- Design, synthesis and in vitro activity of phidianidine B derivatives as novel PTP1B inhibitors with specific selectivity
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A series of phidianidine B derivatives were synthesized by introducing various heterocyclic rings. Their inhibitory effects on PTP1B and other PTPs (TCPTP, SHP1, SHP2 and LAR) were evaluated. A majority of them displayed significant inhibitory potency and specific selectivity over PTP1B. The SAR and molecular docking analysis were also described.
- Zhang, Li,Jiang, Cheng-Shi,Gao, Li-Xin,Gong, Jing-Xu,Wang, Zhong-Hua,Li, Jing-Ya,Li, Jia,Li, Xu-Wen,Guo, Yue-Wei
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supporting information
p. 778 - 781
(2016/05/24)
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- Design of α7 nicotinic acetylcholine receptor ligands in quinuclidine, tropane and quinazoline series. Chemistry, molecular modeling, radiochemistry, in vitro and in rats evaluations of a [18F] quinuclidine derivative
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In this report, we describe the synthesis of a novel library of α7 nAChR ligands based on the modulation of the quinuclidine, quinazoline and tropane moieties. Spirane derivatives were newly synthesized under stereo specific 1,3 dipolar cylcoadditions. On
- Pin, Frédéric,Vercouillie, Johnny,Ouach, Aziz,Mavel, Sylvie,Gulhan, Zuhal,Chicheri, Gabrielle,Jarry, Christian,Massip, Stephane,Deloye, Jean-Bernard,Guilloteau, Denis,Suzenet, Franck,Chalon, Sylvie,Routier, Sylvain
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p. 214 - 224
(2014/06/24)
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- A practical and cost-efficient, one-pot conversion of aldehydes into nitriles mediated by 'activated DMSO'
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Participation of activated DMSO in the one-pot transformation of aldehydes to nitriles has been described by reacting aldehydes with NHHHCl in DMSO in the absence of any added base or catalyst. The method is applicable to access a wide range of aromatic, heterocyclic, and aliphatic nitriles, in which only water is a byproduct. A straightforward and practical procedure is demonstrated on a multigram scale. Georg Thieme Verlag Stuttgart - New York.
- Augustine, John Kallikat,Bombrun, Agnes,Atta, Rajendra Nath
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experimental part
p. 2223 - 2227
(2011/10/31)
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- NOVEL ANTIMALARIA AGENT CONTAINING HETEROCYCLIC COMPOUND
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Disclosed is an antimalarial agent containing a compound represented by the formula: [wherein A1 represents a 3-pyridyl group that may have a substituent, a 6-quinolyl group that may have a substituent, or the like; X1 represents a group represented by the formula -C(=O)-NH- or the like; E represents a furyl group, a thienyl group or a phenyl group; with the proviso that A1 may have one to three substituents, and E has one of two substituents] or a salt thereof or hydrates thereof.
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Page/Page column 51
(2008/06/13)
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- OXAZOLIDINONE DERIVATIVES AS ANTIMICROBIALS
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The present invention relates to certain substituted phenyl oxazolidinones of formula (I) and to processes for the synthesis of the same. This invention also relates to pharmaceutical compositions containing such compounds as antimicrobials. The compounds are useful antimicrobial agents, effective against a number of human and veterinary pathogens, including gram-positive aerobic bacteria such as multiple-resistant staphylococci, streptococci and enterococci as well as anaerobic organisms such as Bacterioides spp. and Clostridia spp. species, and acid-fast organisms such as Mycobacterium tuberculosis, Mycobacterium avium and Mycobacterium spp.
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Page/Page column 29
(2010/02/13)
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- THIENYL COMPOUNDS
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Compounds of formula I : and pharmaceutically-acceptable salts thereof, wherein Ar and R are as defined in the specification, compositions containing such compounds and the use of such compounds and compositions for use in therapy.
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Page/Page column 17
(2008/06/13)
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