62806-31-9Relevant academic research and scientific papers
Non-thiol farnesyltransferase inhibitors: N-(4-tolylacetylamino-3- benzoylphenyl)-3-arylfurylacrylic acid amides
Mitsch, Andreas,Wi?ner, Pia,Silber, Katrin,Haebel, Peter,Sattler, Isabel,Klebe, Gerhard,Schlitzer, Martin
, p. 4585 - 4600 (2007/10/03)
We have designed arylfurylacryl-substituted benzophenones as non-thiol farnesyltransferase inhibitors utilizing a novel aryl binding site of farnesyltransferase. These compounds display activity in the low nanomolar range. We have designed arylfurylacryl-
Structure-activity relationships of novel anti-malarial agents part 8. Effect of different central aryls in biarylacryloylaminobenzophenones on antimalarial activity
Wiesner,Mitsch,Altenkaemper,Ortmann,Jomaa,Schlitzer, Martin
, p. 854 - 856 (2007/10/03)
Replacement of the 2,5-disubstituted furyl residue present in the known antimalarial agents 8 by other aryl residues resulted in a more or less reduced antimalarial activity in most cases. The only exemption was the 2,4-thienylene compound 11a displaying activity with an IC50 value of 120 nM. In conclusion, the 2,5-furylene compound 8e remains to represent the most active antimalarial agent in this series of farnesyltransferase inhibitors.
Structure-activity relationships of novel anti-malarial agents. Part 4: N-(3-Benzoyl-4-tolylacetylaminophenyl)-3-(5-aryl-2-furyl)acrylic acid amides
Wiesner, Jochen,Mitsch, Andreas,Wissner, Pia,Kraemer, Oliver,Jomaa, Hassan,Schlitzer, Martin
, p. 2681 - 2683 (2007/10/03)
In a previous report, we have described novel anti-malarial compounds based on a 2,5-diaminobenzophenone scaffold. Here, we have invesigated acryloyl derivatives carrying a biaryl structure consisting of a terminal aryl residue and a central 2-furyl ring. Several compounds were obtained in the series of para-substituted phenylfurylacryloyl derivatives that displayed improved anti-malarial activity in comparison to earlier described derivatives. From the structure-activity relationships it can be deduced that there has to be a lipophilic moiety in the para-position of the terminal phenyl residue. Furthermore, there are indications that, alternatively, activity may benefit from the presence of a polar moiety with hydrogen bond acceptor properties.
ARYLATION OF FURAN COMPOUNDS BY ARENEDIAZONIUM SALTS
Obushak, N. D.,Ganushchak, N. I.,Lesyuk, A. I.,Dzikovskaya, L. M.,Kisilitsa, P. P.
, p. 748 - 753 (2007/10/02)
3-(5-Aryl-2-furyl)acrylic acids were obtained by the reaction of 5-arylfurfurals with malonic acid.They were arylated by diazonium salts with decarboxylation and the formation of 5-aryl-2-styrylfurans.The latter were also obtained by the interaction of furylacrolein with diazonium salts.This reaction also gave 3-(5-aryl-2-furyl)acroleins and the corresponding arylfurylacrylic acids, which were arylated again with the release of CO2 and the formation of 5-aryl-2-styrylfurans. 3-(5-Aryl-2-furyl)acroleins were also synthesized by the condensation of 5-arylfurfurals with acetaldehyde under phase-transfer conditions.The s-trans configuration of the furan ring and the exocyclic double bond were established in the obtained compounds by the PMR method.
