39684-46-3Relevant academic research and scientific papers
Efficient synthesis of (Z)- and (E)-methyl 2-(methoxyimino)-2-phenylacetate
Wu, Yong-Jin,Huang, Stella,Ng, Alicia,Gao, Qi,Roy Kimura,Langley, David R.
scheme or table, p. 2144 - 2147 (2010/05/19)
Direct oximation of 2-oxo-2-phenylacetate (3) gave the (Z)-methyl 2-(methoxyimino)-2-phenylacetate (1) in 71% yield, while the E oxime 2 was prepared from 3 in 65% yield via oxime isomerization of 2-(methoxyimino)-2-phenylacetic acid (5). Computational st
Combinatorial synthesis through disulfide exchange: Discovery of potent psammaplin A type antibacterial agents active against methicillin-resistant Staphylococcus aureus (MRSA)
Nicolaou,Hughes, Robert,Pfefferkorn, Jeffrey A.,Barluenga, Sofia,Roecker
, p. 4280 - 4295 (2007/10/03)
Psammaplin A is a symmetrical bromotyrosine-derived disulfide natural product isolated from the Psammaplysilla sponge, which exhibits in vitro antibacterial activity against methicillin-resistant Staphylococcus aureus (MRSA). Inspired by the structure of this marine natural product, a combinatorial scrambling strategy for the construction of heterodimeric disulfide analogues was developed and applied to the construction of a 3828-membered library starting from 88 homodimeric disulfides. These psammaplin A analogues were screened directly against various gram positive bacterial strains leading to the discovery of a series of potent antibacterial agents active against methicillin-resistant Staphylococcus aureus (MRSA). Among the most active leads derived from these studies are compounds 104, 105, 113, 115, 123, and 128. The present, catalytically-induced, disulfide exchange strategy may be extendable to other types of building blocks bearing thiol groups facilitating the construction of diverse discovery-oriented combinatorial libraries.
13-substituted milbemycin derivatives, their preparation and their use
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, (2008/06/13)
13-Substituted milbemycin derivatives having the formula (I): STR1 wherein: R1 is methyl, ethyl, isopropyl or sec-butyl; R2 is hydrogen or alkyl; X is (α-hydroxyimino- or α-alkoxyimino-substituted)-arylmethyl or (α-hydroxyimino- or α-alkoxyimino-substituted)-heterocyclylmethyl, N-substituted-aminophenyl or N-substituted-aminophenoxy; m is 0 or 1; and n is 0 or 1; are valuable as agricultural and horticultural anthelmintic, acaricidal and insecticidal agents.
