Improved detection of anthelmintic activity in an in vitro screen utilizing adult Nippostrongylus brasiliensis

Rapson, E. B.; Jenkins, D. C.; Chilwan, A. S.

doi:10.1007/bf00536481

Cited by 15 publications

(10 citation statements)

References 7 publications

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“…It can be used as a parameter for detecting new antiparasitic agents (Rapson et al 1986(Rapson et al , 1987Alonso-Villalobos and Martı´nez-Grueiro 2000) . When comparing in vitro effects of the tested compounds it appears that the secretion of AChE is a much more sensitive test than the release of AcP.…”

Section: Discussionmentioning

confidence: 99%

Nematocidal activity of nitazoxanide in laboratory models

Fonseca-Salamanca

Martı́nez-Grueiro

Martínez-Fernández

2003

Parasitology Research

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The nematocidal activity of a broad-spectrum antiparasitic agent, nitazoxanide [( N-(5-nitrothiazol-2-gammal)salicylamide; NTZ], was evaluated in both in vitro and in vivo models using Caenorhabditis elegans, Heligmosomoides polygyrus and Trichinella spiralis. In vitro, NTZ (100 muM) exhibited a low activity against C. elegans and had no effect on embryonation and hatching of H. polygyrus eggs. At concentrations of 100 and 50 muM, the inhibition of excretion/secretion of acetylcholinesterase and acid phosphatase of adult H. polygyrus by NTZ was variable. The in vitro effects of mebendazole (5 muM), albendazole (1 muM) and levamisole (10 muM) were superior to those of NTZ. In mice, NTZ at 1 g/kg proved to be inactive against preadults of T. spiralis whereas mebendazole at 10 mg/kg reduced the worm burden by up to 83%. NTZ at 1 g/kg per day for 3 consecutive days showed a low activity against adults of H. polygyrus (21% reduction). Levamisole, at a single dose of 10 mg/kg, reduced the worm burden by up to 89.9%. The results of this study suggest that NTZ would not have met criteria of a candidate compound.

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Section: Discussionmentioning

confidence: 99%

Nematocidal activity of nitazoxanide in laboratory models

Fonseca-Salamanca

Martı́nez-Grueiro

Martínez-Fernández

2003

Parasitology Research

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“…The anthelminthic activities of the N-methylated amidoxime analogues in vivo using the mixed-parasite infection in mice, were examined as well [252]. PF1022A showed full anthelminthic efficacy at the oral dose-rate of 50mg kg -1 against H spumosa [255] and a good activity against H polygyrus, but there was no detectable effect against the tapeworm H nana [256]. Two cyclic depsipeptides (268 and 277) displayed anthelminthic activity against H spumosa (full activity at 50mg kg -1 ) comparable to PF1022A (255), whereas the N-methylated amidoxime 257 showed activity against H polygyrus (full activity at 25mg kg -1 ).…”

Section: Iv5 Anthelminthicidesmentioning

confidence: 99%

Recent Developments in the Chemistry and in the Biological Applications of Amidoximes

Fylaktakidou¹,

Hadjipavlou‐Litina

Litinas³

et al. 2008

CPD

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Amidoximes are compounds bearing both a hydroxyimino and an amino group at the same carbon atom which makes them versatile building blocks for the synthesis of various heterocycles. Their importance in chemistry along with their rich biology, make amidoximes an attractive target for medicinal chemists, biochemists and biologists. Amidoximes and simple O-substituted derivatives possess very important biological activities functioning as antituberculotic, antibacterial, bacteriostatic, insecticidal, elminthicidal, antiviral, herbicidal, fungicidal, antineoplastic, antiarrythmic, antihypertensive, antihistaminic, anxiolytic-antidepressant, anti-inflammatory/antioxidant, antiaggregatory (NO donors) or plant growth regulatory agents. A number of amidoximes has already been used as drugs, or currently being in clinical trials. Their numerous pharmaceutical applications have been recently enriched, due to the fact that some mechanistic pathways, concerning their conversion to amidines, as well as their ability to release NO were clarified, giving a new insight to their mode of action and allowing the design of new therapeutic agents. The main subject of the present review paper is to highlight aspects concerning chemical and biological questions on this interesting class of compounds. Some new synthetic methodologies as well as improvements of previously reported general reactions involving amidoximes, acylated amidoximes, and amidines are presented. The biological applications of amidoximes over the end of 2006 are also extensively reviewed.

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“…It is also known that piperazine analogues inhibit AchE. 8 The electrondonating effect is the most important factor on the benzyl benzene ring, suggesting a role in regulating the protonation equilibrium at the benzylic nitrogen of the piperazine skeleton. The smaller the substituent, the more favorable activity at diphenyl methyl site of the molecule.…”

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confidence: 99%