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Beta-carboline-3-carboxamide derivatives as promising antileishmanial agents


, : Beta-carboline-3-carboxamide derivatives as promising antileishmanial agents. Annals of Tropical Medicine and Parasitology 105(8): 549-557

Leishmaniasis has an overwhelming impact on global public health especially in tropical and subtropical countries and the currently available antileishmanial drugs have serious side effects and low efficacy. Natural and synthetic compounds have been tested in the past few years against Leishmania and the beta-carboline class of compounds have shown great results in antiparasitic chemotherapy. In the present study, three 1-substituted beta-carboline-3-carboxamides (3-5) and 1-substituted beta-carboline-3-carboxylic acid (2) were synthesized and screened for in vitro activity against L. amazonensis. Compound 5 (N-benzyl 1-(4-methoxy)phenyl-9H-beta-carboline-3-carboxamide) had the best activity against promastigote and axenic amastigote forms with IC(50) of 2·6 and 1·0 μM, respectively. Its CC(50) on macrophages cell line was higher than 2457·0 μM with an SI ratio of 930·2. Against intracellular amastigote forms, it had a dose-dependent relationship with a 50% growth inhibitory concentration of 1·0 μM. Through morphological and ultrastructure analysis of promastigote forms treated with compound 5, alterations on cell shape and number of flagella and nuclear membrane damage were observed. For this, compound 5 supports the idea for more in vitro and in vivo studies.

US$19.90

PMID: 22325814

DOI: 10.1179/2047773211Y.0000000005


Other references

Kostina, V.S., 1974: A comparative study of water regime in legumes. Information on transpiration, water contents and water-holding capacity is given for peas, peavine [Lathyrus sativus] and chickpea [Cicer arietinum] grown in different regions of the Stavropol' province.

McLaren, M.E.; Szymkowicz, S.M.; O'Shea, A.; Woods, A.J.; Anton, S.D.; Dotson, V.M., 2017: Vertex-wise examination of depressive symptom dimensions and brain volumes in older adults. Differences in brain volumes have commonly been reported in older adults with both subthreshold and major depression. Few studies have examined the association between specific symptom dimensions of depression and brain volumes. This study used ve...

Su, E.; Crowley, K.; Carcillo, J.A.; Michaels, M.G., 2011: Linezolid and lactic acidosis: a role for lactate monitoring with long-term linezolid use in children. Linezolid administration has been associated with lactic acidosis in adults; however, the same phenomenon has not been reported in children. Mitochondrial protein synthesis inhibition is a demonstrated mechanism for toxicity, which therefore may m...

Wood, M.; Joyce, J.; Wood, M.; Joyce, J., 2008: Preparing for certification: Halifax nephrology nurses--in quest of excellence. 1992. Cannt Journal 18(3): 50-51

Govaert, J., 1955: Quantitative study of desoxypentosenucleic acid during maturation and fertilization of Fasciola hepatica egg. Comptes Rendus des Seances de la Societe de Biologie et de Ses Filiales 149(9-10): 1066-1069

Aleksandrov S.N., 1972: The blastomogenic effect of ionizing radiation. Voprosy Onkologii (stsburg). 18(7): 108-117

Chen, J.; Lalancette, R.A.; Jäkle, F., 2013: Synthesis and Lewis acid properties of a ferrocene-based planar-chiral borenium cation. The first planar chiral ferrocenylborenium species (pR)-3(+) is obtained in the enantiopure form by halide abstraction from the corresponding chloroborane adduct (pR)-2 using Krossing's salt. Competition experiments suggest that the Lewis aci...

Tros D.I.arduya, C.; Arangoa, M.A.; Moreno Aliaga, M.J.; Duzgunes, N., 2002: Enhanced gene delivery in vitro and in vivo by improved transferrin-lipoplexes. Cationic liposomes and the complexes they form with DNA (lipoplexes) constitute the most promising alternative to the use of viral vectors for gene therapy. One of the limitations to their application in vivo, however, is the inhibition of gene de...

Chen, Y.; Knappe, D.R.U.; Barlaz, M.A., 2004: Effect of cellulose/hemicellulose and lignin on the bioavailability of toluene sorbed to waste paper. Paper constitutes about 38% of municipal solid waste, much of which is disposed of in landfills. Sorption to such lignocellulosic materials may limit the bioavailability of organic contaminants in landfills. The objective of this study was to iden...

Chmelev, N.A.; Meyer, A.; Raguet, D.F.; Maksoudov, G.B.; Lombardi, N., 1967: Evaluation of the problem posed by tuberculosis. Radiophotographic survey in Mali. Revue de Tuberculose et de Pneumologie 31(4): 532-542