265648-22-4Relevant academic research and scientific papers
Structure-activity relationships of novel anti-malarial agents: Part 5. N-(4-acylamino-3-benzoylphenyl)-[5-(4-nitrophenyl)-2-furyl]acrylic acid amides
Wiesner, Jochen,Kettler, Katja,Sakowski, Jacek,Ortmann, Regina,Jomaa, Hassan,Schlitzer, Martin
, p. 361 - 363 (2007/10/03)
We have developed the [5-(4-nitrophenyl)-2-furyl]acrylic acid substituted benzophenone 4g as a novel lead for anti-malarial agents. Here, we demonstrated that the acyl residue at the 2-amino group of the benzophenone core structure has to be a phenylacetic acid substructure substituted in its para-position with methyl or other substituents of similar size. The trifluoromethyl substituted derivative displayed an IC50 of 47 nM against the multi-drug resistant Plasmodium falciparum strain Dd2.
Use of 2-phenylene diamine derivatives for the treatment of infections
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, (2008/06/13)
The invention relates to the use of compounds of formula (I), wherein n=0-3; R1, R2=H, alkyl, aryl, heteroaryl, acyl; R3=H, halogen, alkyl, aryl, heteroaryl, arylalkyl, acyl, CN, NO2, R4—X—; R4/
Structure-activity relationships of novel anti-malarial agents. Part 3: N-(4-Acylamino-3-benzoylphenyl)-4-propoxycinnamic acid amides
Wiesner, Jochen,Kettler, Katja,Jomaa, Hassan,Schlitzer, Martin
, p. 543 - 545 (2007/10/03)
We have described 5-(4-propoxycinnamoylamino)-2-(4-tolylacetylamino)benzophenone 6e as a novel lead for anti-malarial agents. Anti-malarial activity of these 5-(4-propoxycinnamoylamino)benzophenones proved to be quite sensitive against variations of the a
Different amino acid replacements in CAAX-tetrapeptide based peptidomimetic farnesyltransferase inhibitors
Schlitzer, Martin,Sattler, Isabel,Dahse, Hans-Martin
, p. 124 - 132 (2007/10/03)
In a series of CAAX-tetrapeptide based farnesyltransferase inhibitors it has been shown that the central AA-dipeptide can be replaced by tranexamic acid, 4-aminobenzenesulfonic acid, and 3-amino-N-(2,3- dimethylphenyl)benzenesulfonamide, respectively, yielding inhibitors active in the low micromolar range. Lipophilic derivatives of these compounds showed moderate antiproliferative activity against different tumor cell lines. A promising class of peptidomimetic farnesyltransferase inhibitors was discovered through the replacement of the terminal AAX motif of the CAAX- tetrapeptide by 2-acylamino-5-aminobenzophenones.
