1457-59-6Relevant articles and documents
Synthesis and in vivo lipid-lowering activity of novel imidazoles-5-carboxamide derivatives in Triton-WR-1339-induced hyperlipidemic wistar rats
Jasim, Suhair H.,Sheikha, Ghassan M. Abu,Abuzaid, Haneen M.,Al-Qirim, Tariq M.,Shattat, Ghassan F.,Sabbah, Dima A.,Ala, Samah A.,Aboumair, Mustafa S.,Sweidan, Kamal A.,Bkhaitan, Majdi M.
, p. 953 - 958 (2018)
A new series of imidazole-5-carboxamide derivatives were prepared and tested for their anti-hyperlipidemic activity in Triton-WR-1339-induced hyperlipidemic Wistar rats. The purpose of this research was to improve benzophenone carboxamides water solubility maintaining at the same time the antihyperlipidemic activity. Compounds 4, 6, 10, and 11 were synthesized through a coupling reaction between imidazoles-5-carbonyl chloride and amino benzophenones. The tested animals (n=48) were divided into six groups: The first group (hyperlipidemic control group; HCG) received an intraperitoneal injection (i.p.) of (300 mg/kg) Triton WR-1339. The second group received i.p. injection of Triton WR-1339 followed by an intra-gastric administration of bezafibrate (100 mg/kg) (bezafibrate; BF). The third, fourth, fifth, and sixth groups received i.p. injection of Triton WR-1339 followed by an intra-gastric administration of (30 mg/kg) of compounds 4, 6, 10, and 11, respectively. At a dose of 30 mg/kg body weight compounds 4, 6, 10, and 11 significantly (p0.0001) decreased the plasma level of triglyceride (TG), low-density lipoprotein (LDL) and total cholesterol (TC) levels after 18 h of treatment. Additionally, compounds 4, 6, 11 and bezafibrate (100 mg/kg) significantly (p0.0001) increased the plasma level of high-density lipoprotein (HDL) levels, which is known for its preventive role against atherogenesis. These results demonstrate the possibility of pharmacokinetic properties improvement maintaining the biological and pharmacological profile of these compounds.
Quinoline-based compound and selective androgen receptor agonist comprising the same
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Paragraph 0297-0299, (2016/10/08)
Provided are a novel quinoline-based compound, a pharmaceutical composition containing the quinoline-based compound, and a method for producing the quinoline-based compound. The quinoline-based compound acts on an androgen receptor to increase activities of the androgen receptor, and thus can be favorably used as an agent for treating and preventing diseases or conditions, in which the increased activities of the androgen can lead to improvement of symptoms or the responsiveness to treatment, for example, various hormone-related diseases of the male or female, muscle-wasting disease, osteoporosis, and the like.COPYRIGHT KIPO 2016
Pd/C and NaBH4 in basic aqueous alcohol: An efficient system for an environmentally benign oxidation of alcohols
An, Gwangil,Ahn, Hyunseok,De Castro, Kathlia A.,Rhee, Hakjune
experimental part, p. 477 - 485 (2010/06/13)
We report the oxidation of a wide range of alcohols using an environmentally benign and economical process. The use of Pd/C heterogeneous catalysts along with NaBH4in aqueous ethanol or methanol and either K2CO3 or KOH as base at room temperature under molecular oxygen or air give the corresponding oxidation products. This protocol is versatile since it is capable of oxidizing alcohols to its desired carbonyl or carboxyl counterpart. Room temperature reaction in aqueous system and recyclability of the catalyst are among the advantages of this manipulation. These advantages make the process safe and cheaper rendering it favorable from both economic and environmental viewpoints. Georg Thieme Verlag Stuttgart New York.