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2 edition of Aspects of the biological activity of the schistosomicide oxamniquine found in the catalog.

Aspects of the biological activity of the schistosomicide oxamniquine

Catherine W. Karekezi

Aspects of the biological activity of the schistosomicide oxamniquine

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Published .
Written in English


Edition Notes

Thesis (Ph.D.) - Loughborough University of Technology, 1992.

Statementby Catherine W. Karekezi.
ID Numbers
Open LibraryOL21516219M

Schistosomiasis, also known as snail fever and bilharzia, is a disease caused by parasitic flatworms called schistosomes. The urinary tract or the intestines may be infected. Symptoms include abdominal pain, diarrhea, bloody stool, or blood in the urine. Those who have been infected for a long time may experience liver damage, kidney failure, infertility, or bladder cancer. Oxamniquine – Molecular structure and pharmacokinetics. Oxamniquine was first described in the late s. The compound is 6-hydromethylisopropyl-aminomethylnitro 1,2,4-tetrahydroquinoline. It is produced by biological processes. Biological Problem The parasitic infection schistosomiasis is a worldwide problem that affects over 75 countries and over million individuals. While infection rates in some areas are decreasing and some control projects have had positive results, overall the number of infected individuals has "not been reduced and may well be increasing" (38).


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Aspects of the biological activity of the schistosomicide oxamniquine by Catherine W. Karekezi Download PDF EPUB FB2

Aspects of the biological activity of the schistosomicide oxamniquine. By Catherine W. Karekezi. Download PDF (4 MB) Abstract.

A Doctoral Thesis. Submitted in partial fulfilment of the requirements for the award of Doctor of Philosophy at Loughborough quine, 6-hydroxymethylN-isopropylaminomethylnitro-1,2,3,4-\ud Author: Catherine W.

Karekezi. Aspects of the biological activity of the schistosomicide oxamniquine Oxamniquine, 6-hydroxymethylN-isopropylaminomethylnitro-1,2,3,4- tetrahydroquinoline, is a potent schistosomicide used clinically in the treatment of infections due to Schistosoma mansoni.

Schistosomiasis is the second most important tropical disease after : Catherine W. Karekezi. Oxamniquine derivatives were synthesized and evaluated as novel schistosomicide agents. Oxamniquine (1,2,3,4-tetrahydro[[(1-methylethyl)amino]methyl]nitroquinolinemethanol) was submitted to the Mannich reaction, using formaldehyde, paraformaldehyde and acetaldehyde as reagents, and gave three unexpected products: two of them were cyclized on the alkylamine side Cited by:   Preliminary biological screening aims to evaluate the activity of the compounds 1, 2, and 3, and to compare the prolonged action, especially for the methacrylic copolymer, in relation to oxamniquine.

The in vivo assays were carried out using the quantitative oogram test and the mesenteric veins perfusion technique. 31, 32Cited by: 9. A single oral or intramuscular dose of oxamniquine (6-hydroxymethylisopropylaminomethylnitro-1,2,3,4-tetrahydroquinoline) had potent schistosomicidal action against Schistosoma mansoni in mice and hamsters.

No convincing activity was demonstrated against Chinese S. japonicum in either host, or against Nigerian S. haematobium in hamsters, although the schistosomicide Cited by: The main goal of this work was to syntetize the 6-formyl-oxamniquine derivative and evaluate its biological activity.

The 6-formyl-oxamniquine derivative was obtained by the oxidation of. Activity against S. haematobium 3 infected baboons, B, B and B, were available for treatment. The worms appeared to be almost exclusively in the mesenteric plexus, and efficacy was assessed STUDIES WITH THE SCHISTOSOMICIDE OXAMNIQUINE (UK) by variations in faecal egg output.

Author: Karekezi CW. Search worldwide, life-sciences literature Search. Advanced Search. E.g. "breast cancer" HER2 Smith J. Oxamniquine (UK) is a fairly new schistosomicide [5] and there are as yet no published data regarding its mode of action at the molecular level.

Consequently it was deemed interesting to test the effect of this drug on the OTA activity in 5. mansoni both in vitro and in vivo. Oxamniquine (OXA) is a schistosomicide agent that causes some adverse effects in central nervous system. Intending to improve OXA therapeutic properties, a polymeric prodrug was designed.

Introduction. For more than 25 years, the mainstay of treatment for Schistosoma mansoni infections in Brazil was the drug oxamniquine (OXA, (RS)-1,2,3,4-tetrahydro isopropylaminomethylnitroquinolylmethanol)[1,2].OXA is species-specific, killing i (67 million cases worldwide) but not other schistosome species in Africa (obium, million cases) or in SE Asia (S.

