Insight into the bioreductive mode of action of antitrypanosomal 5-nitrofuryl containing thiosemicarbazones.
نویسندگان
چکیده
In order to get insight into the trypanocidal mechanism of action of a series of 5-nitrofuryl containing thiosemicarbazones some studies related to their bioreduction were performed. Electron spin resonance spectra of radicals generated in T. cruzi by compounds' bioreduction were analyzed. Three different patterns of ESR signals were observed for the different assayed compounds. These results were in agreement with the changes in the T. cruzi-oxygen uptake promoted by these compounds. On the other hand, free-radical scavenger properties, measured as oxygen radical absorbance capacity (ORAC), did not seem to correlate with the trypanocidal activity.
منابع مشابه
Thiosemicarbazones active against Clostridium difficile.
A set of closely related furylidene thiosemicarbazones was prepared and screened against various clinically important Gram-positive bacteria. One compound containing an ethylene spacer and a 5-nitrofuryl group was found to have promising activity against Clostridium difficile.
متن کاملAntitrypanasomal activity of novel benzaldehyde-thiosemicarbazone derivatives from kaurenoic acid.
A series of new thiosemicarbazones derived from natural diterpene kaurenoic acid were synthesized and tested against the epimastigote forms of Trypanosoma cruzi to evaluate their antitrypanosomal potential. Seven of the synthesized thiosemicarbazones were more active than kaurenoic acid with IC₅₀ values between 2-24.0 mM. The o-nitro-benzaldehyde-thiosemicarbazone derivative was the most active...
متن کاملStructural and antitrypanosomal data of different carbasones of piperitone
This article reports data on four carbazones of piperitone: semicarbazone 1, thiosemicarbazone 2, 4-phenyl semicarbazone 3 and 4-phenyl thiosemicarbazone 4 prepared directly in situ from essential oil of Cymbopogon schoenantus, whose GC-FID and GC-MS analysis revealed piperitone as major component (68.20%). The structures of hemi-synthesized compounds were confirmed by high throughput IR, MS, 1...
متن کاملMolecular features for antitrypanosomal activity of thiosemicarbazones revealed by OPS-PLS QSAR studies.
A quantitative structure-activity relationship analysis was employed to explore the relationship between the molecular structure of thiosemicarbazone analogues and the inhibition of the cysteine protease cruzain, a validated target for Chagas' disease treatment. A data set containing 53 thiosemicarbazone derivatives was used to produce a quantitative model for activity prediction of unknown com...
متن کاملEffects of Cryptolepine, 2, 7, dibromocryptolepine and standard drugs on hemoglobin accumulation in cultured Malaria parasites
Cryptolepine is the major alkaloidal constituent of the West African climbing shrub Cryptolepis sanguinolenta, a species used in traditional medicine for the treatment of malaria and a number of other infectious diseases. Cryptolepine and a number of its synthetic analogues have been shown to have potent antiplasmodial activities using P. falciparum lactate dehydrogenase assay (PfLDH). Intraery...
متن کاملذخیره در منابع من
با ذخیره ی این منبع در منابع من، دسترسی به آن را برای استفاده های بعدی آسان تر کنید
برای دانلود متن کامل این مقاله و بیش از 32 میلیون مقاله دیگر ابتدا ثبت نام کنید
ثبت ناماگر عضو سایت هستید لطفا وارد حساب کاربری خود شوید
ورودعنوان ژورنال:
- Medicinal chemistry (Shariqah (United Arab Emirates))
دوره 4 1 شماره
صفحات -
تاریخ انتشار 2008