198991-76-3Relevant articles and documents
Functionalised bicyclic tetramates derived from cysteine as antibacterial agents
Panduwawala, Tharindi D.,Iqbal, Sarosh,Thompson, Amber L.,Genov, Miroslav,Pretsch, Alexander,Pretsch, Dagmar,Liu, Shuang,Ebright, Richard H.,Howells, Alison,Maxwell, Anthony,Moloney, Mark G.
supporting information, p. 5615 - 5632 (2019/06/13)
Routes to bicyclic tetramates derived from cysteine permitting ready incorporation of functionality at two different points around the periphery of a heterocyclic skeleton are reported. This has enabled the identification of systems active against Gram-positive bacteria, some of which show gyrase and RNA polymerase inhibitory activity. In particular, tetramates substituted with glycosyl side chains, chosen to impart polarity and aqueous solubility, show high antibacterial activity coupled with modest gyrase/polymerase activity in two cases. An analysis of physicochemical properties indicates that the antibacterially active tetramates generally occupy physicochemical space with MW of 300-600, clog D7.4 of -2.5 to 4 and rel. PSA of 11-22%. This work demonstrates that biologically active 3D libraries are readily available by manipulation of a tetramate skeleton.
(Substituted)acyl dipeptidyl inhibitors of the ICE/ced-3 family of cysteine proteases
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Page 26, (2010/02/05)
This invention is directed to novel (substituted)acyl dipeptidyl ICE/ced-3 family inhibitor compounds. The invention is also directed to pharmaceutical compositions containing these compounds, as well as the use of such compositions in the treatment of pa
Diels-Alder reactions of 2-azadienes derived from cysteine and serine methyl esters and aldehydes
Gilchrist,Gilchrist, Thomas L.,Rocha Gonsalves D'A.,RochaGonsalves, Antonio M. D'A.,Pinho Melo,PinboMelo, Teresa M. V. D.
, p. 13709 - 13724 (2007/10/02)
The Diels-Alder reactions of N-benzylidenedehydroalanine methyl ester 1a with but-3-en-2-one and with other electron deficient dienophiles have been found to give new dihydro- and tetrahydropyridines. The cycloaddition reactions are regioselective but not