Screening Large Numbers of Compounds in a Model Based on Mortality of Trypanosoma Rhodesiense Infected Mice *

Rane, Leo; Rane, Dora S.; Kinnamon, Kenneth E.

doi:10.4269/ajtmh.1976.25.395

Cited by 25 publications

(15 citation statements)

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“…Of 49 compounds tested, however, 6 were active, and this represents 12.2% hits. This is approximately two times as great as when other methods are employed to select compounds for testing with this same standard test (6). In view of this, consideration of further screening of known antitumor agents from classes with previously unknown anti-trypanosomal activity seems warranted.…”

Section: Discussionmentioning

confidence: 92%

“…Results for the 6 active compounds of the 49 tested in this study are summaized in Table 1. The chemical formulas for these are shown in Fig.…”

Section: Resultsmentioning

confidence: 99%

“…The test system has been described elsewhere (6). Briefly, ICR/Ha Swiss mice of either sex, weighing 30 to 32 g, were given an intraperitoneal injection of 0.5 ml of a 1:50,000 dilution of heparinized heart blood drawn from donor mice infected 3 14 days] are known to occur after a single dose of some oncolytic agents, the previously established criteriafor routine screening were followed [6].)…”

Section: Methodsmentioning

confidence: 99%

“…The compounds selected were tested by utilizing a mouse model which employs experimental infections produced by Trypanosoma rhodesiense (6).…”

mentioning

confidence: 99%

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Activity of Antitumor Drugs Against African Trypanosomes

Kinnamon¹,

Steck

Rane

1979

Antimicrob Agents Chemother

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Of 49 compounds known to have antitumor properties, 6 were found to have significant activity against Trypanosoma rhodesiense infections in mice. Activity against the African trypanosomes has not been reported previously for any of these six compounds. In order of decreasing activity these compounds were: (i) imidazole-4-carboxamide, 5-(3,3-dimethyl-1,1-triazene), (ii) inosine diglycolaldehyde, (iii) cis-diamminedichloro-platinum, (iv) streptozotocin, (v) coralyne sulfate, and (vi) 5-fluoro-2'-deoxyuridine. The percentage of "hits" (12.2%) from these known antitumor agents was approximately twice as great as when other means are employed for the selection of compounds for this test system.

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Section: Discussionmentioning

confidence: 92%

“…Results for the 6 active compounds of the 49 tested in this study are summaized in Table 1. The chemical formulas for these are shown in Fig.…”

Section: Resultsmentioning

confidence: 99%

Section: Methodsmentioning

confidence: 99%

“…The compounds selected were tested by utilizing a mouse model which employs experimental infections produced by Trypanosoma rhodesiense (6).…”

mentioning

confidence: 99%

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Activity of Antitumor Drugs Against African Trypanosomes

Kinnamon¹,

Steck

Rane

1979

Antimicrob Agents Chemother

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“…In 14 repetitions, the positive control, ethidium bromide, had a mean ID50 of 0.55 ,ug/ml for thymidine and a mean ID50 of 0.66 ug/ml for the inhibition of leucine uptake. The distribution of each mean was log normal.…”

Section: Resultsmentioning

confidence: 99%

Activity of 2-acetylpyridine thiosemicarbazones against Trypanosoma rhodesiense in vitro

Casero

Klayman

Childs

et al. 1980

Antimicrob Agents Chemother

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Twenty-seven 2-acetylpyridine thiosemicarbazones and analogs were tested for antitrypanosomal activity against Trypanosoma rhodesiense using a semiautomated in vitro assay system. Activity was determined by relative inhibition of uptake of two radiolabeled macromolecular precursors, [methyl-3H]thymidine and L-[U-14C]leucine, as compared to untreated controls. It was observed that the nitrogen atom of the pyridyl moiety of the 2-acetylpyridine thiosemicarbazones was essential for antitrypanosomal activity. The 2-acetylpyridine thiosemicarbazones generally inhibited the uptake of L-[U-14C]leucine to a greater extent than they inhibited [methyl-3H]thymidine uptake. Twenty-four of the 27 compounds tested exhibited activity comparable to that found for the antitrypanosomal agent ethidium bromide.

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Synthesis of 6‐benzyl‐ and 6‐phenethyl‐2,4‐diamino‐5,6,7,8‐tetrahydropyrimido[4,5‐d]pyrimidines

Delia

Sami

1981

Journal of Heterocyclic Chem

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The preparation of ten aralkyl derivatives of 2,4‐diamino‐5,6,7,8‐tetrahydropyrimido[4,5‐d]pyrimidines (6) has been accomplished. The title compounds were prepared in a simple one step reaction from 2,4,6‐triaminopyrimidine (4), formaldehyde (2), and either substituted benzylamines (1a‐d) or substituted phenethylamines (1e‐j). This modified Mannich reaction has been shown to be a general method for such derivatives. Elemental analysis, 1H nmr and mass spectral data have confirmed the proposed structures. None of the compounds exhibited either antimalarial or antitrypanosomal activity.

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Screening Large Numbers of Compounds in a Model Based on Mortality of Trypanosoma Rhodesiense Infected Mice *

Cited by 25 publications

References 0 publications

Activity of Antitumor Drugs Against African Trypanosomes

Activity of Antitumor Drugs Against African Trypanosomes

Activity of 2-acetylpyridine thiosemicarbazones against Trypanosoma rhodesiense in vitro

Synthesis of 6‐benzyl‐ and 6‐phenethyl‐2,4‐diamino‐5,6,7,8‐tetrahydropyrimido[4,5‐d]pyrimidines

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