823219-88-1Relevant academic research and scientific papers
ISOXAZOLES AS PEPTIDE DEFORMYLASE INHIBITORS
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Page/Page column 24; 32, (2010/02/11)
Isoxazole compounds of formula (I) and pharmaceutically acceptable salts or esters thereof are peptide deformylase inhibitors useful in the treatment or prevention of infections and other disease in which peptide deformylases are involved, especially in t
Sequential ring-closing metathesis/Pd-catalyzed, Si-assisted cross-coupling reactions: General synthesis of highly substituted unsaturated alcohols and medium-sized rings containing a 1,3-cis-cis diene unit
Denmark, Scott E.,Yang, Shyh-Ming
, p. 9695 - 9708 (2007/10/03)
A sequential ring-closing metathesis/silicon-assisted cross-coupling protocol has been developed. Alkenyldimethylsilyl ethers of allylic, homoallylic and bis(homoallylic) alcohols undergo facile ring closure with Schrock's catalyst to afford 5-, 6-, and 7-membered cycloalkenylsiloxanes, respectively, in some cases with substituents on both alkenyl carbons. These siloxanes are highly effective coupling partners that afford styrenes and dienes (with various aryl and alkenyl halides) in high yield and specificity as well as good functional group compatibility. The siloxanes bearing a Z-iodoalkenyl tether undergo an intramolecular coupling process in the presence of [allylPdCl] 2 which constitutes a powerful method for the construction of medium-sized rings with an internal 1,3-cis-cis diene unit. The formation of 9-, 10-, 11-, and 12-membered carbocyclic dienes is achieved in good yield. Extension to the synthesis of 9-membered ring unsaturated ethers has also been accomplished. Noteworthy features of this process include: (1) highly stereospecific intramolecular coupling, (2) flexible positioning of the revealed hydroxy group, and (3) potential extension to other medium-sized carbocycles and heterocycles. Graphical Abstract.
Isoxazole-3-hydroxamic acid derivatives as peptide deformylase inhibitors and potential antibacterial agents
Calí, Patrizia,N?rum, Lars,Mukhija, Seema,Hjelmencrantz, Anders
, p. 5997 - 6000 (2007/10/03)
The synthesis and initial in vitro evaluation of isoxazole-3-hydroxamic acid derivatives as a new class of PDF inhibitors are reported. A series of isoxazole-3-hydroxamic acid derivatives has been identified as a new class of small, nonpeptidic inhibitors of peptide deformylase (PDF). The synthesis, enzyme inhibition and preliminary investigation of the binding mode of this potential antibacterial compounds are reported.
