Tetrahydrophthalazinone Inhibitor of Phosphodiesterase with In Vitro Activity against Intracellular Trypanosomatids
نویسندگان
چکیده
The phosphodiesterase inhibitor tetrahydrophthalazinone NPD-008 was explored by phenotypic in vitro screening, target validation, and ultrastructural approaches against Trypanosoma cruzi . displayed activity different forms strains of T. (50% effective concentration [EC 50 ], 6.6 to 39.5 μM). Increased cAMP levels its combination with benznidazole gave synergistic interaction.
منابع مشابه
In vitro activity of clarithromycin against intracellular Helicobacter pylori.
The in vitro intracellular effect of clarithromycin, amoxicillin, metronidazole, lansoprazole, and rifabutin, tested at concentrations corresponding to one times the MIC, two times the MIC, and four times the MIC, was evaluated against an invasive Helicobacter pylori strain. At four times the MIC, clarithromycin showed an early bactericidal effect within 4 h of incubation and, in determining th...
متن کاملP-108: Effect of Phosphodiesterase Type 3 Inhibitor on Nuclear Maturation and In Vitro Development of Ovine Oocytes
Background: Present study aims to investigate if PMC of ovine oocytes in the presence of cilostamide a phosphodiesterase type 3 (PDE3) inhibitor can improve the shortcomings of conventional IVM system. Materials and Methods: Immature ovine oocytes were retrieved from pre antral follicles of abattoir ovaries by aspiration and after washing in Htcm + %10 FBS were immediately classified in four gr...
متن کاملPhosphodiesterase 3/4 Inhibitor Zardaverine Exhibits Potent and Selective Antitumor Activity against Hepatocellular Carcinoma Both In Vitro and In Vivo Independently of Phosphodiesterase Inhibition
Hepatocellular carcinoma (HCC) is the fifth common malignancy worldwide and the third leading cause of cancer-related death. Targeted therapies for HCC are being extensively developed with the limited success of sorafinib. In the present study, we investigated the potential antitumor activity of zardaverine, a dual-selective phosphodiesterase (PDE) 3/4 inhibitor in HCC cells both in vitro and i...
متن کاملIn-vitro Antimycoplasmal Activity of Triclosan in Combination with Fluoroquinolones against Five mycoplasma Species
Mycoplasmosis caused by mycoplasma has immensely reduced the performance of commercial animal husbandry, along with prevalence and increase of drug resistance in mycoplasma, thus new agents and therapies are urgently needed. Triclosan is a broad spectrum antimicrobial agent with a favorable safety profile. In the present study, we tested the antimycoplasmal activity of triclosan alone, as well ...
متن کاملIn-vitro Antimycoplasmal Activity of Triclosan in Combination with Fluoroquinolones against Five mycoplasma Species
Mycoplasmosis caused by mycoplasma has immensely reduced the performance of commercial animal husbandry, along with prevalence and increase of drug resistance in mycoplasma, thus new agents and therapies are urgently needed. Triclosan is a broad spectrum antimicrobial agent with a favorable safety profile. In the present study, we tested the antimycoplasmal activity of triclosan alone, as well ...
متن کاملذخیره در منابع من
با ذخیره ی این منبع در منابع من، دسترسی به آن را برای استفاده های بعدی آسان تر کنید
ژورنال
عنوان ژورنال: Antimicrobial Agents and Chemotherapy
سال: 2021
ISSN: ['0066-4804', '1070-6283', '1098-6596']
DOI: https://doi.org/10.1128/aac.00960-20