Synthesis and antiprotozoal evaluation of benzothiazolopyrroloquinoxalinones, analogues of kuanoniamine A

Tapia, Ricardo A.

doi:10.1016/s0968-0896(03)00311-0

Cited by 27 publications

(9 citation statements)

References 9 publications

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“…Authors neither discussed any structure activity relationship points nor they proposed any mechanism behind antiprotozoal activity. Although lipophilicity was mentioned as an important factor behind antiprotozoal activity while the presence of boc group and quinoneimine function might be responsible for antiprotozoal activity [52,53] .…”

Section: Kuanoniamine Analoguesmentioning

confidence: 99%

A mini review on pyridoacridines: Prospective lead compounds in medicinal chemistry

Sharma

Kumar

2015

Journal of Advanced Research

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Section: Kuanoniamine Analoguesmentioning

confidence: 99%

A mini review on pyridoacridines: Prospective lead compounds in medicinal chemistry

Sharma

Kumar

2015

Journal of Advanced Research

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“…Some heterocyclic quinones have been reported to be active in vitro against virulent strains of Leishmania sp. (Tournaire et al, 1996;Valderrama et al, 1999;Tapia et al, 2003a;Tapia et al, 2002b;Tapia et al, 2003b), it is why we have explored the antileishmanial activity of various quinonic compounds. We have performed in vitro tests in order to identify three-dimensional structural similarities between these compounds that may explain their potency against L. donovani, or L. major or both strains.…”

Section: Molecular Modeling Studymentioning

confidence: 99%

Antileishmanial activity of polycyclic derivatives

et al. 2005

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Summary :33 polycyclic derivatives have been studied and tested on Leishmania donovani and L. major promastigotes. Their antileishmanial activity was assessed in vitro and an assay of their cytotoxicity was realized on human myelomonocytic cell line. The reference molecules used in the assays were amphotericin B and pentamidine. Among the compounds tested, 29 possess an antileishmanial activity; 25 of those were more active against L. donovani than amphotericin B, and nine were as effective as amphotericin B against L. major. Many synthesized derivatives were more active against L.donovani than against L. major. The cytotoxicity studies have shown that among the thirty-three derivatives tested, 12 molecules have an IC 50 towards THP-1 cells about equal than that reference drugs, the 21 other derivatives are much less toxic. A 3D QSAR study was undertaken and has permitted to predict activity against L. donovani and L. major and to highlight critical area to optimize activity against the two species. Résumé

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“…Many antibiotics and biomolecules containing thiazole and its derivatives are known to have biological importance. The compounds with thiazole ring have applications in pharmacology such as allergies [1], schizophrenia [2], hypertension [3], anti-HIV [4], anti-bacterial [5], anti-thrombotic activity [6], anti-protozoal [7], anti-helminthic [8], antimicrobial [9]. Furthermore, 2-aminothiazoles exhibit potential activity in many human cancer cell lines [10][11][12][13].…”

Section: Introductionmentioning

confidence: 99%

Syntheses, spectral characterization, single crystal X-ray diffraction and computational in gas and solid phases studies on chloro- acetic acid N′-(2- hydroxy-naphthalen- 1-ylmethylene)- N- [4-(3-methyl-3-phenyl-cyclobutyl)-thiazol-2-yl]-hydrazide

2020

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In this study, the molecular structure of single crystal containing Schiff bases has been characterized by X-ray diffraction, NMR, IR and UV-Vis spectral techniques and compared with similar molecules in the literature. For the purpose of supporting X-ray results, geometric parameters and spectroscopic studies of the title compound were theoretically performed by Hartree-Fock and density functional theory methods. In addition, the title compound's molecular energies, Mulliken-ESP-NPA-Hirshfeld charges, molecular electrostatic potential surface, Frontier orbitals and thermodynamic properties to elucidate intermolecular interactions were calculated. All the calculations in gas and solid phases were carried out using Gaussian 09 and Quantum Espresso programs. It was found that the studies of X-ray are more compatible with the calculations made in the solid phase.

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Synthesis and antiprotozoal evaluation of benzothiazolopyrroloquinoxalinones, analogues of kuanoniamine A

Cited by 27 publications

References 9 publications

A mini review on pyridoacridines: Prospective lead compounds in medicinal chemistry

A mini review on pyridoacridines: Prospective lead compounds in medicinal chemistry

Antileishmanial activity of polycyclic derivatives

Syntheses, spectral characterization, single crystal X-ray diffraction and computational in gas and solid phases studies on chloro- acetic acid N′-(2- hydroxy-naphthalen- 1-ylmethylene)- N- [4-(3-methyl-3-phenyl-cyclobutyl)-thiazol-2-yl]-hydrazide

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