- Visible-Light-Mediated Oxidative Amidation of Aldehydes by Using Magnetic CdS Quantum Dots as a Photocatalyst
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A magnetic CdS quantum dot (Fe3O4/polydopamine (PDA)/CdS) was synthesized through a facile and convenient method from inexpensive starting materials. Characterization of the prepared catalyst was performed by means of FTIR spectrosco
- Xu, Ling,Zhang, Shuai-Zheng,Li, Wei,Zhang, Zhan-Hui
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p. 5483 - 5491
(2021/03/01)
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- Design and synthesis of 6-fluoro-2-naphthyl derivatives as novel CCR3 antagonists with reduced CYP2D6 inhibition
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In our previous study on discovering novel types of CCR3 antagonists, we found a fluoronaphthalene derivative (1) that exhibited potent CCR3 inhibitory activity with an IC50 value of 20 nM. However, compound 1 also inhibited human cytochrome P450 2D6 (CYP2D6) with an IC50 value of 400 nM. In order to reduce its CYP2D6 inhibitory activity, we performed further systematic structural modifications on 1. In particular, we focused on reducing the number of lipophilic moieties in the biphenyl part of 1, using C log D7.4 values as the reference index of lipophilicity. This research led to the identification of N-{(3-exo)-8-[(6-fluoro-2-naphthyl)methyl]-8-azabicyclo[3.2.1]oct-3-yl}-3-(piperidin-1-ylcarbonyl)isonicotinamide 1-oxide (30) which showed comparable CCR3 inhibitory activity (IC50 = 23 nM) with much reduced CYP2D6 inhibitory activity (IC50 = 29,000 nM) compared with 1.
- Sato, Ippei,Morihira, Koichiro,Inami, Hiroshi,Kubota, Hirokazu,Morokata, Tatsuaki,Suzuki, Keiko,Iura, Yosuke,Nitta, Aiko,Imaoka, Takayuki,Takahashi, Toshiya,Takeuchi, Makoto,Ohta, Mitsuaki,Tsukamoto, Shin-ichi
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p. 8607 - 8618
(2008/12/23)
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- (2,6-DIOXO-3-PIPERINYL)AMIDOBENZOIC IMMUNOMODULATORY AND ANTI-CANCER DERIVATIVES
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The present invention is concerned with certain benzoic acid derivatives and their use in the treatment of neoplastic disorders and as immune modulators. In particular the present invention is concerned with carboxybenzoyl glutamic acid analogues and their uses.
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Page/Page column 15
(2010/11/29)
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- DIASTEREO- AND ENANTIOSELECTIVE SYNTHESIS OF 1,2-DIOLS BY VANADIUM(II) PROMOTED PINACOL CROSS COUPLING
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The V(II) promoted pinacol cross coupling of a chiral aromatic aldehyde with achiral aliphatic aldehydes occurs to afford syn diols in up to 91:9 diastereoisomeric ratio and up to 84percent enantiomeric excess.The pinacol coupling of (S)-lactaldehyde and (R)-glyceraldehyde derivatives has also been studied and matching and mis-matching pairs have been identified.The stereochemistry of the products was established by correlation.The sense and degree of stereoselection is discussed.
- Annunziata, Rita,Cinquini, Mauro,Cozzi, Franco,Giaroni, Paola,Benaglia, Maurizio
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p. 5737 - 5758
(2007/10/02)
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