Synthesis and antibacterial activities of some 1-[2-(substituted pyrrol-1-yl)ethyl]-2-methyl-5-nitroimidazole derivatives

In this study, some 1-[2-(substituted pyrrol-1-yl)ethyl]-2-methyl-5-nitroimidazole derivatives were synthesized by reacting 2-(2-methyl-5-nitro-1H-imidazolyl)ethylamine dihydrochloride, which was prepared using metronidazole, with some 1,4-dicarbonyl compounds. The structure elucidation of the compounds was performed by IR, H-1-NMR and mass spectroscopic data and elemental analysis results. Antimicrobial activities of the compounds were examined and notable activity was obtained. (C) Elsevier, Paris

Synthesis of some 1-(2-arylvinyl)-3-arylpyrazino[1,2-a]benzimidazole derivatives and their antimicrobial activities

Some 1-(2-arylvinyl)-3-arylhyrazino[1,2-a] benzimidazole derivatives were synthesized, their structures were elucidated, and their antibacterial and antifungal activities were examined. None of the compounds proved to be sufficiently active

Synthesis and preliminary evaluation of new 5-pyrazolinone derivatives as analgesic agents

New 4-(aroyloxyalkanoyl)-2,3-dimethyl-1-phenyl-3-pyrazolin-5-ones (5) were cyclized to 4-(2-aryl-5-unsubstituted/substituted oxazol-4-yl)-2,3-dimethyl-1-phenyl-3-pyrazolin-5-ones (6) employing the Davidson procedure. Preliminary evaluation of analgesic activity revealed that the effect of 4-(2-phenyl-5-ethyloxazol-4-yl)-2,3-dimethyl-1-phenyl-3-pyrazolin-5-one and 4-[2-(4-chlorophenyl)-5-ethyloxazol-4-yl]-2,3-dimethyl-1-phenyl-3-pyrazoline-5-one on acetic acid induced writhing was superior to that of antypyrine and aminopyrine. 4-[2-(4-Chlorophenyl)-5-methyloxazol-4-yl]-2,3-dimethyl-1-phenyl-3-pyrazolin-5-one and 4-[2-(4-methoxyphenyl)-5-ethyloxazol-4-yl]-2,3- dimethyl-1-phenyl-3-pyrazolin-5-one were more potent than aminopyrine, whereas 4-(2-phenyl-5-methyloxazol-4-yl)-2,3-dimethyl-1-phenyl-3-pyrazolin-5-one and 4-[2-(4-methoxyphenyl)-5-methyl-oxazol-4-yl]-2,3-dimethyl-1-phenyl-3-pyrazolin-5-one were not as active (modified Koster's Test; 0.19-0.21 mmol.kg(-1)). None of the selected entries showed inhibition of formaldehyde-induced paw oedema. (C) 2000 Editions scientifiques et medicales Elsevier SAS

Uterine artery ligation at the beginning of total laparoscopic hysterectomy reduces total blood loss and operation duration

WOS: 000369867900014PubMed ID: 25517762The purpose of this study was to compare the feasibility, blood loss, duration of surgery and complications between patients in whom both uterine arteries were ligated by surgical clips and cut using a 5-mm ligature at the beginning of total laparoscopic hysterectomy (TLH) and patients in whom uterine arteries were not ligated at the beginning of TLH. In our prospective study, a total of 60 women underwent TLH. Uterine artery ligation (UAL) was done at the beginning of the procedure. Women were divided into TLH + UAL (n = 30) and TLH (n = 30) groups. In TLH group, TLH was done without ligating the uterine arteries at the beginning of the procedure. In TLH + UAL group, TLH was done with ligation of both uterine arteries at the beginning of the procedure. The mean operating time was longer for the TLH group (99.16 +/- 7.01) than TLH + UAL group (63.27 +/- 7.16). The median total blood loss was higher in TLH group (109.38 +/- 33.03 mL) than TLH + UAL group (47.50 +/- 8.12 mL). UAL at the beginning of TLH is a technically feasible procedure. It reduces the total blood loss and decreases the time taken for the procedure and length of hospital stay

Synthesis and antifungal activities of some aryl (3-methyl-benzofuran-2-yl) ketoximes

In this study, some aryl (3-methyl-benzofuran-2-yl) ketoximes and their. ethers and esters were synthesised. The structure elucidation of the compounds was performed by IR, H-1-NMR, MASS spectroscopy and elemental analyses. Antifungal activities of the compounds were examined and moderate activity was obtained

Platinum(II)-thiosemicarbazone drugs override the cell resistance due to glutathione; assessment of their activity against human adenocarcinoma cells

<p>New platinum(II) compounds of the thiosemicarbazone 1-(1H-Benzimidazol-2-yl)ethan-1-one thiosemicarbazone (BzimetTSCH), [Pt(BzimetTSCH)Cl]·2H₂O (<b>1</b>) and [Pt(BzimetTSCH)(tpp)]Cl·H₂O·MeCN (<b>2</b>) were synthesized. The complexes were characterized by FT-IR spectroscopy and ¹H NMR spectroscopy. The crystal structures of <b>1</b> and <b>2</b> were determined with single-crystal X-ray diffraction analysis. The coordination around platinum is square planar in both complexes. Compounds <b>1</b> and <b>2</b> were evaluated for their <i>in vitro</i> cytotoxic activity against human adenocarcinoma breast (MCF-7) and cervix (HeLa) cells. The apoptotic pathway of cell death was confirmed by cell cycle arrest test. Since deactivation of cisplatin caused by glutathione (GSH) seems to be an important determinant of its cytotoxic effects, the reactions of <b>1</b> and <b>2</b> with GSH were investigated by UV-absorption spectroscopy. The genotoxicities on normal human fetal lung fibroblast cells (MRC-5) caused by <b>1</b> and <b>2</b> were evaluated by fluorescence microscopy. The absence of micronucleus in MRC-5 cells confirms the <i>in vitro</i> non toxic behavior of the compounds. Moreover, the <i>in vivo</i> genotoxicities of <b>1</b> and <b>2</b> were evaluated by the <i>Allium cepa</i> test. Due to negligible genototoxic effect and high antitumor activity which is similar to that of cisplatin, <b>2</b> could be a candidate for further study as potential drug since the mitotic index is unchanged.</p

(1Z)-1-(1-Benzofuran-2-yl)ethanone oxime

The title compound, C10H9NO2, is almost planar (r.m.s. deviation for the non-H atoms = 0.027 Å) and the conformation across the C=N bond is syn. Further, the O atom of the benzofuran ring is syn to the CH3 group in the side chain. In the crystal, molecules are linked into C(3) chains propagating in [010] by O—H...N hydrogen bonds