74470-32-9Relevant academic research and scientific papers
Triazolothiadizepinylquinolines as potential MetAP-2 and NMT inhibitors: Microwave-assisted synthesis, pharmacological evaluation and molecular docking studies
Shaikh, Saba Kauser J.,Kamble, Ravindra R.,Bayannavar, Praveen K.,Somagond, Shilpa M.,Joshi, Shrinivas D.
, (2019/12/11)
The enzymes MetAP-2 and NMT play a crucial role in the process of myristoylation of oncoproteins which is deregulated in many types of cancers. Execution of both these enzymes is considered as strategy for the intervention of various cancers and relative fungal infections, and hence the discovery of novel MetAP-2 and NMT inhibitors necessitate their high relevancy. In this investigation, we have synthesized a series of novel seven-membered triazolothiadiazepinyl quinolines 10(a–m) distinctively under microwave irradiation technique and identified as selective MetAP-2 and NMT inhibitors. Amongst the functionalized derivatives when evaluated for the in vitro antifungal assay, compounds 10b, 10c, 10e and 10f were considered promising due to notable inhibitory effects (MIC = 0.2 mg/mL) on Aspergillus fumigatus. Screening of the anticancer activity against NCI-60 Human tumor cell lines portrayed that conjugates 10b, 10c, 10e and 10f were found to be moderately effective against the Renal Cancer cell line UO-31. The data acquired from biological studies was further validated by molecular docking studies and pharmacokinetic evaluation.
COMPOUNDS AND COMPOSITIONS FOR TREATING CONDITIONS ASSOCIATED WITH NLRP ACTIVITY
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Page/Page column 298-299, (2020/06/05)
In one aspect, compounds of Formula AA, or a pharmaceutically acceptable salt thereof, are featured or a pharmaceutically acceptable salt thereof, wherein the variables shown in Formula A can be as defined anywhere herein.
Nitrogen-containing fatty alcohol ester barium salt, and preparation method, composition and application thereof
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Paragraph 0029-0032, (2019/10/01)
The invention discloses a nitrogen-containing fatty alcohol ester barium salt, and a preparation method, a composition and an application thereof. The chemical formula of the nitrogen-containing fattyalcohol ester barium salt is Ba(C7H3O2NSR)2, and R is a C12-20 alkyl group. The barium salt belongs to a mercaptide, can act as an antioxidant, and can significantly improve the long-acting stabilityof PVC. The barium salt of the invention contains the nitrogen atom, a stabilizer formed by combining the barium salt with a nitrogen-containing zinc salt and an auxiliary stabilizer can obviously improve the thermal stability of the PVC, and the nitrogen-containing zinc has higher activity than common zinc carboxylate, and can fast absorb allyl chloride, significantly improve initial dyeing andprolong later zinc burning.
PEPTIDE MACROCYCLES AGAINST ACINETOBACTER BAUMANNII
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, (2017/06/01)
The present invention provides compounds of formula (I) wherein X1 to X8 and R1 to R8 are as described herein, as well as pharmaceutically acceptable salts thereof. Further the present invention is concerned with the manufacture of the compounds of formula (I), pharmaceutical compositions comprising them and their use as medicaments for the treatment of diseases and infections caused by Acinetobacter baumannii.
INDOLE DERIVATIVES AS LIGANDS OF CRTH2 RECEPTORS
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Page/Page column 24, (2010/12/29)
The following compounds are CRTH2 antagonists, useful in treatment of respiratory disease: {3-[3-chloro-4-(pyridine-2-sulfonyl)isothiazol-5-ylmethyl]-5-fluoro-2- methylindol-1-yl}acetic acid, [3-(5-benzenesulfonyl-3-methyl-3H-imidazol-4-ylmethyl)-5-fluoro
