- Design, synthesis, and structure-activity relationship of a novel series of 2-aryl 5-(4-oxo-3-phenethyl-2-thioxothiazolidinylidenemethyl)furans as HIV-1 entry inhibitors
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We previously identified two small molecules targeting the HIV-1 gp41, N-(4-carboxy-3-hydroxy)phenyl-2,5-dimethylpyrrole 12 (NB-2) and N-(3-carboxy-4-chloro)phenylpyrrole 13 (NB-64), that inhibit HIV-1 infection at low micromolar levels. On the basis of m
- Katritzky, Alan R.,Tala, Srinivasa R.,Lu, Hong,Vakulenko, Anatoliy V.,Chen, Qi-Yin,Sivapackiam, Jothilingam,Pandya, Keyur,Jiang, Shibo,Debnath, Asim K.
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supporting information; experimental part
p. 7631 - 7639
(2010/09/03)
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- THE USE OF SELECTIVE P2X7 RECEPTOR ANTAGONISTS
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The present invention relates to the use of selective P2X7 receptor antagonists of formula (I), or a pharmaceutically acceptable salt or prodrug thereof wherein D, R1 and R2 are as defined in claim 1, for the treatment of neuropathic pain, chronic inflammatory pain, inflammation, neurodegeneration and for promoting neuroregeneration.
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Page/Page column 59
(2008/06/13)
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- Ortho-metalation of unprotected 3-bromo and 3-chlorobenzoic acids with hindered lithium dialkylamides
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Upon treatment of 3-chloro/bromobenzoic acids with hindered lithium dialkylamides (LDA or LTMP) at -50 °C, lithium 3-chloro/bromo-2-lithiobenzoates are generated. These dianions can be trapped as such to afford after electrophilic quenching a variety of s
- Gohier, Frederic,Mortier, Jacques
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p. 2030 - 2033
(2007/10/03)
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- The acidifying effects of chlorine and bromine: Little difference
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Lithium diisopropylamide deprotonates ortho- and para-bromochlorobenzene randomly at the two halogen adjacent positions. Obviously for steric reasons, the bulkier base lithium 2,2,6,6-tetramethylpiperidide favors the attack in the vicinity of the chlorine rather than the bromine atom to the extent of 2:1. At -75°C, both 2-bromo-3-chlorophenyllithium and 3-bromo-2-chlorophenyllithium isomerize to give 2-bromo-6-chlorophenyllithium. The latter species can be directly generated from 1-bromo-3-chlorobenzene.
- Mongin, Florence,Schlosser, Manfred
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p. 1559 - 1562
(2007/10/03)
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- Lithiations directed by carboxylic acid, fluorine and chlorine: The regioselective synthesis of polysubstituted benzoic acids and acetophenones
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Lithiation/electrophilic quenching of ortho-lithiated benzoates allows the totally regiocontrolled synthesis of a wide range of 2,3-, 2,3,4-, and 2,3,4,5-polysubstituted benzoic acids and related acetophenones. Elsevier,.
- Moyroud, Joel,Guesnet, Jean-Luc,Bennetau, Bernard,Mortier, Jacques
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p. 133 - 141
(2007/10/03)
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- Regiospecific Synthesis of Mixed 2,3-Dihalobenzoic Acids and Related Acetophenones via Ortho-Metalation Reactions
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Concise general routes to mixed 2,3-dihalobenzoic acids and related acetophenones-based on directed ortho-metalation and ipso-desilylation reactions are described.
- Moyroud, Joel,Guesnet, Jean-Luc,Bennetau, Bernard,Mortier, Jacques
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p. 881 - 884
(2007/10/02)
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