104479-01-8Relevant 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.
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
Synthesis, molecular modeling, and structure - Activity relationship of benzophenone-based CAAX-peptidomimetic farnesyltransferase inhibitors
Sakowski,B?hm,Sattler,Dahse,Schlitzer
, p. 2886 - 2899 (2007/10/03)
Because of the involvement of farnesylated proteins in oncogenesis, inhibition of the protein-modifying enzyme farnesyltransferase is considered a major emerging strategy in cancer therapy. Here, we describe the structure - activity relationship of a nove
Quinone Imine Route to Benzimidazol-2-ylcarbamates. Part 1. Synthesis of Open-chain and Cyclic 5-Acylamino Derivatives.
Rajappa, Srinivasachari,Sreenivasan, Ramaswami,Khalwadekar, Asha
, p. 1657 - 1675 (2007/10/02)
The synthesis of the N',N''-bismethoxycarbonyl-N-(4-acylaminophenyl)guanidines (4) and (7) is described.Oxidation of these with LTA has led to the benzimidazol-2-ylcarbamates. (8), (9) and (10) through a regiospecific cyclisation of quinone imine intermediates.If the acylamino group is part of a ring, the yield of benzimidazoles (15) increases with the size of the lactam ring.The direction of ring closure may be controlled by electronic and steric factors.
