Dardari Zainaba, Lemrani Meryem, Sebban Abdelfatah, Bahloul Abdelmejid, Hassar Mohammed, Kitane Said, Berrada Mohammed, Boudouma Mohammed
Laboratoire de Microbiologie et Biologie Moléculaire, Département de Biologie, Faculté des Sciences Ben M'sik-Casablanca, Université Hassan Il-Mohammedia, Casablanca, Morocco.
Arch Pharm (Weinheim). 2006 Jun;339(6):291-8. doi: 10.1002/ardp.200500266.
Here, we report for the first time the synthesis and the antileishmanial activity of a new pyrazole derivative, namely 4-[2-(1-(ethylamino)-2-methylpropyl)phenyl]-3-(4-methyphenyl)-1-phenylpyrazole). Micromolar concentrations of this compound were found to inhibit the in vitro multiplication of Leishmania tropica, Leishmania major, and Leishmania infantum, three species causing different forms of leishmaniasis. Furthermore, the 50% inhibitory concentration (IC50) values for the compound are only slightly higher than those of amphotericin B, one of the most active antileishmanial agents used as a satisfactory substitute in cases not responding to pentostam. The IC50 values after 48 h for L. tropica, L. major, and L. infantum promastigote growth were 0.48 microg/mL, 0.63 microg/mL and 0.40 microg/mL, respectively for the compound, while they were 0.23 microg/mL, 0.29 microg/mL and 0.24 microg/mL, respectively for amphotericin B. We also tested this compound for its antibacterial activity against several bacteria. The strongest antibacterial activity was observed against Entrococcus feacalis and Staphylococcus aureus with a minimal inhibitory concentration (MIC) of 60 microg/mL.
在此,我们首次报告了一种新型吡唑衍生物,即4-[2-(1-(乙氨基)-2-甲基丙基)苯基]-3-(4-甲基苯基)-1-苯基吡唑的合成及其抗利什曼原虫活性。发现该化合物的微摩尔浓度可抑制热带利什曼原虫、硕大利什曼原虫和婴儿利什曼原虫这三种导致不同形式利什曼病的寄生虫在体外的增殖。此外,该化合物的50%抑制浓度(IC50)值仅略高于两性霉素B,两性霉素B是在对喷他脒无反应的病例中用作满意替代药物的最有效的抗利什曼原虫药物之一。该化合物作用48小时后,对热带利什曼原虫、硕大利什曼原虫和婴儿利什曼原虫前鞭毛体生长的IC50值分别为0.48微克/毫升、0.63微克/毫升和0.40微克/毫升,而两性霉素B的IC50值分别为0.23微克/毫升、0.29微克/毫升和0.24微克/毫升。我们还测试了该化合物对几种细菌的抗菌活性。观察到对粪肠球菌和金黄色葡萄球菌的抗菌活性最强,最低抑菌浓度(MIC)为60微克/毫升。