- Synthesis and in vivo lipid-lowering activity of novel imidazoles-5-carboxamide derivatives in Triton-WR-1339-induced hyperlipidemic wistar rats
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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.
- 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.
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Read Online
- Bromine structural domain inhibitor compound and application thereof
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The invention relates to a bromine structural domain inhibitor and provides a compound shown in a general formula I, pharmaceutical salt, an enantiomer, a diastereoisomer, an atropisomer, racemate, apolymorphic substance and solvate of the compound or an isotope labelled compound (including a deuterium substituted compound), a preparation method of the compound, pharmaceutical composition containing the compound and an application of the above components in pharmaceuticals.
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Paragraph 0143-0146
(2019/08/02)
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- Quinoline-based compound and selective androgen receptor agonist comprising the same
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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
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Paragraph 0297-0299
(2016/10/08)
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- Study of direction of cyclization of 1-azolil-4-aryl/alkyl- thiosemicarbazides
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On a four series of 1-azolil-4-aryl/alkyl-thiosemicabazides, a study on the influence of azole moiety on the capability for intramolecular cyclization and its direction was carried out. It was found that for 4-aryl/alkyl- thiosemicabazides with triazole, imidazole, or pyrrole moiety at N-1 nitrogen atom possible products were only s-triazoles, both in alkaline and acidic medium. Successful dehydrocyclization of 1-azolil-4-aryl/alkyl- thiosemicarbazides leading to a thiadiazole has been documented only for a series of 1-(4-methyl-1,2,3-thiadiazol-5-yl-carbonyl)-4-aryl/alkyl- thiosemicarbazides. It can be speculative that the determination of pK a value of oxygen atom of 1-azolil-4-aryl/alkyl-thiosemicarbazide can be a very valuable parameter in the prediction of the possibility of dehydrocyclization to form thiadiazole.
- Siwek, Agata,Wujec, Monika,Dobosz, Maria,Wawrzycka-Gorczyca, Irena
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p. 521 - 532
(2011/08/03)
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- Pd/C and NaBH4 in basic aqueous alcohol: An efficient system for an environmentally benign oxidation of alcohols
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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.
- An, Gwangil,Ahn, Hyunseok,De Castro, Kathlia A.,Rhee, Hakjune
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experimental part
p. 477 - 485
(2010/06/13)
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- Environmentally benign oxidation reaction of aldehydes to their corresponding carboxylic acids using Pd/C with NaBH4 and KOH
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Pd/C catalyst in aqueous methanol with sodium borohydride and potassium hydroxide under the air efficiently oxidized aldehydes to their corresponding carboxylic acids at room temperature. The utilization of room temperature reaction, aqueous methanol solvent, and the open-air conditions make this manipulation very interesting for economic and environmental perspectives.
- Lim, Minkyung,Yoon, Cheol Min,An, Gwangil,Rhee, Hakjune
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p. 3835 - 3839
(2008/02/07)
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- INHIBITORS OF AKT ACTIVITY
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The instant invention provides for substituted naphthyridine compounds that inhibit Akt activity. In particular, the compounds disclosed selectively inhibit one or two of the Akt isoforms. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting Akt activity by administering the compound to a patient in need of treatment of cancer.
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Page/Page column 140
(2010/11/25)
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- Protease inhibitors
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The present invention provides compounds of formula (I) which inhibit proteases, including cathepsin K, pharmaceutical compositions of such compounds, and methods for treating diseases of excessive bone loss or cartilage or matrix degradation, including osteoporosis; gingival disease including gingivitis and periodontitis; arthritis, more specifically, osteoarthritis and rheumatoid arthritis; Paget's disease; hypercalcemia or malignancy; and metabolic bone disease therewith.
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- Imidazole plant growth regulators
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Imidazoles of the following structural formula are plant growth regulators: STR1 wherein R4 is selected from the group consisting of --H, --lower alkyl, --NO2, --CN, and --CONHY; and R5 is selected from the group consistin
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