50903-50-9Relevant articles and documents
Combination of silyl carbamate and amino acid fluoride for solid-phase peptide synthesis
Sakamoto, Kimitoshi,Nakahara, Yoshiaki,Ito, Yukishige
, p. 1515 - 1518 (2002)
Diketopiperadine (DKP) formation is an often encountered side reaction in the synthesis of peptide having C-terminal proline ester. A novel strategy for the avoidance of this side reaction was developed, which utilizes Pfp ester of Tsoc-amino acid and Fmo
Simultaneous protection and activation of amino acids using propargyl pentafluorophenyl carbonate
Ramesh, Ramapanicker,Rajasekaran, Sakthidevi,Gupta, Rohit,Chandrasekaran, Srinivasan
, p. 1933 - 1936 (2007/10/03)
A very efficient method for the simultaneous protection of the amino group and activation of the carboxyl group of amino acids is reported using propargyl pentafluorophenyl carbonate (PocOPfp). The amino group is protected as a propargyloxycarbonyl (Poc) derivative, and the carboxyl group is activated as a pentafluorophenyl ester. The yields obtained are good to excellent ranging from 60 to 87%.
Synthesis, Degradation, and Antimicrobial Properties of Targeted Macromolecular Prodrugs of Norfloxacin
Roseeuw, Eveline,Coessens, Veerle,Balazuc, Anne-Marie,Lagranderie, Micheline,Chavarot, Pierre,Pessina, Augusto,Neri, Maria Grazia,Schacht, Etienne,Marchal, Gilles,Domurado, Dominique
, p. 3435 - 3441 (2007/10/03)
Long-term antibiotic treatment is required to cure tuberculosis. Targeted antibiotics should improve the efficacy of treatment by concentrating the drugs close to the bacteria. The aim of the present study was to synthesize targeted conjugates. For this purpose, we used mannose as a homing device to direct norfloxacin into macrophages. Dextran was used as the polymer bearing both mannose and norfloxacin. Using different peptide spacer arms to link norfloxacin to dextran, we demonstrated that norfloxacin acts as an antibiotic only when it is released in its native form. Also, targeting by using mannose as a homing device is required to achieve antimycobacterial activity in vivo. Thus, norfloxacin, which is inactive against mycobacteria in its native form in vivo, can be transformed into an active drug by targeting.