210686-42-3Relevant academic research and scientific papers
Multistep solid-phase synthesis of an antibiotic and receptor tyrosine kinase inhibitors using the traceless phenylhydrazide linker
Stieber, Frank,Grether, Uwe,Mazitschek, Ralph,Soric, Natascha,Giannis, Athanassios,Waldmann, Herbert
, p. 3282 - 3291 (2003)
The hydrazide group is an oxidatively cleavable traceless linker for solid-phase chemistry. This linker technology was used to develop a multistep solid-phase synthesis of an antibiotic that is active against Mycobacterium tuberculosis. Furthermore, we describe an efficient method for the traceless synthesis of 2-aminothiazoles that display dual inhibitory activity against the receptor tyrosine kinases VEGFR-2 and Tie-2. The synthesis method proceeds through 9 steps on the solid phase and should give access to a much larger library of 2-aminothiazoles, from which a new class of anti-angiogenesis drugs may be developed.
Antimycobacterial activity of new ortho-, meta- and para-toluidine derivatives
Biava, Mariangela,Fioravanti, Rossella,Porretta, Giulio Cesare,Sleiter, Giancarlo,Deidda, Delia,Lampis, Giorgio,Pompei, Raffaello
, p. 721 - 727 (2007/10/03)
Novel toluidine derivatives are described. Some of them showed an interesting in vitro activity against Mycobacterium tuberculosis, M. smegmatis, M. marinum, M. gordonae, and M. avium. Some of them were more active than Streptomycin and Isoniazid, which were used as controls, against M. avium and M. gordonae. In particular, we confirm the good activity of biphenyl derivatives.
An oxidation-labile traceless linker for solid-phase synthesis
Stieber, Frank,Grether, Uwe,Waldmann, Herbert
, p. 1073 - 1077 (2007/10/03)
Traceless release of biaryls, acetylenes, alkenes, heterocycles, thioethers, and secondary amines from different solid supports can be achieved under very mild conditions by using a hydrazide group. This group, which is converted into an acyl diazene by oxidation and subsequently cleaved by a nucleophile (see scheme), is thus an attractive new linker for solid- phase synthesis and combinatorial chemistry.
N-[4-(1,1'-biphenyl)methyl]-4-(4-thiomorpholinylmethyl) benzenamines as non-oxazolidinone analogues of antimycobacterial U-100480
Artico, Marino,Mai, Antonello,Sbardella, Gianluca,Massa, Silvio,Lampis, Giorgio,Deidda, Delia,Pompei, Raffaello
, p. 1493 - 1498 (2007/10/03)
Thiomorpholine analogues of U-100480 with the biphenylmethyl group replacing the acetamidomethyloxazolidinone moiety have been synthesized and tested as antimycobacterial agents together with various related derivatives. Some biphenyl derivatives were endowed with high activity against Mycobacterium tuberculosis and other non-tuberculous mycobacteria.