Oxamniquine 3 was discovered through an optimization study on Mirasan 2, a lead found by Kikuth and Gönnert at Bayer. Compound 2 was found to have schistosomicidal activity in mice while completely inactive in a monkey model.

It was later discovered that an active metabolite isolated from the urine of treated mice proved to have high potency. Oxamniquine (UK) is a 2-aminomethyltetrahydroquinoline derivative. It is prepared by biological hydroxylation from compound UK [this Bulletin,v.

69, abstr. It is % soluble in water at 27°C. In the present experiments it was shown that a single oral or intramuscular dose of mg/kg had potent action against Puerto Rican Schistosoma mansoni infections in mice. When oxamniquine was used to treat S. mansoni infections in monkeys (Cebus, Cercopithecus, or Papio), a single dose of mg/kg intramuscularly (i.m.) or intravenously completely suppressed passage of eggs in the faeces.

This effect was due to killing of the male worms, while many female worms remained alive. When given by mouth the required dose depended on the genus of the host. Med. Chem. All Publications/Website. OR SEARCH CITATIONS. Livia Pica-Mattoccia's 50 research works with 2, citations and 6, reads, including: Structural and Enzymatic Insights into Species-specific Resistance to Schistosome Parasite Drug Therapy.

Oxamniquine (UK), a tetrahydroquinoline, was examined for schistosomicidal activity in white mice, multimammate mice and vervet monkeys infected with a South African strain of Schistosoma mansoni.

Treatment in rodents and monkeys commenced 10 weeks and 8 months after infection respectively. Results were poor in rodents at doses as high as 60 mg/kg.

Abstract. The changes in eosinophil levels and in eosinophilmediated antibody-dependent schistosomular cytotoxicity, following treatment for Schistosoma manson. Title:Synthesis and Biological Potentials of Quinoline Analogues: A Review of Literature VOLUME: 16 ISSUE: 7 Author(s):Leena Kumari, Salahuddin*, Avijit Mazumder, Daman Pandey, Mohammad Shahar Yar*, Rajnish Kumar, Rupa Mazumder, Mohammad Sarafroz, Mohamed Jawed Ahsan, Vivek Kumar and Sushma Gupta Affiliation:Noida Institute of Engineering and Technology (Pharmacy Institute), Plot No.

Trans R Soc Trop Med Hyg. ;67(5) Studies with the schistosomicide oxamniquine (UK). Activity in rodents and in vitro. Foster R, Cheetham BL. Recent advances in schistosome biochemistry - Volume 89 Issue 3 - G.

Coles. To send this article to your Kindle, first ensure [email protected] is added to your Approved Personal Document E-mail List under your Personal Document Settings on the Manage Your Content and Devices page of your Amazon account. Biological activity of 4-loaded liposomes.

Ethical aspects and statistics. Oxamniquine, a well-known schistosomicide that acts by inhibiting nucleic synthesis and promoting irreversible alkylation of schistosomal DNA (2), was encapsulated into conventional liposomes (LOXA). Trans R Soc Trop Med Hyg.

;67(5) Studies with the schistosomicide oxamniquine (UK). Activity in primates. Foster R, Cheetham BL, King DF. Oxamniquine (OXA) has been the cornerstone of Brazilian schistosomiasis control programs during the last 25 years and still is one of the two commercially available drugs that are effective against Schistosoma mansoni (Coura & AmaralWHO ).

Available information on the mechanism of action of OXA (and of the related agent hycanthone) suggests that the drug becomes active only upon. Novel drugs. Several drugs targeting other parasites were tested for potential schistosomicidal activity (Table 1).The anti malarial drug artemether, a methoxy derivative of artemisinin, has been shown to be active against S.

japonica, S. mansoni, and S. haematobium in experimentally infected animals.A single oral injection of mg/kg artemether to mice infected with approximately A schistosomicide is a drug used to combat schistosomiasis.

Examples listed in MeSH include. amoscanate; arteether; artemether; chloroxylenol; hycanthone. 3 The Use of Brazilian Medicinal Plants to Combat Schistosoma mansoni Silmara Marques Allegretti, Claudineide Nascimento Fernandes de Oliveira, Rosimeire Nunes de Oliveira, Tarsila Ferraz Frezza and Vera Lúcia Garcia Rehder Universidade Estadual de Campinas Brazil.

