5555-32-8Relevant academic research and scientific papers
Synthesis of Imidazoles and Oxazoles via a Palladium-Catalyzed Decarboxylative Addition/Cyclization Reaction Sequence of Aromatic Carboxylic Acids with Functionalized Aliphatic Nitriles
Dai, Ling,Yu, Shuling,Lv, Ningning,Ye, Xuanzeng,Shao, Yinlin,Chen, Zhongyan,Chen, Jiuxi
supporting information, p. 5664 - 5668 (2021/08/01)
We herein report an efficient approach for the assembly of multiply substituted imidazoles and oxazoles in a single-step manner. These transformations are based on a decarboxylation addition and annulation of readily accessible aromatic carboxylic acids a
Nickel-Catalyzed Construction of 2,4-Disubstituted Imidazoles via C–C Coupling and C?N Condensation Cascade Reactions
Fang, Shengyang,Yu, Haihua,Yang, Xicheng,Li, Jianqi,Shao, Liming
supporting information, p. 3312 - 3317 (2019/06/13)
A convenient Ni(II)-catalyzed C?C and C?N cascade coupling reaction was developed to directly access various 2,4-disubstituted imidazoles. The reaction scope covers a variety of aryl and aliphatic substitutions, which demonstrate moderate-to-excellent yie
An optimised series of substituted N-phenylpyrrolamides as DNA gyrase B inhibitors
Tiz, Davide Benedetto,Skok, ?iga,Durcik, Martina,Toma?i?, Tihomir,Ma?i?, Lucija Peterlin,Ila?, Janez,Zega, Anamarija,Draskovits, Gábor,Révész, Tamás,Nyerges, ákos,Pál, Csaba,Cruz, Cristina D.,Tammela, P?ivi,?igon, Du?an,Kikelj, Danijel,Zidar, Nace
, p. 269 - 290 (2019/02/20)
ATP competitive inhibitors of DNA gyrase and topoisomerase IV have great therapeutic potential, but none of the described synthetic compounds has so far reached the market. To optimise the activities and physicochemical properties of our previously reported N-phenylpyrrolamide inhibitors, we have synthesized an improved, chemically variegated selection of compounds and evaluated them against DNA gyrase and topoisomerase IV enzymes, and against selected Gram-positive and Gram-negative bacteria. The most potent compound displayed IC50 values of 6.9 nM against Escherichia coli DNA gyrase and 960 nM against Staphylococcus aureus topoisomerase IV. Several compounds displayed minimum inhibitory concentrations (MICs) against Gram-positive strains in the 1–50 μM range, one of which inhibited the growth of Enterococcus faecalis, Enterococcus faecium, S. aureus and Streptococcus pyogenes with MIC values of 1.56 μM, 1.56 μM, 0.78 μM and 0.72 μM, respectively. This compound has been investigated further on methicillin-resistant S. aureus (MRSA) and on ciprofloxacin non-susceptible and extremely drug resistant strain of S. aureus (MRSA VISA). It exhibited the MIC value of 2.5 μM on both strains, and MIC value of 32 μM against MRSA in the presence of inactivated human blood serum. Further studies are needed to confirm its mode of action.
N-cyanoalkyl-N-haloalkylthio carboxamides as fungicides
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, (2008/06/13)
N-cyanoalkyl-N-haloalkylthio alkyl-, aryl- and aralkyl-carboxamides of the general formula: STR1 wherein R is alkyl of 1 to 10 carbon atoms, cycloalkyl of 3 to 10 carbon atoms, lower alkenyl of 2 to 6 carbon atoms or lower alkynyl of 2 to 6 carbon atoms, all optionally substituted with 1 to 4 halogen atoms; lower alkoxyalkylene; aryl of 6 to 12 carbon atoms; aralkyl of 7 to 16 carbon atoms; or substituted aryl or substituted aralkyl both substituted with 1 to 3 substituents independently selected from phenyl, lower alkyl of 1 to 6 carbon atoms, lower alkoxy of 1 to 6 carbon atoms, lower alkylthio of 1 to 6 carbon atoms, halogen, nitro, cyano, STR2 wherein R4 is hydrogen or lower alkyl of 1 to 6 carbon atoms, STR3 wherein R5 and R6 are independently hydrogen or lower alkyl of 1 to 6 carbon atoms; R1 and R2 are independently hydrogen, or lower alkyl of 1 to 6 carbon atoms; and R3 is alkyl of 1 to 3 carbon atoms substituted with 3 to 6 halogen atoms or trihalovinyl are fungicidal.
