Atebrin, ein Neues Heilmittel Gegen Malaria

Mauss, H.; Mietzsch, F.

doi:10.1007/bf01788930

Cited by 35 publications

(4 citation statements)

References 7 publications

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“…from Muhlens, 1928, and Sioli, 1929). At that point, those involved in these studies turned attention to the newly prepared Atebrin (quinacrine) (18).…”

Section: Rc-12 [12-dimethoxy-4-(bis-diethylaminoethyl)-amino-5-mentioning

confidence: 99%

Antimalarial activities and subacute toxicity of RC-12, a 4-amino-substituted pyrocatechol

Schmidt¹,

Rossan²,

Fradkin³

et al. 1985

Antimicrob Agents Chemother

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RC-12 [1,2-dimethoxy-4-(bis-diethylaminoethyl)-amino-5-bromobenzeneI was evaluated for prophylactic, radical curative, and suppressive activities against infections with Plasmodium cynomolgi and subacute toxicity in rhesus monkeys. Applied as a prophylactic agent, RC-12, administered in doses of 6.25 to 25.0 mg/kg daily throughout the incubation period, provided near-complete to complete protection against 105 to 106 times the minimum infective dose of sporozoites. Applied as a suppressive agent, daily doses of 100.0 mg of RC-12 per kg did not eradicate blood schizonts regularly; hence, the need for concomitant administration of a blood schizonticide, such as chloroquine, in assessments of radical curative activity. In such appraisals, daily doses of 6.25 to 25.0 mg of RC-12 per kg for 14 days, in combination with 2.5 mg of chloroquine per kg daily for 7 days, effected cure of 69 and 93% of established infections, respectively. The curative activity of RC-12 was related to the total dose and could be achieved with a regimen as brief as 4 days. With respect to outward expressions of toxicity, daily doses of 50.0 mg/kg or lower for 15 to 225 days evoked no reactions. Doses of 100.0 or 200.0 mg/kg, scheduled for 15 days, evoked convulsions and depression and were, respectively, lethal to 4 of 17 and 7 of 7 recipients. Doses of 25.0 mg/kg or lower evoked no discrete reactions. Doses of 50.0 mg/kg and higher evoked hepatomegaly, vacuolation of hepatocytes, and elevations of glutamic oxalacetic and glutamic pyruvic transferase activities in serum, reactions related in intensity to dose but not duration of dosage.

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“…from Muhlens, 1928, and Sioli, 1929). At that point, those involved in these studies turned attention to the newly prepared Atebrin (quinacrine) (18).…”

Section: Rc-12 [12-dimethoxy-4-(bis-diethylaminoethyl)-amino-5-mentioning

confidence: 99%

Antimalarial activities and subacute toxicity of RC-12, a 4-amino-substituted pyrocatechol

Schmidt¹,

Rossan²,

Fradkin³

et al. 1985

Antimicrob Agents Chemother

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“…Quinacrine (Atebrin, Atabrine, mepacrine) was discovered by Mauss and Mietsch (1933) Wiselogle (1946).…”

Section: Human Malariamentioning

confidence: 99%

Protozoan parasites of domestic animals and of man

Levine¹

1961

516

493

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A disease which is common to man and lower animals is known as a zoo)iosis. Zoonoses were redefined in 1958 by the Joint WHO FAO Expert Committee on Zoonoses as "those diseases and infections which are naturally transmitted between vertebrate animals and man" (World Health Organization, 1959). Less than 20 years ago it was said that there were 50 zoonoses, but in the above report the World Health Organization listed more in connection with vector-borne diseases, altho it need not be restricted to them. epidemiology, taxonomy, evolution, etc.(see ). A dei)ie is a natural population within a species. It lies more or less below the subspecies level, but it is not a formal taxon and is not given a Latin name. There are different types of deme. Nosodemes differ in their clinical manifestations. One example is Leishmania donovani, which has five nosodemes, Indian, Mediterranean, Sudanese, Chinese and South American, which produce different types of disease. Serodemes differ serologically. These are best known among the bacteria and viruses, but also occur among the animal parasites. Tritrichonionas foetus, for example, has several serological types or serodemes. were markedly resistant to infection with Ostertagia circunicincta. while Rambouillets were less so and Southdowns, Shropshires and Hampshires were least resistant.Certain individuals among the more susceptible breeds, however, were just as resistant as the Romneys. Whitlock(1958) has studied genetic resistance to trichostrongylidosis in sheep in some detail.The nutritional status of the host may affect its resistance. Poorly nourished animals are usually more susceptible to infection and suffer more severely from its effects.Protein depletion or protein starvation is particularly important. Lack of specific vitamins and minerals generally decreases resistance, but there are cases in which lack of a certain vitamin which the parasite requires may affect the parasite adversely. Thus, Becker and Smith (1942) found that when calcium pantothenate was added to a ration containing restricted vitamins B,, Bg and pantothenate, the number of oocysts produced hy Einteria nieschulzi infections in the rat was increased.

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“…In the preparation of the 9-anilinoacridines (9, arylamines (4) were coupled with 9-chloroacridines (2), obtained directly from the ring closure of an N-arylanthranilic acid (1) with POCl,.20-22 When the ring closure with POCl, was not desirable, this was effected with H2S04, H3P04, polyphosphoric acid, or polyphosphate ester to give the 9(10H)acridones (3), which were easily converted into the desired 9chloroacridines (2) with SOC1,-Me2NCH0. 23 An alternative method of obtaining 9( l0H)-acridones is the Chapman rearrangement 24*25 of N-arylbenzimidates (6) (Scheme 1).…”

Section: Niigata College Of Pharmac Y 5829 Kamishin 'Ei-cho Niigata 9...mentioning

confidence: 99%

Mechanism of the Chapman rearrangement of N-arylbenzimidates on the basis of a molecular structure established by X-ray crystallography

Kimura¹

1987

J. Chem. Soc., Perkin Trans. 2

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Atebrin, ein Neues Heilmittel Gegen Malaria

Cited by 35 publications

References 7 publications

Antimalarial activities and subacute toxicity of RC-12, a 4-amino-substituted pyrocatechol

Antimalarial activities and subacute toxicity of RC-12, a 4-amino-substituted pyrocatechol

Protozoan parasites of domestic animals and of man

Mechanism of the Chapman rearrangement of N-arylbenzimidates on the basis of a molecular structure established by X-ray crystallography

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