930101-83-0Relevant academic research and scientific papers
Design, synthesis and cytotoxic evaluation of a library of oxadiazole-containing hybrids
Barrionuevo, Elizabeth,Bellizzi, Yanina,Blank, Viviana C.,Boggián, Dora B.,Camacho, Cristián M.,Mata, Ernesto G.,Pizzio, Marianela G.,Roces, David L.,Roguin, Leonor P.
, p. 29741 - 29751 (2021/10/07)
The development of hybrid compounds led to the discovery of new pharmacologically active agents for some of the most critical diseases, including cancer. Herein, we describe a new series of oxadiazole-containing structures designed by a molecular hybridiz
Structure-based design of novel dihydroisoquinoline BACE-1 inhibitors that do not engage the catalytic aspartates
Bowers, Simeon,Xu, Ying-Zi,Yuan, Shendong,Probst, Gary D.,Hom, Roy K.,Chan, Wayman,Konradi, Andrei W.,Sham, Hing L.,Zhu, Yong L.,Beroza, Paul,Pan, Hu,Brecht, Eric,Yao, Nanhua,Lougheed, Julie,Tam, Danny,Ren, Zhao,Ruslim, Lany,Bova, Michael P.,Artis, Dean R.
, p. 2181 - 2186 (2013/04/23)
The structure-activity relationship of a series of dihydroisoquinoline BACE-1 inhibitors is described. Application of structure-based design to screening hit 1 yielded sub-micromolar inhibitors. Replacement of the carboxylic acid of 1 was guided by X-ray
IAP ANTAGONISTS
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Paragraph 00265, (2014/01/09)
There are disclosed compounds that modulate the activity of inhibitors of apoptosis (IAPs), pharmaceutical compositions containing said compounds and methods of treating proliferative disorders and disorders of dysregulated apoptosis, such as cancer, utilizing the compounds of the invention.
The preparation of optically active α-amino 4H-[1,2,4]oxadiazol-5-ones from optically active α-amino acids
Mangette, John E.,Johnson, Matthew R.,Le, Van-Duc,Shenoy, Rajesh A.,Roark, Howard,Stier, Michael,Belliotti, Thomas,Capiris, Thomas,Guzzo, Peter R.
experimental part, p. 9536 - 9541 (2009/12/28)
Optically active α-amino 4H-[1,2,4]oxadiazol-5-ones (oxadiazolones) were prepared from optically active α-amino acids in five synthetic steps. The oxadiazolone moiety serves as a bioisosteric replacement for the carboxylic acid. Incorporation of an α-amino oxadiazolone into a representative dipeptide mimic is described.
Synthesis of 1,2,4-oxadiazole-linked orthogonally urethane-protected dipeptide mimetics
Sureshbabu, Vommina V.,Hemantha, Hosahalli P.,Naik, Shankar A.
, p. 5133 - 5136 (2008/12/20)
The synthesis of a new class of 1,2,4-oxadiazole-linked orthogonally urethane-protected dipeptide mimetics is described. The protocol employs a reaction between an N-protected amino acyl fluoride and an amino acid-derived amidoxime. All the three commonly
Synthesis of 3,5-disubstituted 1,2,4-oxadiazoles as peptidomimetic building blocks
Jakopin, ?iga,Ro?kar, Robert,Dolenc, Marija Sollner
, p. 1465 - 1468 (2008/02/02)
Twelve new 1,2,4-oxadiazole based compounds have been synthesized. Their structures contain a protected amine and a carboxyl or an ester group, and thus serve as potential peptidomimetic building blocks. The synthetic route is simple and mild conditions are used so that the chirality of the starting amino acids is retained.
