Detail of "57695-04-2"

Reference

Activity of antileishmanial agents against amastigotes in human monocyte-derived macrophages and in mouse peritoneal macrophages

Activity of antileishmanial agents against amastigotes in human monocyte-derived macrophages and in mouse peritoneal macrophages. Berman, Jonathan D.; Lee, Linda S. (Dep. Parasitol., Walter Reed Army Inst. Res., Washington, DC 20307, USA). J. Parasitol., 70(2), 220-5 (English) 1984. CODEN: JOPAA2. ISSN: 0022-3395. DOCUMENT TYPE: Journal CA Section: 1 (Pharmacology) Leishmania Multiplying within either human monocyte-derived macrophages (HM) or mouse peritoneal exudate cells (PEC) have recently been shown to be susceptible to pentavalent antimony (Sb) by several investigators. The Sb susceptibilities of 5 cutaneous strains of Leishmania were compared in the 2 model systems, with infection of the macrophages initiated with either amastigotes or promastigotes. The susceptibility to Sb of amastigote-induced infections was statistically the same as the susceptibility of promastigote-induced infections for 4 strains in the PEC model, and for 3 of 4 strains in the HM model. Promastigote-induced infections with the 5th strain were non-viable in both macrophage types. The susceptibility of Leishmania to Sb within PEC was the same statistically as that of organisms within HM for amastigote-induced infections for 4 of 5 strains and for promastigote-induced infections by 3 of 4 strains. These data suggested that the susceptibilities of organisms to Sb within PEC and HM were generally comparable and that either amastigotes or viable promastigotes could be used to initiate the infection. The several tech. advantages of the PEC model may make it more useful than the HM model for testing susceptibility to Sb. The modest susceptibility of some strains in both models to the peak serum amts. of Sb which may be achieved by presently recommended treatment regimes may partially explain the high current failure rate in simple cutaneous disease. The susceptibility of one strain within peritoneal cells to primaquine [90-34-6] and WR 6026 [57695-04-2] (8-aminoquinolines), ketoconazole [65277-42-1] (an imidazole) and formycin B [13877-76-4] (an anosine analog) was similar to that previously reported in human macrophages. Organisms within peritoneal cells were relatively resistant to peak achievable serum amts. of pentamidine [100-33-4] (a diamidine). These results suggest that the antileishmanial activity of 3 of the latter 4 tested classes of compds. can be evaluated in either the PEC or the HM models.

High-performance liquid chromatographic method for the analysis of a candidate 8-aminoquinoline antileishmanial drug using oxidative electrochemical detection

High-performance liquid chromatographic method for the analysis of a candidate 8-aminoquinoline antileishmanial drug using oxidative electrochemical detection. Anders, John C.; Theoharides, Anthony D.; Thomas, Lena M.; Smyth, Michael H.; Chung, Ho (Dep. Pharmacol., Walter Reed Army Inst. Res., Washington, DC 20307, USA). J. Chromatogr., 311(1), 117-23 (English) 1984. CODEN: JOCRAM. ISSN: 0021-9673. DOCUMENT TYPE: Journal CA Section: 1 (Pharmacology) An anal. method was developed for the quantitation of a candidate antileishmanial drug, 6-methoxy-8-(6-diethylaminohexylamine)-4-methylquinoline (I) [57695-04-2], in canine plasma. The assay utilized an internal std. technique with a structurally similar 8-aminoquinoline, 6-methoxy-8-(7-diethylaminoheptylamine)-4-methylquinoline, dihydrochloride, as the internal std. The method employs a liq.-solid extn. procedure with prepackaged silica gel columns upon which the drug and internal std. are adsorbed, then selectively washed and eluted. Reversed-phase chromatog. was then employed to analyze the extd. sample by means of oxidative electrochem. detection at +0.75V. Good accuracy and precision were obtained over the concn. range tested (10-1500 ng/mL plasma). Analyses of plasma samples from human volunteers given the drug demonstrate that the method is also suitable for anal. of human plasma samples. The procedure is relatively simple and requires only 1 mL of plasma.