98412-23-8Relevant articles and documents
Ultrasound improves the synthesis of 5-hydroxymethyl-2-mercapto-1-benzylimidazole as a base compound of some pharmaceutical products
Entezari, Mohammad H.,Asghari, Azam
, p. 2835 - 2839 (2008)
Application of ultrasound in synthesis appears to be a promising alternative for high-value chemicals and pharmaceuticals. This work describes the results of investigations carried out towards the synthesis of 5-hydroxymethyl-2-mercapto-1-benzylimidazole (HMMBI) in the presence of ultrasound (sono-synthetic) and in the absence of ultrasound (control method). Instead of mixing for long time in control method, the mixture was sonicated indirectly with 500 kHz and directly with 20 kHz apparatus. In some experiments the yield of the reaction was optimized by suitable manipulation of conditions such as temperature, vapor pressure of the solvent, ultrasonic intensity, and contact time. In control method, the yield of the reaction was increased by increasing the temperature but in sono-synthetic method, the thermal dependency was different in the range of temperature studied (7-25 °C). Kinetic results at 7 °C indicate that the yield of the reaction was reached to 90% after half an hour sonication but in control method it was reached to 70% after 72 h under the same conditions. Therefore, it is possible to reach a high yield of product under proper conditions of sonication.
Design, synthesis and biological evaluation of novel 5-(imidazolyl-methyl) thiazolidinediones as antidiabetic agents
Shakour, Neda,Sahebkar, Amirhossein,Karimi, Gholamreza,Paseban, Maryam,Tasbandi, Aida,Mosaffa, Fatemeh,Tayarani-Najaran, Zahra,Ghodsi, Razieh,Hadizadeh, Farzin
, (2021/07/28)
A newly designed series of imidazolyl-methyl- l-2,4-thiazolidinediones 9 (a-m) were synthesized and In Silico studies were carried out to rationalize their anti-diabetic activity. Generally, all newly synthesized thiazolidinediones had anti-hyperglycemic activity compared with a diabetic-control group, without toxicity in 3T3 cells (viability ≥ 90%). These studies revealed that the compounds 9e and 9b (11?10-6mol/kg) lowered blood glucose more effectively when compared to pioglitazone at the same dose. Following the administration of compound 9e, no weight gains or any serious side effects on liver and pancreas were observed. Moreover, the glucose consumption assay results showed a significant glucose-lowering effect (p 0.001) in HepG2 cells, which were exposed to 11 mM of glucose at concentrations of 1.25–10 mM of compound 9e. Also, the PPAR-γ gene expression study revealed that pioglitazone and 9e showed similar behavior relative to the control group.
AZOLE HETEROCYCLIC COMPOUND, PREPARATION METHOD, PHARMACEUTICAL COMPOSITION AND USE
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Paragraph 0242, (2014/05/20)
The present invention relates to the filed of pharmarcutical chemistry, and in particular, to a novel class of azole compounds represented by general formula (I), (II) or (III) amd a preparation method thereof, a pharmarcutical composition with the compounds as active components, and a use of the azole compounds and the pharmarcutical composition in the preparation of a medicament for treatment of diseases associated with Lp-PLA2 enzyme activities, wherein each substituent is as deinfed in the specifictaion.
