Trypanocide Diamidine mit drei Ringen in zwei isolierten Ringsystemen

Dann, Otto; Fernbach, Rainer; Pfeifer, Wolfgang; Demant, Ekke; Bergen, Gerhard; Lang, Siegfried; Lürding, Gerd

doi:10.1002/jlac.19727600105

Cited by 25 publications

(16 citation statements)

References 36 publications

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“…Compounds X and XVII have only a low activity against 7: congolense [Dann et al, 1970[Dann et al, , 1971[Dann et al, , 1972[Dann et al, , 1973[Dann et al, , 1975[Dann et al, , 1982.…”

Section: Discussionmentioning

confidence: 99%

Hemodynamic effects of a series of new trypanocidal indoleamidino compounds

Steinmann

Estler

Dann

1986

Drug Development Research

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The influence of 17 recently developed trypanocidal amidino compounds on blood pressure, heart rate, and carotid blood flow has been investigated in rats. Their cardiovascular effects were compared with those produced by pentamidine (Lomidine@) and diminazen (Berenil@). All compounds lowered the arterial blood pressure, especially the diastolic pressure, and almost all agents caused a reflex tachycardia and some reduction of the carotid blood flow. The hypotensive potency of the compounds can be reduced by alterations of the chain length between the cation moieties.

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“…Compounds X and XVII have only a low activity against 7: congolense [Dann et al, 1970[Dann et al, , 1971[Dann et al, , 1972[Dann et al, , 1973[Dann et al, , 1975[Dann et al, , 1982.…”

Section: Discussionmentioning

confidence: 99%

Hemodynamic effects of a series of new trypanocidal indoleamidino compounds

Steinmann

Estler

Dann

1986

Drug Development Research

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“…A protocol similar to that described above was used for the condensation of 4-(N-cyclopentylamidino)-1,2-phenylene diamine with 1-methyl-2,5-pyrrole dicarboxaldehyde (12) to give an 85% yield of a blue solid; mp, 324 to 326°C dec. 1 A protocol similar to that described above was used for the condensation of 4-(N-cyclopentylamidino)-1,2-phenylene diamine with 2,5-bis(4-formylphenyl) furan to give a 77% yield of a yellow solid; mp 295 to 297°C dec. 1 (14) to give an 86% yield; mp, 110 to 111°C (literature mp, 108 to 111°C). 1 furan was prepared by reduction of the bis-nitrile with DIBAL, which was added dropwise to a stirred solution of the bis-nitrile (1.68 g, 0.01 mol) in 150 ml of dry methylene chloride under nitrogen.…”

Section: 5-bis[2-(5-n-cyclopentylamidino)benzimidazoyl]-1-methylpyrmentioning

confidence: 99%

Structure-In Vitro Activity Relationships of Pentamidine Analogues and Dication-Substituted Bis-Benzimidazoles as New Antifungal Agents

Poeta

Schell

Dykstra

et al. 1998

Antimicrob Agents Chemother

224

102

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Twenty analogues of pentamidine, 7 primary metabolites of pentamidine, and 30 dicationic substituted bis-benzimidazoles were screened for their inhibitory and fungicidal activities againstCandida albicans and Cryptococcus neoformans. A majority of the compounds had MICs at which 80% of the strains were inhibited (MIC80s) comparable to those of amphotericin B and fluconazole. Unlike fluconazole, many of these compounds were found to have potent fungicidal activity. The most potent compound against C. albicans had an MIC80 of ≤0.09 μg/ml, and the most potent compound against C. neoformans had an MIC80 of 0.19 μg/ml. Selected compounds were also found to be active againstAspergillus fumigatus, Fusarium solani,Candida species other than C. albicans, and fluconazole-resistant strains of C. albicans and C. neoformans. It is clear from the data presented here that further studies on the structure-activity relationships, mechanisms of action and toxicities, and in vivo efficacies of these compounds are warranted to determine their clinical potential.

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“…[21,23,26], Pneumocystis carinii [27][28][29][30], Toxoplasma gondii [31], and Trypanosoma sp. [32][33][34][35][36][37]. Despite the broad-spectrum activity of this class of compounds, only pentamidine has been found to be of significant use in the clinic to date, where it has been used against primary stage African trypanosomiasis, antimony-resistant leishmaniasis and AIDs-associated Pneumocystis carinii [38][39][40].…”

Section: Introductionmentioning

confidence: 99%