- Synthesis and evaluation of unsymmetrical heterocyclic thioureas as potent β-glucuronidase inhibitors
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Thiourea analogs 1-20 were synthesized and evaluated for their in vitro β-glucuronidase inhibitory potential. The compounds 9 (0.86 ± 0.01 μM), 6 (1.24 ± 0.01 μM), 16 (1.64 ± 0.02 μM) and 15 (2.12 ± 0.02 μM) showed potent activity. Other analogs 1-5, 7, 8
- Taha, Muhammad,Ismail, Nor Hadiani,Jamil, Waqas,Khan, Khalid Mohammed,Salar, Uzma,Kashif, Syed Muhammad,Rahim, Fazal,Latif, Yawar
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p. 3166 - 3173
(2015/08/03)
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- NEW FLUOROUS TAGGING AND SCAVENGING REACTANTS AND METHODS OF SYNTHESIS AND USE THEREOF
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The present invention includes methods and compositions for increasing the fluorous nature of an organic compound by reacting it with at least one fluorous compound to produce a fluorous tagged organic compound. The increased fluorous nature of the fluorous tagged organic compound can then be utilized to separate the fluorous organic compound from untagged reagents, reactants, catalysts and/or products derived therefrom. The resultant fluorous tagged organic compound can be subjected to subsequent chemical transformations, wherein the fluorous nature of the tagged compound is utilized to increase the ease of separation of the fluorous tagged organic compound from untagged reagents, reactants, catalysts and/or products derived therefrom, after each chemical transformation. The chemical transformations result in a second fluorous tagged organic compound wherein the fluorous nature of the second fluorous tagged organic compound can then be reduced by removing the fluorous group therefrom, thereby producing a second organic compound that may be employed as a pharmaceutical compound or intermediate, or a combinatorial library component.
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Page 58, 59, 61, 62
(2008/06/13)
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- Fluorous electrophilic scavengers for solution-phase parallel synthesis
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A fluorous isatoic anhydride and isocyanate are synthesized and used as scavengers for amines in solution-phase parallel synthesis of urea, thiourea, and β-hydroxyamine analogs. The resulting fluorous derivatives are readily separated from the reaction mi
- Zhang, Wei,Chen, Christine Hiu-Tung,Nagashima, Tadamichi
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p. 2065 - 2068
(2007/10/03)
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- Synthesis of N-substituted-N-acylthioureas of 4-substituted piperazines endowed with local anaesthetic, antihyperlipidemic, antiproliferative activities and antiarrythmic, analgesic, antiaggregating actions
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Three series of N-acyl and N-cyclohexyl- or N-methyl or N-phenyl-thioureas of 4-substituted (methyl, phenyl, 2-pyridyl)piperazines (4-12) were synthesised according to a highly convergent one-pot procedure and tested in vivo (local anaesthetic, anti-hyper
- Ranise, Angelo,Spallarossa, Andrea,Bruno, Olga,Schenone, Silvia,Fossa, Paola,Menozzi, Giulia,Bondavalli, Francesco,Mosti, Luisa,Capuano, Annalisa,Mazzeo, Filomena,Falcone, Giuseppe,Filippelli, Walter
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p. 765 - 780
(2007/10/03)
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