161192-29-6Relevant articles and documents
Dual-acting diamine antiplasmodial and chloroquine resistance modulating agents
Yeh, Susan,Smith, Peter J.,Chibale, Kelly
, p. 156 - 165 (2006)
On the basis of structural features known to be critical for the antimalarial activity, accumulation and uptake of chloroquine (CQ), as well as chemosensitization of CQ resistant Plasmodium falciparum, an exploratory novel series of potential dual acting antiplasmodial and chemosensitizing agents was designed and synthesized for biological evaluation. All four compounds contain a common alkyl side chain with two amino groups and differ only in the chemical nature of the hydrophobic aromatic moieties. Among them, N′-[4-(biphenyl-2-ylmethoxy)-benzyl]-N,N-dimethyl-propane-1,3-diamine (P7) displayed the greatest potential as a dual-acting antiplasmodial agent against CQ-resistant strains (I C50K 1 / RSA 11 K1 = 0.67; RMIRSA11 = 0.82) while displaying low in vitro cytotoxicity against a mammalian cell line (CHO). At 1 μM, P7 caused a 8.5 and 4-fold potentiation in CQ accumulation in resistant P. falciparum K1 and RSA11 strains, respectively. In a parallel experiment, 1 μM verapamil showed a 6.5 (K1) and 2 (RSA11)-fold increase in CQ accumulation. The preliminary studies point to structural features that may determine antiplasmodial and/or CQ resistance modulating activity in this new series of compounds. An additive effect was observed against both CQS (D10) and CQR (RSA11) strains when CQ and P7 were used at their corresponding IC50 concentrations in isobologram analysis.
Phenolic compounds containing benzyloxy phenyl and preparation method and application of phenolic compounds
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Paragraph 0571-0575, (2017/09/19)
The invention discloses phenolic compounds (I) containing benzyloxy phenyl and a preparation method and application of the phenolic compounds. Pharmacological experiments prove that the phenolic compounds have high inhibiting activity on sphingosine kinase SphK, and part of the compounds has a certain inhibiting effect on inflammatory bowel disease induced by tumor and DSS. The phenolic compounds and the pharmaceutical preparations thereof can be used for preparing drugs for treating a series of cancer and inflammatory diseases such as colon cancer, lung cancer, breast cancer, liver cancer, stomach cancer, inflammatory bowel disease, hepatitis, asthma, chronic obstructive pulmonary disease, rheumatoid arthritis and multiple sclerosis.
Synthesis and analysis of anticonvulsant activities of new 4-[2-(4-alkoxybenzylamino)ethyl]-2H-1,2,4-triazol-3(4H)-one derivatives
Shen, Qing-Kun,Wang, Shi-Ben,Gong, Guo-Hua,Yin, Xiu-Mei,Quan, Zhe-Shan
, p. 430 - 438 (2015/06/22)
The present study involved the design and synthesis of new substituted 4-[2-(4-alkoxybenzylamino) ethyl]-2H-1,2,4-triazol-3(4H)-one derivatives (8a-w) starting from 1,2-ethanediamine. The final compounds were screened for their in vivo anticonvulsant activities and neurotoxicities by maximal electroshock (MES) and rotarod tests, respectively. Among the compounds studied, 4-[2-(4-butoxybenzylamino)ethyl]-2H-1,2,4-triazol-3(4H)-one hydrochloride (8b) was found by intraperitoneal administration in mice to be the most potent compound with a median effective dose (ED50) value of 33.2 mg/kg and a high protective index (PI) value of 11.4. Compound 8b showed significant oral activity against MES-induced seizures in mice with an ED50 value of 83.1 mg/kg and a PI of 18.1. The results demonstrated that compound 8b possessed better anticonvulsant activity and higher safety than the marketed drug carbamazepine.