Schistosomiasis, a parasitic disease caused by trematodes of the genus Schistosoma, is the second most prevalent parasitic disease in the world. It affects around million people. Clinical treatment, prophylaxis, and prevention are performed in countries susceptible to schistosomiasis.

In the pharmacological treatment for an acute form of schistosomiasis, the use of antiparasitics, mainly. b. Biological clock and their significance leading to chronotherapy.

Dose calculation in pharmacological experiments. Antiallergic activity by mast cell stabilization assay. Study of anti-ulcer activity of a drug using pylorus ligand (SHAY) rat model and NSAIDS induced ulcer model.

Study of effect of drugs on gastrointestinal. Schistosomiasis is a chronic neglected tropical disease, highlighted by the presence of Schistosomaworms, which presents in advanced cases in approximately 80 countries, affecting almost.

Eucalyptus is the most important genera in the botanical family Myrtaceae; it is widely distributed in different regions around the world, with more than species (Hassine et al. Eucalyptus camaldulensis Dehnh, commonly known as the river red gum, is endemic in Australia (Singab et al.

).Leaves of E. camaldulensis are known to possess several biological and pharmacological. Structure Activity Relationships (SAR) Once the structure of lead compound is known, the medicinal chemist moves on to study its SAR. The aim is to discover which parts of the molecule are important to biological activity and which are not.

X-ray crystallography and NMR can be used to study and identify important binding interactions between. The oxamniquine methacrylate and the acrylamide, groups 1 and 2, respectively, showed a decrease in the number of eggs compared to the untreated group, so that antiparasitic activity may be associated.

Oxamniquine polymethacrylate, group 3, provided a decrease in the number of eggs, particularly in the 1st and 2nd stages (20th day). STRUCTURE ACTIVITY RELATIONSHIPS (SARs) (Chapter No.

7) Once the structure of lead compound is known, the medicinal chemist moves on to study its SAR. The aim is to discover which parts of the molecule are important to biological activity and which are not. see more details of hycanthone and oxamniquine oxamniquine Subject Category: Chemicals and Chemical Groups see more details by V.

RAY, H. HOLDEN, J. ELLIS, Jr, and M. HYNECK (p. ) follows. Oxamniquine, a schistosomicide currently under clinical investigation, was the subject of a series of genetic tests designed to detect.

In at least one instance — the antischistosomal action of trivalent organic antimonials — trematocidal activity can be ascribed to an inhibitory effect of the drug on a single enzyme. On the other hand, in the case of the action of piperazine on Ascaris, inhibition of the formation of succinate has been found to be the result, rather than.

Structure Activity Relationships (S AR), therapeutic uses and synthesis of important drugs. Objectives: Upon completion of the course student shall be able to 1.

Understand the importance of drug design and different techniques of drug design. Understand the chemistry of drugs with respect to their biological activity. It contains over genera with nearly species.

Species from this family were subjected to intensive investigation due to the presence of different secondary metabolites with potent biological activity, such as triterpenes, flavonoids, alkaloids and coumarins.

2, 3 Among the pharmacologically interesting genera are Sterculia and Brachychiton. Furthermore, 63 gene products have ATPase activity, 49 possess helicase activity, 48 exhibit motor activity, 39 actin-binding properties and 32 have calmodulin-binding activity.

In vitro metabolic behavior was investigated for two chromium tricarbonyl derivatives of the antischistosomal drug praziquantel (PZQ) with the formula (η6-PZQ)Cr(CO)3 (1 and 2), by use of human liver microsomes.

The metabolic profiles of the derivatives differ significantly. The optically pure (η6-PZQ)Cr(CO)3 derivatives (S, Sp)-1, (R, Rp)-1, (S, Rp)-2, and (R, Sp)-2 were also prepared to. The LibreTexts libraries are Powered by MindTouch ® and are supported by the Department of Education Open Textbook Pilot Project, the UC Davis Office of the Provost, the UC Davis Library, the California State University Affordable Learning Solutions Program, and Merlot.

We also acknowledge previous National Science Foundation support under grant numbers, and   The three activity categories are based on the PubChem activity score, an evaluation parameter relying on the [] values, which marks compounds as having a score of 0 as being inactive, as inconclusive, and as active.Oxamniquine is an aminoethyltetrahydroquinolone derivative that was first described in the late s.

It is known to be effective only against S. mansoni, particularly the invasive stages and adult worms, with male worms more sensitive to the drug than female worms. 37, 39 Like praziquantel, oxamniquine is rapidly absorbed, reaching its.