500127-73-1Relevant articles and documents
A new lead for nonpeptidic active-site-directed inhibitors of the severe acute respiratory syndrome coronavirus main protease discovered by a combination of screening and docking methods
Kaeppler, Ulrich,Stiefl, Nikolaus,Schiller, Markus,Vicik, Radim,Breuning, Alexander,Schmitz, Werner,Rupprecht, Daniel,Schmuck, Carsten,Baumann, Knut,Ziebuhr, John,Schirmeister, Tanja
, p. 6832 - 6842 (2005)
The coronavirus main protease, Mpro, is considered to be a major target for drugs suitable for combating coronavirus infections including severe acute respiratory syndrome (SARS). An HPLC-based screening of electrophilic compounds that was perf
Synthesis and Evaluation of Non-peptidic Cysteine Protease Inhibitors of P. falciparum Derived from Etacrynic Acid
Dude, Marie-Adrienne,Kaeppler, Ulrich,Herb, Monika,Schiller, Markus,Schulz, Franziska,Vedder, Birgit,Heppner, Saskia,Pradel, Gabriele,Gut, Jiri,Rosenthal, Philip J.,Schirmeister, Tanja,Leippe, Matthias,Gelhaus, Christoph
scheme or table, p. 19 - 35 (2009/09/08)
A series of etacrynic acid derivatives was synthesized and screened for their in vitro activity against Plasmodium falciparum, as well as their activity against recombinantly expressed falcipain-2 and -3. The two most active compounds of the series displayed IC50 values of 9.0 and 18.8 μM against Plasmodia.
Palladium-catalyzed cleavage of O/N-propargyl protecting groups in aqueous media under a copper-free condition
Pal, Manojit,Parasuraman, Karuppasamy,Yeleswarapu, Koteswar Rao
, p. 349 - 352 (2007/10/03)
(Figure presented) A copper-free palladium-mediated cleavage of O/N-propargyl bonds in aqueous media has been investigated, affording a mild and convenient method for the deprotection of phenols and anilines. The methodology could be utilized for the selective removal of propargyl groups from aryl ethers and amines without affecting a variety of unprotected functional groups present in the substrates. The mechanism and scope of the reaction is discussed.
