154972-38-0Relevant articles and documents
Peptidomimetic inhibitors of bacterial peptide deformylase
East, Stephen P.,Ayscough, Andrew,Toogood-Johnson, Ian,Taylor, Steven,Thomas, Wayne
scheme or table, p. 4032 - 4035 (2011/08/06)
A series of N-formyl hydroxylamine peptide deformylase inhibitors containing a cyclic azaamino acid moiety between the P1′ and P3′ substituents are presented. Selected compounds display antibacterial activity against pathogens associated with respiratory
The synthesis, structure and reactivity of 1-thioxotetrahydropyridazino[1,2-α][1,2,4]triazin-4(1H)-one
Jarrett, Sandra,Brown, Ainka,Singh-Wilmot, Marvadeen
scheme or table, p. 2755 - 2768 (2010/04/25)
The synthesis of 1-thioxotetrahydropyridazino[1,2-a][1,2,4]triazin-4-(1H)-one 3 in five steps from tert-butyl carbazate and its transformation into 3-benzylidene and 1-amino derivatives are described. Its crystal structure is presented showing it to be an
Development of orally bioavailable bicyclic pyrazolones as inhibitors of tumor necrosis factor-α production
Clark, Michael P.,Laughlin, Steven K.,Laufersweiler, Matthew J.,Bookland, Roger G.,Brugel, Todd A.,Golebiowski, Adam,Sabat, Mark P.,Townes, Jennifer A.,VanRens, John C.,Djung, Jane F.,Natchus, Michael G.,De, Biswanath,Hsieh, Lily C.,Xu, Susan C.,Walter, Rick L.,Mekel, Marlene J.,Heitmeyer, Sandra A.,Brown, Kimberly K.,Juergens, Karen,Taiwo, Yetunde O.,Janusz, Michael J.
, p. 2724 - 2727 (2007/10/03)
2-Aryl-3-pyrimidinyl based tumor necrosis factor-α (TNF-α) inhibitors, which contain a novel bicyclic pyrazolone core, are described. Many showed low-nanomolar activity against lipopolysaccharide-induced TNF-α production in monocytic cells. Secondary scre
Novel compounds and therapeutic uses thereof
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Page 25, (2010/02/03)
The invention discloses a novel series of compound represented by general formula (I), its derivatives, analogs, tautomeric forms, stereoisomers, polymorphs, pharmaceutically acceptable salts, solvates wherein X, n, k, z, R1, R2, R3, R4, R5 and R6 are as defined in the specification that are useful in (i) normalizing elevated blood glucose levels in diabetes, (ii) treating disorders related to glucose intolerance and (iii) for scavenging free radicals of mammals. The invention also discloses pharmaceutically acceptable composition comprising these compounds, method for preparation of the compounds as defined above and method of treating mammals including human beings by administering an effective amount of said compounds to a subject in need thereof. The invention further discloses use of these compounds in the manufacture of a medicament useful for treatment of different disease conditions as stated above.
Synthesis, molecular modeling and biological evaluation of aza-proline and aza-pipecolic derivatives as FKBP12 ligands and their in vivo neuroprotective effects
Wilkinson, Douglas E.,Thomas IV, Bert E.,Limburg, David C.,Holmes, Agnes,Sauer, Hansjorg,Ross, Douglas T.,Soni, Raj,Chen, Yi,Guo, Hong,Howorth, Pamela,Valentine, Heather,Spicer, Dawn,Fuller, Mike,Steiner, Joseph P.,Hamilton, Gregory S.,Wu, Yong-Qian
, p. 4815 - 4825 (2007/10/03)
Nonimmunosuppressant ligands, exemplified by GPI 1046 (1), for the peptidyl-prolyl isomerase FKBP12 have been found to unexpectedly possess powerful neuroprotective and neuroregenerative effects in vitro and in vivo. We have extensively explored the thera
Cyclic dibenzoylhydrazines reproducing the conformation of ecdysone agonists, RH-5849
Toya, Tetsuya,Yamaguchi, Kentaro,Endo, Yasuyuki
, p. 953 - 961 (2007/10/03)
We have investigated the biologically active conformation of the non-steroidal ecdysone agonist, 1-tert-butyl-1,2-dibenzoylhydrazine (RH-5849) by means of design, synthesis and conformational analysis of cyclic derivatives of RH-5849. Among the synthesize
Synthesis and conformational preferences in solution and crystalline states of an aza-tripeptide
Hemmerlin, Christine,Cung, Manh Thong,Boussard, Guy
, p. 5009 - 5012 (2007/10/03)
The aza-tripeptide Boc-Ala-AzPip-Ala-NHiPr (AzPip: 2-aza pipecolyl residue) was synthesized in seven steps using preferentially the diisopropylcarbodiimide/1-hydroxy-7-aza-benzotriazole (DIPCDI/AtOH) coupling method and via the Boc-AzPip-OBzl pivotal inte
Azapeptide acids as cell adhesion inhibitors
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, (2008/06/13)
Azapeptide acids of Formula I are antagonists of VLA-4 and/or alpha 4 beta 7, and as such are useful in the inhibition or prevention of cell adhesion and cell-adhesion mediated pathologies. These compounds may be formulated into pharmaceutical composition
Quinaldoyl-amine derivatives of oxo-and hydroxy-substituted hydrocarbons
-
, (2008/06/13)
The present invention discloses the compounds of general formula (1) STR1 wherein R1, R2, R3 are optionally substituted carbonyl and amide derivatives which are useful as inhibitors of retroviral proteases, and are effecti
