Effect of Some Synthesized Pyrrolidines in Growth of L. infantum Promastigotes
Article Sidebar
Main Article Content
Abstract
In this research, three pyrrolidine compounds (P1-P3) were synthesized and then tested for efficacy against L. infantum promastigotes in vitro.
The study included preparation of some chalcones and schiff bases then the condensation of both to get the pyrrolidines and studying the effect of pyrrolidine compounds in growth, generation number and time of parasites. They determined using concentrations between (5-30) μg/ml. The effect of the compounds was found to be important to the parasite growth as the more the concentration the less the growth, generation number and increased the generation time. At the logarithmic phase, the LD50 were (10), (20) and (30)μg/ml for (P1-P3) compounds, respectively.
Article Details
This work is licensed under a Creative Commons Attribution 4.0 International License.
Tikrit Journal of Pure Science is licensed under the Creative Commons Attribution 4.0 International License, which allows users to copy, create extracts, abstracts, and new works from the article, alter and revise the article, and make commercial use of the article (including reuse and/or resale of the article by commercial entities), provided the user gives appropriate credit (with a link to the formal publication through the relevant DOI), provides a link to the license, indicates if changes were made, and the licensor is not represented as endorsing the use made of the work. The authors hold the copyright for their published work on the Tikrit J. Pure Sci. website, while Tikrit J. Pure Sci. is responsible for appreciate citation of their work, which is released under CC-BY-4.0, enabling the unrestricted use, distribution, and reproduction of an article in any medium, provided that the original work is properly cited.
References
1. J. Alvar, I. D. Vales, C. Bern, M. Herrero, P. Desjeux, and J. Cano, Leishmaniasis worldwide and global estimates of its incidence. PloS One. Vol. 7(5), (2012). e3561 http://dx.doi.org.
2. S. Gupta, and N. Shakya, Visceral Leishmaniasis: Experimental methods for drug discovery. Indian J. Med. Res. Vol. 133, (2011). pp 27-29.
3. R. J. A Postigo, Leishmaniasis in the World Health Organization Eastern Mediterranean Region. Intern. J. of Antimicrobial Ag. Vol. 36, (2010). pp 62-65.
4. J. P. Menezes, C. E. Guedes, A. L. Petersen, D. B. Fraga, and P. S. Veras, Advances in development of new treatment for Leishmaniasis. Bio. Med. Res. Int. (2015). 11 page.
(http://dx.doi.org/10.1155/2015/815023).
5. M. S. Hussein, Synthesis, characterization and antibacterial evaluation of some substituted Pyrrolidines. Chem. Sc. Int. J. Vol. 17(2), (2016). Pp 1-8.
6. M. Narayana Babu, L. Sharma, and D. Madhavan, Synthesis and antimicrobial activity of some Novel pyrrolidine derivatives. Int. J. of Chem. Tech. Res. Vol. 4(3), ( 2012). pp 403-409.
7. P. Elías-Rodríguez, E. Moreno-Clavijo, S. Carrión-Jiménez, A. T. Carmona, A. J. Moreno-Vargas, I. Caffa, F. Montecucco, M. Cea, A. Nencioni, and I. Robinaa, Synthesis and cancer growth inhibitory activities of 2-fatty-alkylated pyrrolidine-3,4-diol derivatives. ARKIVOC Vol. 3, (2014). pp 197-214.
8. H. Fiaux, F. Popowycz, S. Favre, C. Schutz, P. Vogel, S. Gerber-Lemaire, and L. Juillerat-Jeanneret, Functionalized pyrrolidines inhibit α-mannosidase activity and growth of Human glioblastoma and melanoma cells. J. Med. Chem. Vol. 48, (2005). pp 4237-4246.
9. T. M. Chapman, I. G. Davies, B. Gu, T. M. Block, D. I. C. Scopes, P. A. Hay, S. M. Courtney, L. A. McNeill, C. J. Schofield, and B. G. Davis, Glyco- and peptidomimetics from three-component Joullie´-Ugi coupling show selective antiviral activity. J. Am. Chem. Soc. Vol. 127, (2005). pp 506-507.
10. A. Vogel, "Practical Organic Chemistry". Longmans, 5th ed. (1989). pp 1034.
11. L. Bin, L. Xi-Qun, Z. Wen-Jieomed, and Z. Me-Yun, Synthesis of ionic liquid supported schiff bases. ARKIVOC. Vol, 9 (2009). pp 165-171.
