Version 1
: Received: 21 December 2023 / Approved: 22 December 2023 / Online: 22 December 2023 (14:33:06 CET)
Version 2
: Received: 24 February 2024 / Approved: 26 February 2024 / Online: 26 February 2024 (12:02:52 CET)
How to cite:
Zampieri, E.H.; Dos Anjos, L.R.; Santiago, P.H.D.O.; Nascimento, T.R.D.S.; Ellena, J.; González, E.R.P. Study of the Conformation of Bromated Guanidines with Potential Anti-leishmania Activity. Preprints2023, 2023121728. https://doi.org/10.20944/preprints202312.1728.v2
Zampieri, E.H.; Dos Anjos, L.R.; Santiago, P.H.D.O.; Nascimento, T.R.D.S.; Ellena, J.; González, E.R.P. Study of the Conformation of Bromated Guanidines with Potential Anti-leishmania Activity. Preprints 2023, 2023121728. https://doi.org/10.20944/preprints202312.1728.v2
Zampieri, E.H.; Dos Anjos, L.R.; Santiago, P.H.D.O.; Nascimento, T.R.D.S.; Ellena, J.; González, E.R.P. Study of the Conformation of Bromated Guanidines with Potential Anti-leishmania Activity. Preprints2023, 2023121728. https://doi.org/10.20944/preprints202312.1728.v2
APA Style
Zampieri, E.H., Dos Anjos, L.R., Santiago, P.H.D.O., Nascimento, T.R.D.S., Ellena, J., & González, E.R.P. (2024). Study of the Conformation of Bromated Guanidines with Potential Anti-leishmania Activity. Preprints. https://doi.org/10.20944/preprints202312.1728.v2
Chicago/Turabian Style
Zampieri, E.H., Javier Ellena and Eduardo René Pérez González. 2024 "Study of the Conformation of Bromated Guanidines with Potential Anti-leishmania Activity" Preprints. https://doi.org/10.20944/preprints202312.1728.v2
Abstract
Leishmaniasis are neglected diseases that affect regions such as South Asia, South Africa and Latin America, less developed regions. Current treatment, for cutaneous, mucocutaneous and visceral leishmaniosis, which are the main forms of the disease, is based on the administration of pentavalent antimonial and amphotericin B. However, these drugs have low efficacy and high toxicity. For this reason, the search for new treatments for this disease is necessary, based on studies of new molecules and their conformations. The research proposed the conformational study of brominated guanidine compounds with potential antileishmanial activity using Nuclear Magnetic Resonance (NMR) and X-ray diffraction (XRD) techniques. The present study involves the bro-minated molecules, LQOF-G2, LQOF-G30, LQOF-G35 and LQOF-G35-Br. The later was synthesized by the reaction of LQOF-G35 with NBS under IR irradiation at 120 Watts of potency and dichloro-methane as solvent by 12-h of exposition. The obtained results demonstrated the efficiency of the bromination method, since two bromines atoms entered the molecule. Furthermore, NMR analysis showed the occurrence of a conformational change from Z to E when compound LQOF-G35 was brominated to LQOF-G35-Br. This feature was well confirmed by comparative DRX study of the LQOF-G35 and LQOF-G35-Br compounds. The antileishmanial activity of LQOF-G2 e LQOF-G35 motivated the synthesis of new brominated compounds LQOF-G30 e LQOF-G35-Br.
Keywords
Guanidines compounds; Leishmaniasis; Bromination; NBS; X-ray and NMR conformational study.
Subject
Chemistry and Materials Science, Analytical Chemistry
Copyright:
This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.
,
,
,
