375-16-6Relevant articles and documents
Synthesis and evaluation of novel monosubstituted sulfonylurea derivatives as antituberculosis agents
Pan, Li,Jiang, Ying,Liu, Zhen,Liu, Xing-Hai,Liu, Zhuo,Wang, Gang,Li, Zheng-Ming,Wang, Di
scheme or table, p. 18 - 26 (2012/07/01)
A series of novel monosubstituted sulfonylurea derivatives 10a-y were synthesized and characterized by 1H NMR, 13C NMR and HRMS. These compounds were evaluated against Mycobacterium tuberculosis H37Rv in vitro. The results showed compounds 10f, 10k and 10s exhibited moderate antituberculosis activities with MIC values in the range of 20-100 mg/L. Compounds 10b and 10o displayed good antituberculosis activities (MIC 10 mg/L), which were comparable with that of the sulfometuron methyl. Both of the two compounds showed little cytotoxicities, with an IC50 against THP-1 cells greater than 100 mg/L.
Multiple pathways in cyclodextrin-catalyzed hydrolysis of perfluoroalkylamides
Granados, Alejandro,De Rossi, Rita H.
, p. 3690 - 3696 (2007/10/02)
The hydrolysis of p-nitroanilide of perfluoroalkanoic acids, CF3(CF2)nCO-, with n = 1, 2, 3, 5, 6, and 7, 1a-f, was studied in the presence of β-cyclodextrin (CD). All reactions were catalyzed by CD through the formation of a 1:1 and 1:2 inclusion complexes. The association equilibrium constants for the 1:1 complexes were dependent on the number of carbons of the fluoroalkyl chain, whereas those of the 1:2 complexes were almost independent. These results indicate that, in the former case, the perfluoroalkyl chain is included, while in the latter, the CD unit encloses the aryl ring. For compounds 1a,b both complexes were more reactive than the substrate itself. The ratio of the reaction of complexed to uncomplexed substrate had its highest value for 1a in the case of the 1:1 complex, and for 1b, the 1:2 complex. This is attributed to the geometry of the complexes. Although compounds 1c-e reacted at the same rates in the free or 1:1 complexed form, CD accelerated the reactions because of an increase of the pKa of the substrate, which results in a higher concentration of the neutral reactive substrate at the same pH. Compound 1f formed aggregates even at 10-6 M concentration, and CD-induced deaggregation resulted in catalysis of the reaction.
REGIOSPECIFIC PREPARATION OF α,α-DIHALOFLUOROMETHYL PERFLUOROALKYL KETONES.
Jeong, In Howa,Burton, Donald J.,Cox, Daryl G.
, p. 3709 - 3712 (2007/10/02)
Acylation of F-phosphoranium salts with F-acyl chlorides gives the corresponding Z-perfluoro betaine in high yield.Subsequent chlorination or bromination regiospecifically yields the α,α-dihalofluoromethyl perfluoroalkyl ketones.
