87341-45-5Relevant academic research and scientific papers
Phenotypic Screening of Chemical Libraries Enriched by Molecular Docking to Multiple Targets Selected from Glioblastoma Genomic Data
Aryal, Uma K.,Bailey, Barbara J.,Bum-Erdene, Khuchtumur,Corson, Timothy W.,Fishel, Melissa L.,Lee, Jonathan A.,Liu, Sheng,Meroueh, Samy O.,Pollok, Karen E.,Sishtla, Kamakshi,Wan, Jun,Wells, Clark D.,Xu, David,Zhou, Donghui
, p. 1424 - 1444 (2020/07/15)
Like most solid tumors, glioblastoma multiforme (GBM) harbors multiple overexpressed and mutated genes that affect several signaling pathways. Suppressing tumor growth of solid tumors like GBM without toxicity may be achieved by small molecules that selec
ANTIVIRAL COMPOUNDS
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Paragraph 0718; 0729, (2018/04/13)
The present invention relates to novel compounds of general formula (I) wherein the groups X, and R1 to R4 have the meanings given in the description and claims, process for preparing these compounds and their use as for treating, preventing or ameliorating viral infections and their use for treating, preventing or ameliorating diseases which are associated with PLA2G16.
Synthesis and identification of chiral aminomethylpiperidine carboxamides as inhibitor of collagen induced platelet activation
Anil Kumar,Misra, Ankita,Siddiqi, Tanveer Irshad,Srivastava, Stuti,Jain, Manish,Bhatta, Rabi Sankar,Barthwal, Manoj,Dikshit, Madhu,Dikshit, Dinesh K.
, p. 456 - 472 (2014/06/09)
A series of chiral lactam carboxamides of aminomethylpiperidine were synthesized and investigated for the collagen induced in vitro anti-platelet efficacy and collagen plus epinephrine induced in vivo pulmonary thromboembolism. The compound 31a (30 μM/kg) displayed a remarkable antithrombotic efficacy (60% protection) which was sustained for more than 24 h and points to its excellent bioavailability. The compounds 31a (IC50 = 6.6 μM) and 32a (IC50 = 37 μM), as well as their racemic mixture 28i (IC50 = 16 μM) significantly inhibited collagen-induced human platelet aggregation in vitro. Compound 34c displayed dual mechanism of action against both collagen (IC50 = 3.3 μM) and U46619 (IC50 = 2.7 μM) induced platelet aggregation. The pharmacokinetic study of 31a indicated very faster absorption, prolonged and constant systemic exposure and thereby exhibiting better therapeutic response.
CHIRAL 1-(4-METHYLPHENYLMETHYL)-5-OXO-{N-[(3-T-BUTOXYCARBONYL- AMINOMETHYL)]-PIPERIDIN-1-YL}-PYRROLIDINE-2-CARBOXAMIDES AS INHIBITORS OF COLLAGEN INDUCED PLATELET ACTIVATION AND ADHESION
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Page/Page column 16, (2012/08/27)
Chiral l-(4-methylphenylmethyl)-5-oxo-{N-[(3-t-butoxycarbonyl-aminomethyl)]- piperidin-l-yl}-pyrrolidine-2-carboxamides as inhibitors of collagen induced platelet activation and adhesion The present invention provides chiral (2S)-l-(4-methylphenylmethyl)-5-oxo-(3S)-{N-[(3-t- butoxycarbonyl aminomethyl)]-piperidin-l-yl}-pyrrolidine-2-carboxamide, and (2S)-1-(4- methylphenylmethyl)-5-oxo-(3R)-{N-[(3-t-butoxycarbonyl amino methyl)]-piperidin-l-yl}- pyrrolidine-2-carboxamide of formula 6 and 7 respectively. The present invention also relates to use of these moieties as inhibitors of collagen induced platelet adhesion and aggregation mediated through collagen receptors. The present invention provides a process for preparation of chiral carboxamides of formula 6 and 7 using the process which has advantage to avoid any racemization at the a-carboxylic center, during N-alkylation. The reagent LiHMDS is used at low temperatures to furnish methyl N-(p- methylphenylmethyl)lpyroglutamate in good chiral purity.
The improved synthesis of enantiopure (s)-N-arylmethyl-5-oxoprolines
Marchalin, Stefan,Kadlecikova, Katarina,Bar, Nathalie,Decroix, Bernard
, p. 3619 - 3624 (2007/10/03)
A mild procedure for the preparation of enantiopure N-alkylated (S)- (+)-5-oxoprolines 3a-r is described. The method starting from (S)-glutamic acid appears generally applicable to substrates with a wide range of substituents.
