57181-86-9Relevant articles and documents
ICI 56,780 optimization: Structure-activity relationship studies of 7-(2-phenoxyethoxy)-4(1H)-quinolones with antimalarial activity
Maignan, Jordany R.,Lichorowic, Cynthia L.,Giarrusso, James,Blake, Lynn D.,Casandra, Debora,Mutka, Tina S.,LaCrue, Alexis N.,Burrows, Jeremy N.,Willis, Paul A.,Kyle, Dennis E.,Manetsch, Roman
, p. 6943 - 6960 (2016/08/05)
Though malaria mortality rates are down 48% globally since 2000, reported occurrences of resistance against current therapeutics threaten to reverse that progress. Recently, antimalarials that were once considered unsuitable therapeutic agents have been revisited to improve physicochemical properties and efficacy required for selection as a drug candidate. One such compound is 4(1H)-quinolone ICI 56,780, which is known to be a causal prophylactic that also displays blood schizonticidal activity against P. berghei. Rapid induction of parasite resistance, however, stalled its further development. We have completed a full structure-activity relationship study on 4(1H)-quinolones, focusing on the reduction of cross-resistance with atovaquone for activity against the clinical isolates W2 and TM90-C2B, as well as the improvement of microsomal stability. These studies revealed several frontrunner compounds with superb in vivo antimalarial activity. The best compounds were found to be curative with all mice surviving a Plasmodium berghei infection after 30 days.
2-Aminobenzothiazole derivatives: Search for new antifungal agents
Catalano, Alessia,Carocci, Alessia,Defrenza, Ivana,Muraglia, Marilena,Carrieri, Antonio,Van Bambeke, Fran?oise,Rosato, Antonio,Corbo, Filomena,Franchini, Carlo
, p. 357 - 364 (2013/07/27)
A new series of 6-substituted 2-aminobenzothiazole derivatives were synthesized and screened in vitro as potential antimicrobials. Almost all the compounds showed antifungal activity. In particular, compounds 1n,o, designed on the basis of molecular modeling studies, were the best of the series, showing MIC values of 4-8 μg/mL against Candida albicans, Candida parapsilosis and Candida tropicalis. None of the two compounds did show any cytotoxicity effect on human THP-1 cells.
Arylisothiocyanate for the regulation of plant growth
-
, (2008/06/13)
New arylisothiocyanates corresponding to the formula STR1 wherein R represents alkyl, alkoxy or halogen X represents oxygen or sulfur and P represents an integer of from 2 to 5 are disclosed. They can be used for the regulation of plant growth especially for the dessication and defoliation of unlignified parts of plants above the soil.