi,Matsumoto, Hiroshi,Matsuura, Naosuke,Yasumoto, Mitsugi,Koda, Akihide,Hori, Mikio
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p. 3330 - 3336
(2007/10/03)
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