63762-07-2Relevant academic research and scientific papers
Synthesis and anti-Candida activity of novel 2-hydrazino-1,3-thiazole derivatives
Maillard, Ludovic T.,Bertout, Sébastien,Quinonéro, Ophélie,Akalin, Gül?en,Turan-Zitouni, Gülhan,Fulcrand, Pierre,Demirci, Fatih,Martinez, Jean,Masurier, Nicolas
, p. 1803 - 1807 (2013/04/10)
Eighteen new hydrazino-1,3-thiazole derivatives were evaluated against 8 strains of multi-resistant Candida spp. Introduction of an indolyl moiety linked to the hydrazone function enhanced the in vitro anti-Candida activity, with an activity spectrum towards Candida albicans strains. Introduction of a (S)-2-aminoethyl chain on the thiazole nucleus largely enhanced the in vitro antifungal activity, with a selectivity oriented towards non-C. albicans species.
Synthesis and SAR Studies of diarylpyrrole anticoccidial agents
Qian, Xiaoxia,Liang, Gui-Bai,Feng, Dennis,Fisher, Michael,Crumley, Tami,Rattray, Sandra,Dulski, Paula M.,Gurnett, Anne,Leavitt, Penny Sue,Liberator, Paul A.,Misura, Andrew S.,Samaras, Samantha,Tamas, Tamas,Schmatz, Dennis M.,Wyvratt, Matthew,Biftu, Tesfaye
, p. 2817 - 2821 (2007/10/03)
2-(4-Fluorophenyl)-3-(4-pyridinyl)-5-substituted pyrroles were prepared and evaluated as anticoccidial agents in both in vitro and in vivo assays. Among the compounds evaluated, the dimethylamine-substituted pyrrole 19a is the most potent inhibitor of Eimeria tenella PKG (cGMP-dependent protein kinase). Further SAR studies on the side chain of the 2-pyrrolidine nitrogen did not enhance in vivo anticoccidial activity.
α-Amino Ketones - A Contribution to the Synthesis of Optically Active Derivatives of Amino Acids and Peptides
Fittkau, Siegfried,Jahreis, Guenther,Peters, Klaus,Balaspiri, Lajos
, p. 529 - 538 (2007/10/02)
The synthesis of N-Z-protected methyl ketones from amino acids via the chloromethyl ketones and dehalogenation of the latter with zinc in glacial acetic acid is described.Deprotection of the methyl ketones results in the formation of hydrohalogenides of the α-aminoalkyl methyl ketones further converted to N-acylated peptide ketones as analogs of peptide hormones or as competitively acting substrate analogs of proteolytic enzymes.Aminoacetone is conveniently prepared as well as methyl-pyrrolidyl ketone and methyl-piperidyl ketone.
