- Discovery of novel and potent leukotriene B4 receptor antagonists. Part 1
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The inhibition of LTB4 binding to and activation of G-protein-coupled receptors BLT1 and BLT2 is the premise of a treatment for several inflammatory diseases. In a lead optimization effort starting with the leukotriene B4 (LTB4
- Goodnow, Robert A.,Hicks, Alexandra,Sidduri, Achyutharao,Kowalczyk, Agnieszka,Dominique, Romyr,Qiao, Qi,Lou, Jian Ping,Gillespie, Paul,Fotouhi, Nader,Tilley, Jefferson,Cohen, Noal,Choudhry, Satish,Cavallo, Gary,Tannu, Shahid A.,Ventre, Jessica D.,Lavelle, Danielle,Tare, Nadine S.,Oh, Hyesun,Lamb, Martin,Kurylko, Grazyna,Hamid, Rachid,Wright, Matthew B.,Pamidimukkala, Anjula,Egan, Thomas,Gubler, Ueli,Hoffman, Ann F.,Wei, Xin,Li, Ying L.,O'Neil, John,Marcano, Ruben,Pozzani, Karen,Molinaro, Tina,Santiago, Jennifer,Singer, Laura,Hargaden, Maureen,Moore, David,Catala, A. Robert,Chao, Lisa C. F.,Hermann, Gesine,Venkat, Radhika,Mancebo, Helena,Renzetti, Louis M.
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experimental part
p. 3502 - 3516
(2010/09/08)
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- Leukotriene B4 Inhibitors
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Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of diseases such as, for example, COPD
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Page/Page column 29
(2009/04/24)
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- Coupling compounds and hair dyeing compositions containg them
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The present invention refers to Compound of the formula (I) wherein X is oxygen or sulphur; R1 is (C1-C4)-alkyl, (C1-C4)-alkyl which is substituted by hydroxy, (C1-C4)-alkoxy, hy
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Page/Page column 9
(2008/06/13)
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- Allosteric regulation of the conformational dynamics of a cavitand receptor
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Inspired by allostery in nature, we synthesized cavitand 1 and investigated regulation of its conformational dynamics. Quantitative 1H NMR studies have revealed that the rate of the conformational isomerization of 1 can be modulated using the e
- Yan, Zhiqing,Chang, Yuning,Mayo, Dennis,Maslak, Veselin,Xia, Shijing,Badjic, Jovica D.
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p. 3697 - 3700
(2007/10/03)
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- Substituted benzamide inhibitors of rhinovirus 3C protease
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Nonpeptide benzamide-containing inhibitors of human rhinovirus (HRV) 3C protease are described.
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Page column 12-13
(2010/01/31)
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- Substituted benzamide inhibitors of human rhinovirus 3C protease: Structure-based design, synthesis, and biological evaluation
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A series of nonpeptide benzamide-containing inhibitors of human rhinovirus (HRV) 3C protease was identified using structure-based design. The design, synthesis, and biological evaluation of these inhibitors are reported. A Michael acceptor was combined with a benzamide core mimicking the P1 recognition element of the natural 3CP substrate, α,β-Unsaturated cinnamate esters irreversibly inhibited the 3CP and displayed antiviral activity (EC50 0.60/μM, HRV-16 infected H1-HeLa cells). On the basis of cocrystal structure information, a library of substituted benzamide derivatives was prepared using parallel synthesis on solid support. A 1.9 A? cocrystal structure of a benzamide inhibitor in complex with the 3CP revealed a binding mode similar to that initially modeled wherein covalent attachment of the nucleophilic cysteine residue is observed. Unsaturated ketones displayed potent reversible inhibition but were inactive in the cellular antiviral assay and were found to react with nucleophilic thiols such as DTT.
- Reich, Siegfried H.,Johnson, Theodore,Wallace, Michael B.,Kephart, Susan E.,Fuhrman, Shella A.,Worland, Stephen T.,Matthews, David A.,Hendrickson, Thomas F.,Chan, Fora,Meador III, James,Ferre, Rose Ann,Brown, Edward L.,DeLisle, Dorothy M.,Patick, Amy K.,Binford, Susan L.,Ford, Clifford E.
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p. 1670 - 1683
(2007/10/03)
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- Synthesis of Unlabelled and Carboxyl-Labelled 3-Amino-5-hydroxybenzoic Acid
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Efficient syntheses are reported of the natural amino acid 3-amino-5-hydroxybenzoic acid in unlabelled and carboxyl-labelled forms from 3,5-dinitrobenzoic acid and 3,5-dinitroanisole, respectively.
- Herlt, Anthony J.,Kibby, Jeffrey J.,Rickards, Rodney W.
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p. 1319 - 1324
(2007/10/02)
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