12. K. Popandova-Yambolieva, and C. Ivanov, Synthesis of new spiropyrrolidines and michael addition products using phase transfer catalyzed addition of schiff bases to 9-arylmethylenefluorenes. Chemica. Scripta. Vol. 29, (1989). pp 269-271.
13. E. J. Tobie, T. V. Brand, and B. Mehlman, Cultural and physiological observations on Trypanosoma rhodesiense and Trypanosoma gambiense. J. Parasitol., Vol. 36, (1950). pp 48 – 54.
14. Benjamin, C. L. and G.R. German, Students study guide microbiology. (1993). Concepts and Application. Mc GPAW-HILL. Book Company.
15. A. Indrayan, and S. B. Sarmukaddam, Medical Biostatics. (2001). Morcel Dekker, Inc, USA.: pp. 299, 303,405.
16. T.W.J.Y. Qitto, Synthesis of some fused heterocycles and study their expected biological activity. M. Sc. thesis. College of Science. Mosul University. (2007). Mosul. Iraq.
17. C. B. Patil, S.K. Mohajan, and S. A. Katli, Chalcone: A versatile molecule. J. Pharm. Sci. and Res. Vol. 1(3), (2009). pp 11-22.
18. A.J. AL-Hamdany, A. M. Dabbagh. and O. A. Shareef, Synthesis of Spiropyrrolidines via 1, 3 Anionic Cycloaddition. Raf. J. Sci., Vol. 23(3), (2012). pp 94-105.
19. A.A. Al-Kadhimi1, A.J. AL-Hamdany, and S.S. Jasim, Synthesis and Antibacterial Evaluation of Bis-pyrrolidinyl Ketones. RJPBCS. Vol. 3(1), (2012). pp 908-921.
20. G. H. Schmidt, "Organic chemistry". University of Toronot. Jamis M. Smith Inc. (1996). USA. pp 1063.
21. V. Alptuzun, G. Cakiroglu, M. Emin-Limoncu, B. Erac, M. Hosgor-Limoncu, and E. Erciyas, Synthesis and antileishmaniasis activity of novel pyridinium-hydrazone derivatives. J. of Enz. Inh. and Med. Chem. Vol. 28(5), (2013). pp 960-967.
22. V. D. S. Carrara, E. F. Cunha-Junior, E. C. Terres-Santos, A. G. Corre, L. Monteiro, I. G. Demarchi, M. V. C. Lonardoni, and D. A. G. Cortez, Antileishmanial activity of amides from Piper amalago and synthetic analogs. Brazilian J. of Pharmacognosy. Vol. 23(3), (2013). pp 447-454.
23. A. Mendoza, S. Perez-Silanes, M. Quiliano, A. Pabon, G. Gonzales, G. Garavito, M. zimic, A. Vaisberg, I. Aldana, A. Mongo, and E. Deharo, Aryl piprazine and pyrrolidine as antimalarial agents. Synthesis and investigation of structure-activity relationships. Vol. 128(2), (2011). pp 97-103.
24. A. Buchynskyy, J. R. Gillespie, Z. M. Herbst, R. M. Ranade, F. S. Buckner, and M. H. Gelb, 1‑Benzyl-3-aryl-2-thiohydantoin derivatives as new anti-Trypanosoma brucei agents: SAR and In Vivo efficacy. ACS Med. Chem. Lett. Vol. 8, (2017). pp 886−891.
25. S. P. Wagh, Synthesis of 3,4-Diylidine and N-substituted pyrrolidines and its anti-microbial activity. Am. J. Pharm. Tech. Res. Vol. 5(3), (2015). pp 153-159.
26. H. L. Al-Hayali, M. H. Al-Hammoshi, and T. M. Al-Mushhadani, Synthesis and study effects of 3,4-dihydro-4-(p-anisyl)-6-phenyl pyrimidine-(1H)-one on growth and morphology of Leishmania tropica promastigotes in vitro. Tikrit J. of Pure Sci. Vol. 13(3), (2008). pp 209-218.
27. M.H. Al-Hammoshi, Effects of some heterocyclic compounds on growth and metabolism of Leishmania tropica promastigotes. Ph. D thesis. College of Science. Mosul University. (2006). Mosul. Iraq.