Antitrypanosomal activity

Hoet S, Stevigny C, Block S, et al. Alkaloids from Cassytha filiformis and related apor-phines antitrypanosomal activity, cytotoxicity, and interaction with DNA and topoisomerases. Planta Med 2004 70 407-413. 

There was particular interest in the analogous reactions of 1-Oacetyl-2,3,5-tri-0-benzoyl-4-bromo-/ -D-ribose (37), because of the potential to prepare from it compounds related to nucleocidin, which is a 4 -fluoroaden-osine derivative having antitrypanosomal activity. With silver fluoride in acetonitrile, this bromide also reacted mainly with inversion of configuration, and gave the l-lyxo fluoride 140 (53% isolated yield), whereas, with silver tetrafluoroborate, much more of the more interesting 1-0-acetyl-2,3,4-tri-0-benzoyl-4-fluoro-/ -D-ribose (141) was obtained.38... 

Among other activities, investigations were concerned with radio-protective effects (83MI3), antitrypanosomal activity (80JMC578), and amplifiers of phleomycin (85AJC1685). Pyridazines were shown to be potent tyrosine hydroxylase dopamine /3-hydroxylase inhibitors (83MI11). 

Compounds (21-23) illustrate further examples of nonclassical bioisosteres. Compound (21) was reported to display antitrypanosomal activity (18). The analogs (22) and (23) also displayed antitrypanosomal activity (19). Compound (22) demonstrated the most impressive activity (IC50 values of 40 and... 

Purinethol mercaptopurine. puromycin ban, inn, usan] (puromycin hydrochloride [USAN] NSC 3055 CL 16536 antibiotic CL 16536 CL 13900 3123L P 638 antibiotic CL 13900 antibiotic 3123L antibiotic P 638) is a nucleoside-type ANTIBIOTIC isolated from Streptomyces alboniger. It has anticancer and ANTITRYPANOSOMAL activity, puromycin hydrochloride puromycin. p-xylotocopherol p-tocopherol. 

Antifungal activity. Ginkgetin and isoginkgetin were active leishmanicidal compounds. These compounds also showed good antitrypanosomal activity. 

Podocarpus latifolius (Thunb.) R. Br. ex Mirb. (leaves) Biflavones Amentoflavone (1) I-7,4 -di-O-methyl-amentoflavone (= ginkgetin) (7) heveaflavone (18) I-7,4, II-7,4 -tetra-O-methylamentoflavone (19). Used in Zulu traditional medieine. Ginkgetin is an aetive leishmanicidal compound. Ginkgetin also showed a good antitrypanosomal activity. Antimicrobial activity. Fozdar et al., 1989[483] Abdillahi et al., 2008[484], 2010[485]. 

Taxus wallichiana Zucc. (leaves and branches) Biflavones Sequoiaflavone (2) ginkgetin (7) sciadopitysin (15). Ginkgetin is an active leishmanicidal compound. Ginkgetin also showed a good antitrypanosomal activity. Qiu et ah, 1989[492] Weniger etal.,2006[86]. 

Antiprotozoal Activity (Antiplasmodial, Leishmanicidal and Antitrypanosomal Activities)... 

Weniger, B. Vonthron-Senecheau, C. Kaiser, M. Bnm, R. Anton, R., Comparative antiplasmodial, leishmanicidal and antitrypanosomal activities of several biflavonoids, Phytomedicine, 2006, 13, 176-180. 

Pozharskii s interest for A -aminoazoles <92AHC(53)85> continues he described the Schilf bases derived from 1- and 2-aminoindazole <93ZORi896>. It has been shown that A -aminopyrazole reacts with nitrofurfural to alford the Schiff base (28), which has interesting antitrypanosomal activity <87AP(320)115> (see Section 3.01.13.2). Other imines derived from jV-aminopyrazoles and 7V-amino-pyrazolinones have been reduced by hydrogenation into A -alkylamino derivatives <92JHC32i>. 

Diamino-4-arylazo-2//-l,2,6-thiadiazine 1,1-dioxides have been used as yellow range dyestuffs for paper <92GEP4208535>. Antitrichomonal and antitrypanosomal activity of 1,2,6-thiadiazine 1,1-dioxides has been noted <92MI 616-02). 

Plants accumulate STLs as a means of chemical defence. Thus, one of the primary ecological benefits of these compounds is certainly the fact that they are toxic to all kinds of microorganisms. Once more it is their alkylant potency that is most obviously responsible. The work on antimicrobial activity of earlier years has been summarized in various reviews, e.g. [1-3]. More recent work has indicated that some STLs may have potential as leads for new antiprotozoal drugs. Apart from the prominent antimalarial artemisinin which will be treated separately in the following section, several more common STLs have been demonstrated to possess antiplasmodial [77-79], antileishmanial [80] and antitrypanosomal activity [81-84], Unfortunately, in most cases such activities are accompanied by high non-specific cytotoxicity so that it is always necessary to compare the antiprotozoal activity with cytotoxic effects determined under the same conditions. 

Bodley AL, Wani MC, Wall ME et al. Antitrypanosom activity of camptothecin analogs. Structure-activity correlations. Biochem Pharmacol 1995 50 937-942. 

Gamage SA, Fi itt DP, Wojcik Sj et al. Structure-activity relationships for the antileishmanial and antitrypanosomal activities of T-substituted 9-anilinoacridines. J Med Chem 1997 40 2634-42. Werbovetz KA, Lehnert EK, Macdonald TL et al. Cytotoxicity of acridine compounds for Leishmania promastigotes in vitro. Antimicrob Agents Chemother 1992 36 495-497. 

Hopp, K.H. Cunningham, L.V. Bromel, M.C. Schermeister, L.J. 8c Kahlil, S.K.W. 1976. In vitro antitrypanosomal activity of certain alkaloids against Trypanosoma lewisi. Lloydia Vol. 39 375-377. 

In the second route, 3-methoxy phenylethanamine 106 was brominated and then it was N-alkylated to get convolutamine I (95) [52]. By employing the same synthetic strategies, Pham et al. prepared a variety of analogues of convolutamine I (95) and evaluated for antitrypanosomal activity against Trypanosoma brucei brucei and few of the analogues were found more potent than parent natural product [52]. 

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