Trypanocide Diamidine des 2‐Phenyl‐benzofurans, 2‐Phenyl‐indens und 2‐Phenyl‐indols

Abstract

Es werden Diamidine synthetisiert, welche die Amidino-Gruppen in 4'.5-bzw. 4'.6-Stellung der Ringgeruste des 2-Phenyl-benzofurans (4e, 5e und 3e), des 2-Phenyl-indens (lOd, 16a, 16 b, 16c, 16d), des 2-Phenyl-2.3-dihydro-indens (17b) sowie des 2-Phenyl-indols (18 1, 18n, 18p, 19d, 19e) enthalten; von letzterem werden auRerdem die 3'.5-bzw. 3'.6-Diamidine (18m bzw. 180) dargestellt. -Das 4'.5-Diamidin 4e des 2-Phenyl-benzofurans besitzt eine uberragende Wirksamkeit gegen Trypanosoma rhodesiense. Die Diamidine des 2-Phenylindens haben ein Wirkungsspektrum wie jene des 2-Phenyl-thionaphthens mit dem Schwerpunkt gegen T. garnbiense, und das 4'.6-Diamidin 18n des 2-Phenyl-indols besitzt eine iiberragende, seltene Wirksamkeit gegen T. congolense. Trypanocide Diamidines of 2-Phenylbenzofuran, 2-Phenylindene and 2-PhenylindoleDiamidines with the amidino-groups in 4'.5-and 4'.6-posititon of the ring skeletons of 2-phenylbenzofuran (4e, 5e, 3e), of 2-phenylindene (lOd, 16a, 16b, 16c, 16d), of 2-phenyl-2.3-dihydroindene (17b) and of 2-phenylindole (18 1, 18n, 18p, 19d, 19e) are synthesized; the 3'.5-and 3'.6-diamidines 18m, 180 of 2-phenylindole are also prepared. -The activity of 4'.5-diamidine 4e of 2-phenylbenzofuran against Trypanosoma rhodesiense surpasses all others. The spectrum of activity of diamidines of 2-phenylindene resembles that of the diamidines of 2-phenylthionaphthene with the main activity against T. garnbiense. The 4'.6-diamidine 18n of 2-phenylindole exhibits the highest and rarely found activity against T. congolense.

Development-Dependent Changes in the Amount and Structural Organization of Plastid DNA

“…The appearance of plastid DNA in sub-plastomic bodies further sparked scienti fi c interest. Various methods were used to obtain information on the structure and organization of the plastid DNA within the chloroplast, which ranged from early analyses of plastids isolated from thymidine labeled tissue by microscopic autoradiography to the later use of a DNA-speci fi c, fl uorescent stain, DAPI (4 ¢ ,6-diamidino-2-phenylindole) (Herrmann 1970 ;Herrmann and Kowallik 1970 ;Dann et al 1971 ;Kowallik and Herrmann 1972 ;Coleman 1978Coleman , 1979James and Jope 1978 ; .…”

Dicationic DNA Minor Groove Binders as Antimicrobial Agents

“…[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].…”

Selection of aggressive pathogenic and solopathogenic strains of Ustilago maydis to improve Huitlacoche production

“…To stain the DNA, a drop of this suspension was placed on a slide with 0.5 µg mL −1 of the reagent 4', 6-diamino-2-phenylindole (DAPI) in phosphate-buffered saline (pH 7.2) for 20 min at 60 °C and subsequently washed with the same buffer (Dann et al 1971). After 20 min, samples were observed under a fluorescence microscope with mercury short arc lamps HBO 50 W at a wavelength of 350 nanometers (Axiolab, Carl Zeiss, Germany).…”