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Hajjaj H. M. Abdu-Allah,Bahaa G. M. Youssif,Mostafa H. Abdelrahman,Mohammed K. Abdel-Hamid,Rudraraju Srilakshmi Reshma,Perumal Yogeeswari,Tarek Aboul-Fadl,Dharmarajan Sriram 대한약학회 2017 Archives of Pharmacal Research Vol.40 No.2
The antitubercular drug; para-aminosalicylicacid (PAS) was used as the core scaffold for the design of aseries of 1H-1,2,3-triazolylsalicylhydrazones upon couplingwith triazole and arylhydrazone moietis to furnish asingle molecular architecture. The obtained derivativeswere screened against Mycobacterium tuberculosis H37Rvrevealing good to high activity for the active compounds(MIC values of 0.39–1.5 lg/mL) compared to the marketeddrugs isoniazid, rifampicin and ethambutol. Moreover, themost active analogue N-(1-(4-chlorobenzyl)-2-oxoindolin-3-ylidene)-2-hydroxy-4-(4-phenyl-1H-1,2,3-triazol-1-yl)-benzohydrazide (20) was found to be ten-fold more potentthan PAS and equipotent to rifampicin (MIC 0.39 lg/mL),while exhibiting low cytotoxicity with a selectivity indexof[128. In addition, this compound was shown to beactive against persistent forms of mycobacteria comparableto standard drugs in nutrient starvation model. Accordingly,we introduce compound 20 as a valuable lead forfurther development. A 3D-QSAR study was also conductedto help in explaining the observed activity and toserve as a tool for further development.
Amal T. Abou Elghait,Tarek. M. Mostafa,Fatma K. Gameaa,Gamal K. Mohammed,Fatma Y. Meligy,Manal M. Sayed 대한해부학회 2022 Anatomy & Cell Biology Vol.55 No.3
As a synthetic analog of codeine, tramadol is often prescribed to treat mild to moderate pains. This study was designed to estimate and compare the histological effect of tramadol on testes of both juvenile and adult male albino mice. A total number of 40 healthy male albino mice were classified into two main groups as follows: group I (juvenile group, includes 20 mice aged three weeks) subdivided equally into group Ia (control group received isotonic saline) and group Ib (tramadol-treated group received 40 mg/kg/d tramadol orally for 30 days); group II (adult group, includes 20 mice aged two months) subdivided equally into group IIa (control group received isotonic saline) and group IIb (tramadol-treated group). Juvenile and adult tramadol-treated groups showed numerous testicular changes, including blood vessels congestion, widening of intercellular spaces, vacuolization in interstitial tissues, luminal germ cells exfoliation, and increased expression of caspase-3 that indicated cellular apoptosis. In the ultrastructural examination, spermatogenic cells degenerated with the frequent appearance of apoptotic cells. Sertoli cells showed vacuolations, large lipid droplets, and disrupted intercellular cell junctions. These observed testicular changes were markedly observed in the juvenile group. Testicular abnormalities and apoptotic changes can be caused by tramadol administration. These abnormalities are more common in juvenile mice.