- IMIDAZOLINE DERIVATIVES AS CXCR4 MODULATORS
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The present invention provides novel compounds of formula (I) and pharmaceutical compositions containing these compounds. The compounds of formula (I) can act as CXCR4 modulators that specifically target the CXCR4 minor pocket, and they have further been
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Page/Page column 91; 102; 103
(2020/10/19)
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- USE OF CASEINOLYTIC PROTEASE P FUNCTION AS A BIOMARKER OF DRUG RESPONSE TO IMIPRIDONE-LIKE AGENTS
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Use of caseinolytic protease P (ClpP) function and/or concentration as a biomarker for predicting the response of a neoplastic disease, preferably cancer or another disease where enhancing ClpP activity may provide a therapeutic benefit, to a compound of Formula I. In other aspects it relates to methods and kits, as well as methods of treatment involving the use of the biomarker.
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Page/Page column 125
(2020/09/12)
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- Discovery of Benzylidene Derivatives as Potent Syk Inhibitors: Synthesis, SAR Analysis, and Biological Evaluation
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Four scaffolds of varied benzylidene derivatives were synthesized and evaluated as Syk inhibitors for the treatment of rheumatoid arthritis (RA). Among these 31 compounds, 3-benzylidene pyrrolidine-2,5-dione derivatives (including 12k) universally showed good Syk inhibitory activities in the low micromolar to submicromolar range. In the cellular profiling, compound 12k, the most efficient compound, showed excellent antiproliferative activity against fibroblast-like synoviocytes (FLS)-RA, and demonstrated potencies for suppression of IL-6 and MMP-3 secretion almost equal to R406 (positive control). The oral efficacy of 12k in the murine collagen-induced arthritis model was significant, despite being weaker than R406. Taken together, all preliminary pharmacological results supported 12k as a potential small-molecule inhibitor targeting Syk for the treatment of RA.
- Zhang, Lingling,Liu, Wei,Mao, Fei,Zhu, Jin,Dong, Guoqiang,Jiang, Hualiang,Sheng, Chunquan,Miao, Liyan,Huang, Lixin,Li, Jian
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p. 463 - 474
(2015/07/07)
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- Potent antimalarial activity of 2-aminopyridinium salts, amidines, and guanidines
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We describe the design, synthesis, and antimalarial activity of 60 bis-tertiary amine, bis-2(1H)-imino-heterocycle, bis-amidine, and bis-guanidine series. Bis-tertiary amines with a linker from 12 to 16 methylene groups were active against the in vitro growth of Plasmodium falciparum within the 10 -6-10-7 M concentration range. IC50 decreased by 2 orders of magnitude for bis-2-aminopyridinium salts, bis-amidines, and bis-guanidines (27 compounds with IC50 a over 12.5. Maximal activity occurs for bis-2-aminopyridinium, two C-duplicated bis-amidines, and three bis-guanidines, with IC50 values lower than 1 nM. In comparison to similar quaternary ammonium salts, amidinium compounds have distinct structural requirements for antimalarial activity and likely additional binding opportunities on account of their hydrogen-bond-forming properties.
- Calas, Michèle,Ouattara, Mahama,Piquet, Gilles,Ziora, Zyta,Bordat,Ancelin, Marie L.,Escale, Roger,Vial, Henri
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p. 6307 - 6315
(2008/09/16)
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- Compounds with antiparasitic activity and medicines containing same
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The invention relates to compounds having an anti-parasitic, in particular antimalarial activity, characterized in that they correspond to general formula (I) Applications in particular as compounds with anti-parasitic activity.
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Page/Page column 8
(2008/06/13)
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- Solution parallel synthesis of cyclic guanidines
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An efficient method for the solution phase synthesis of cyclic guanidines is presented. A variety of 2-substituted monoprotected propanediamines react with a set of 5-substituted 2-methylthio-3,4,5,6- tetrahydropyrimidines under Rathke conditions for the construction of a potential library of 81 cyclic guanidines.
- Marmillon, Christelle,Bompart, Jacques,Calas, Michèle,Escale, Roger,Bonnet, Pierre-Antoine
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p. 1317 - 1328
(2007/10/03)
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- 1,5-Bis substituted-1,4-pentadien-3-one substituted amidino hydrazone salts and method of preparing the same
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The preparation of 1,5-bis-substituted-1,4-pentadien-3-one, substituted amidinohydrazone salts are described. They are prepared by the reaction of a 1,5-bis(substituted)-1,4-pentadiene-3-one with a substituted aminoguanidine salt. These compounds are useful as anti-malarial and anti-tubercular agents in warm-blooded animals.
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