- PIKFYVE KINASE INHIBITORS
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The present invention relates to compounds useful as inhibitors of phosphatidylinositol-3-phosphate 5-kinase (PIKfyve) as well as their use for treating diseases and disorders associated with PIKfyve.
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Page/Page column 320-321
(2021/08/20)
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- Design, synthesis and anti-HIV evaluation of 5-alkyl- 6-(benzo[d][1,3]dioxol-5-alkyl)-2-mercaptopyrimidin-4(3H)-ones as potent HIV-1 NNRTIs
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In order to discover and develop the new HIV-1 NNRTIs, a series of 5-alkyl-6-(benzo[d][1,3]dioxol-5-ylalkyl)-2-mercaptopyrimidin-4(3H)-ones was synthesized and screened for their in vitro cytotoxicity against HIV-1. Most of the compounds we synthetized sh
- Cui, Yi-Man,He, Yan-Ping,Huang, Si-Ming,Li, Sui-Yuan,Li, Xiao-Li,Li, Yi-Ming,Luo, Rong-Hua,Ni, Dong-Xuan,Tang, E.,Xiao, Wei-Lie,Yang, Liu-Meng,Zhang, Hong-Bin,Zhang, Rui-Han,Zhang, Xing-Jie,Zheng, Yong-Tang,Zheng, Yu-Gui
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- Bicyclic Pyridinylpyrazoles
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Bicyclic pyridinylpyrazoles of the formula (I) in which the symbols have the meanings given in the description and agrochemically active salts thereof and their use for controlling unwanted microorganisms in crop protection and the protection of materials
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Page/Page column 31
(2011/10/19)
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- A novel and efficient approach to pyrazolo[1,5-a]pyridine derivatives via one-pot tandem reaction
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An unusual intramolecular condensation of a, α,β-unsaturated esters with aldehydes was discovered and the pyrazolo[1,5-α]pyridine derivatives were conveniently synthesized by this novel tandem reaction under very mild conditions. The reaction mechanism was also proposed.
- Ge, Yan-Qing,Jia, Jiong,Li, Yan,Yin, Ling,Wang, Jianwu
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experimental part
p. 197 - 206
(2009/05/07)
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- New flexible synthesis of pyrazoles with different, functionalized substituents at C3 and C5
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Syntheses of pyrazoles featuring a functionalized side chain attached to carbon 3 and varying alkyl and aryl substituents attached to carbon 5 are presented. Installation of R = methyl, isopropyl, tert-butyl, adamantyl, or phenyl groups at C5 is reported
- Grotjahn, Douglas B.,Van, Sang,Combs, David,Lev, Daniel A.,Schneider, Christian,Rideout, Marc,Meyer, Christoph,Hernandez, Genaro,Mejorado, Lupe
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p. 9200 - 9209
(2007/10/03)
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- Inhibitors of acyl-coA:cholesterol O-acyltransferase. 2. Identification and structure-activity relationships of a novel series of N-alkyl-N- (heteroaryl-substituted benzyl)-N'-arylureas
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A series of N-alkyl-N-(heteroaryl-substituted benzyl)-N'-arylurea and related derivatives represented by 2 and 3 have been prepared and evaluated for their ability to inhibit acyl-CoA:cholesterol O-acyltransferase in vitro and to lower plasma cholesterol levels in cholesterol-fed rats in vivo. Among these novel compounds, the type 3 series was superior. A pyrazol-3-yl group on the N-benzyl group of this trisubstituted urea (i.e. 3, Ar1 = pyrazol-3- yl) was identified as a heteroaromatic ring providing a good profile of biological activity. As a result of optimization of the combination with the N-alkyl group (R) and N-aryl group (At3), compound 3aq (FR186054) was identified as a new, orally efficacious ACAT inhibitor, which exhibited potent in vitro ACAT inhibitory activity (rabbit intestinal microsomes IC50 = 99 nM) and excellent hypocholesterolemic effects in cholesterol-fed rats, irrespective of administration mode (ED50 = 0.046 mg/kg dosed via the diet, ED50 = 0.44 mg/kg administered by gavage in PEG400 vehicle). Moreover, a toxicological study revealed compound 3aq to be nontoxic to the adrenal glands of dogs when tested at a single dose of 10 mg/kg po.
- Tanaka, Akira,Terasawa, Takeshi,Hagihara, Hiroyuki,Sakuma, Yuri,Ishibe, Noriko,Sawada, Masae,Takasugi, Hisashi,Tanaka, Hirokazu
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p. 2390 - 2410
(2007/10/03)
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