The anti-amoebic potential of carboxamide derivatives containing sulfonyl or sulfamoyl moieties against brain-eating Naegleria fowleri (2024)

Akbar, N., Siddiqui, R., El-Gamal, M. I., Zaraei, S.-O., Alawfi, B. S., & Khan, N. A. (2023). The anti-amoebic potential of carboxamide derivatives containing sulfonyl or sulfamoyl moieties against brain-eating Naegleria fowleri. Parasitology Research, 122(11), 2539-2548. https://doi.org/10.1007/s00436-023-07953-w

Akbar, Noor ; Siddiqui, Ruqaiyyah ; El-Gamal, Mohammed I. et al. / The anti-amoebic potential of carboxamide derivatives containing sulfonyl or sulfamoyl moieties against brain-eating Naegleria fowleri. In: Parasitology Research. 2023 ; Vol. 122, No. 11. pp. 2539-2548.

@article{6cf3f0c2c6224adfafc77aaba8916abb,

title = "The anti-amoebic potential of carboxamide derivatives containing sulfonyl or sulfamoyl moieties against brain-eating Naegleria fowleri",

abstract = "Naegleria fowleri is a free-living thermophilic flagellate amoeba that causes a rare but life-threatening infection called primary amoebic meningoencephalitis (PAM), with a very high fatality rate. Herein, the anti-amoebic potential of carboxamide derivatives possessing sulfonyl or sulfamoyl moiety was assessed against pathogenic N. fowleri using amoebicidal, cytotoxicity and cytopathogenicity assays. The results from amoebicidal experiments showed that derivatives dramatically reduced N. fowleri viability. Selected derivatives demonstrated IC50 values at lower concentrations; 1j showed IC50 at 24.65 μM, while 1k inhibited 50% amoebae growth at 23.31 μM. Compounds with significant amoebicidal effects demonstrated limited cytotoxicity against human cerebral microvascular endothelial cells. Finally, some derivatives mitigated N. fowleri-instigated host cell death. Ultimately, this study demonstrated that 1j and 1k exhibited potent anti-amoebic activity and ought to be looked at in future studies for the development of therapeutic anti-amoebic pharmaceuticals. Further investigation is required to determine the clinical relevance of our findings.",

keywords = "Humans, Naegleria fowleri, Amoeba, Endothelial Cells, Amebicides/pharmacology, Brain/pathology, Central Nervous System Protozoal Infections/drug therapy",

author = "Noor Akbar and Ruqaiyyah Siddiqui and El-Gamal, {Mohammed I.} and Seyed-Omar Zaraei and Alawfi, {Bader S.} and Khan, {Naveed Ahmed}",

note = "{\textcopyright} 2023. The Author(s), under exclusive licence to Springer-Verlag GmbH Germany, part of Springer Nature.",

year = "2023",

month = nov,

doi = "10.1007/s00436-023-07953-w",

language = "English",

volume = "122",

pages = "2539--2548",

journal = "Parasitology Research",

issn = "0932-0113",

publisher = "Springer",

number = "11",

}

Akbar, N, Siddiqui, R, El-Gamal, MI, Zaraei, S-O, Alawfi, BS & Khan, NA 2023, 'The anti-amoebic potential of carboxamide derivatives containing sulfonyl or sulfamoyl moieties against brain-eating Naegleria fowleri', Parasitology Research, vol. 122, no. 11, pp. 2539-2548. https://doi.org/10.1007/s00436-023-07953-w

The anti-amoebic potential of carboxamide derivatives containing sulfonyl or sulfamoyl moieties against brain-eating Naegleria fowleri. / Akbar, Noor; Siddiqui, Ruqaiyyah; El-Gamal, Mohammed I. et al.
In: Parasitology Research, Vol. 122, No. 11, 11.2023, p. 2539-2548.

Research output: Contribution to journal › Article › peer-review

TY - JOUR

T1 - The anti-amoebic potential of carboxamide derivatives containing sulfonyl or sulfamoyl moieties against brain-eating Naegleria fowleri

AU - Akbar, Noor

AU - Siddiqui, Ruqaiyyah

AU - El-Gamal, Mohammed I.

AU - Zaraei, Seyed-Omar

AU - Alawfi, Bader S.

AU - Khan, Naveed Ahmed

N1 - © 2023. The Author(s), under exclusive licence to Springer-Verlag GmbH Germany, part of Springer Nature.

PY - 2023/11

Y1 - 2023/11

N2 - Naegleria fowleri is a free-living thermophilic flagellate amoeba that causes a rare but life-threatening infection called primary amoebic meningoencephalitis (PAM), with a very high fatality rate. Herein, the anti-amoebic potential of carboxamide derivatives possessing sulfonyl or sulfamoyl moiety was assessed against pathogenic N. fowleri using amoebicidal, cytotoxicity and cytopathogenicity assays. The results from amoebicidal experiments showed that derivatives dramatically reduced N. fowleri viability. Selected derivatives demonstrated IC50 values at lower concentrations; 1j showed IC50 at 24.65 μM, while 1k inhibited 50% amoebae growth at 23.31 μM. Compounds with significant amoebicidal effects demonstrated limited cytotoxicity against human cerebral microvascular endothelial cells. Finally, some derivatives mitigated N. fowleri-instigated host cell death. Ultimately, this study demonstrated that 1j and 1k exhibited potent anti-amoebic activity and ought to be looked at in future studies for the development of therapeutic anti-amoebic pharmaceuticals. Further investigation is required to determine the clinical relevance of our findings.

AB - Naegleria fowleri is a free-living thermophilic flagellate amoeba that causes a rare but life-threatening infection called primary amoebic meningoencephalitis (PAM), with a very high fatality rate. Herein, the anti-amoebic potential of carboxamide derivatives possessing sulfonyl or sulfamoyl moiety was assessed against pathogenic N. fowleri using amoebicidal, cytotoxicity and cytopathogenicity assays. The results from amoebicidal experiments showed that derivatives dramatically reduced N. fowleri viability. Selected derivatives demonstrated IC50 values at lower concentrations; 1j showed IC50 at 24.65 μM, while 1k inhibited 50% amoebae growth at 23.31 μM. Compounds with significant amoebicidal effects demonstrated limited cytotoxicity against human cerebral microvascular endothelial cells. Finally, some derivatives mitigated N. fowleri-instigated host cell death. Ultimately, this study demonstrated that 1j and 1k exhibited potent anti-amoebic activity and ought to be looked at in future studies for the development of therapeutic anti-amoebic pharmaceuticals. Further investigation is required to determine the clinical relevance of our findings.

KW - Humans

KW - Naegleria fowleri

KW - Amoeba

KW - Endothelial Cells

KW - Amebicides/pharmacology

KW - Brain/pathology

KW - Central Nervous System Protozoal Infections/drug therapy

U2 - 10.1007/s00436-023-07953-w

DO - 10.1007/s00436-023-07953-w

M3 - Article

C2 - 37665414

SN - 0932-0113

VL - 122

SP - 2539

EP - 2548

JO - Parasitology Research

JF - Parasitology Research

IS - 11

ER -

Akbar N, Siddiqui R, El-Gamal MI, Zaraei SO, Alawfi BS, Khan NA. The anti-amoebic potential of carboxamide derivatives containing sulfonyl or sulfamoyl moieties against brain-eating Naegleria fowleri. Parasitology Research. 2023 Nov;122(11):2539-2548. Epub 2023 Sept 4. doi: 10.1007/s00436-023-07953-w