- Novel pyrazole amide compound and preparation thereof, and application of novel pyrazole amide compound in prevention and treatment of plant pathogenic diseases and pest killing
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The invention relates to a novel pyrazole amide compound I and a preparation method thereof and application of the novel pyrazole amide compound I in prevention and treatment of plant pathogenic disease and pest killing. The novel pyrazole amide compound
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Paragraph 0035; 0046-0047
(2021/06/26)
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- Nucleophilic aromatic substitution reactions under aqueous, mild conditions using polymeric additive HPMC
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The use of the inexpensive, benign, and sustainable polymer, hydroxypropyl methylcellulose (HPMC), in water enables nucleophilic aromatic subsitution (SNAr) reactions between various nucleophiles and electrophiles. The mild reaction conditions facilitate a broad functional group tolerance that can be utilized for subsequent derivatization for the synthesis of pharmaceutically relevant building blocks. The use of only equimolar amounts of all reagents and water as reaction solvent reveals the greenness and sustainability of the methodology presented herein.
- Ansari, Tharique N.,Borlinghaus, Niginia,Braje, Leon H.,Braje, Wilfried M.,Handa, Sachin,Ogulu, Deborah,Wittmann, Valentin
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supporting information
p. 3955 - 3962
(2021/06/17)
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- Optimisation of 2-(N-phenyl carboxamide) triazolopyrimidine antimalarials with moderate to slow acting erythrocytic stage activity
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Malaria is a devastating parasitic disease caused by parasites from the genus Plasmodium. Therapeutic resistance has been reported against all clinically available antimalarials, threatening our ability to control the disease and therefore there is an ongoing need for the development of novel antimalarials. Towards this goal, we identified the 2-(N-phenyl carboxamide) triazolopyrimidine class from a high throughput screen of the Janssen Jumpstarter library against the asexual stages of the P. falciparum parasite. Here we describe the structure activity relationship of the identified class and the optimisation of asexual stage activity while maintaining selectivity against the human HepG2 cell line. The most potent analogues from this study were shown to exhibit equipotent activity against P. falciparum multidrug resistant strains and P. knowlesi asexual parasites. Asexual stage phenotyping studies determined the triazolopyrimidine class arrests parasites at the trophozoite stage, but it is likely these parasites are still metabolically active until the second asexual cycle, and thus have a moderate to slow onset of action. Non-NADPH dependent degradation of the central carboxamide and low aqueous solubility was observed in in vitro ADME profiling. A significant challenge remains to correct these liabilities for further advancement of the 2-(N-phenyl carboxamide) triazolopyrimidine scaffold as a potential moderate to slow acting partner in a curative or prophylactic antimalarial treatment.
- Bailey, Brodie L.,Nguyen, William,Ngo, Anna,Goodman, Christopher D.,Gancheva, Maria R.,Favuzza, Paola,Sanz, Laura M.,Gamo, Francisco-Javier,Lowes, Kym N.,McFadden, Geoffrey I.,Wilson, Danny W.,Laleu, Beno?t,Brand, Stephen,Jackson, Paul F.,Cowman, Alan F.,Sleebs, Brad E.
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- Decarboxylative ipso Amination of Activated Benzoic Acids
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In the presence of a bimetallic Pd/Cu system with 1,10-phenanthroline as the ligand and either air or N-methylmorpholine N-oxide as the oxidant, electron-deficient benzoic acids undergo oxidative decarboxylative coupling with unprotected amines. This operationally simple aniline synthesis is widely applicable with respect to the amine and gives good yields, even on multigram scale. The orthogonality of this reaction to other Pd-catalyzed cross-couplings allows the concise synthesis of multisubstituted arenes by sequential C?C, C?Cl, and C?N functionalizations. Mechanistic investigations suggest the intermediacy of a hypervalent Pd species.
- Pichette Drapeau, Martin,Bahri, Janet,Lichte, Dominik,Goo?en, Lukas J.
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supporting information
p. 892 - 896
(2019/01/04)
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- Trifluoromethyl arylamides with antileukemia effect and intracellular inhibitory activity over serine/arginine-rich protein kinases (SRPKs)
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The serine/arginine-rich protein kinases (SRPKs) have frequently been found with altered activity in a number of cancers, suggesting they could serve as potential therapeutic targets in oncology. Here we describe the synthesis of a series of twenty-two tr
- Siqueira, Raoni Pais,Barros, Marcus Vinícius de Andrade,Barbosa, éverton de Almeida Alves,Onofre, Thiago Souza,Gon?alves, Victor Hugo Sousa,Pereira, Higor Sette,Silva Júnior, Abelardo,de Oliveira, Leandro Licursi,Almeida, Márcia Rogéria,Fietto, Juliana Lopes Rangel,Teixeira, Róbson Ricardo,Bressan, Gustavo Costa
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- METHOD OF REGULATING PHOSPHORYLATION OF SR PROTEIN AND ANTIVIRAL AGENTS COMPRISING SR PROTEIN ACTIVITY REGULATOR AS THE ACTIVE INGREDIENT
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The present invention provides: (1) antiviral agents that act by reducing or inhibiting the activity of SR proteins, more specifically, (i) antiviral agents that act by enhancing dephosphorylation of SR proteins, and (ii) antiviral agents that act by inhi
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Page/Page column 34; 35
(2008/06/13)
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- (Aminophenyl)morpholines and use thereof
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(2-Aminophenyl)morpholine compounds having a haloalkyl, lower alkylsulfonyl, halo-lower alkylsulfonyl, or branched-chain alkyl substituent on the aromatic ring para to the morpholino nitrogen. The compounds are useful as herbicides and may be used as inte
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- Morpholinobenzimidazole N-oxides
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Tricyclic 1,2-morpholinobenzimidazole N-oxides having a trifluoromethyl or branched-chain alkyl group on the aromatic ring para to the morpholino nitrogen. The compounds are herbicidal and can be used as intermediates for preparing herbicidal compounds.
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- Herbicidal morpholinobenzimidazoles
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Tricyclic 1,2-morpholinobenzimidazoles having a haloalkyl, alkylsulfonyl, haloalkylsulfonyl, halo or lower alkyl substituent on the aromatic ring para to the morpholino nitrogen. The aromatic ring and morpholino ring may also have other substituents. The
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