New nitazoxanide derivatives: design, synthesis, biological evaluation, and molecular docking studies as antibacterial and antimycobacterial agents

Saleh, Mahmoud; Mostafa, Yaser A.; Kumari, Jyothi; Thabet, Momen M.; Sriram, Dharmarajan; Kandeel, Mahmoud; Abdu-Allah, Hajjaj H. M.

doi:10.1039/d3md00449j

RSC Med. Chem.

2023

DOI: 10.1039/d3md00449j

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New nitazoxanide derivatives: design, synthesis, biological evaluation, and molecular docking studies as antibacterial and antimycobacterial agents

Mahmoud Saleh,

Yaser A. Mostafa,

Jyothi Kumari

et al.

Abstract: Multifunctional nitazoxanide derivatives were designed, synthesized and screened as multitarget antibacterial and mycobacterial agents.

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2024

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Cyclization of acyl thiosemicarbazides led to new Helicobacter pylori α‐carbonic anhydrase inhibitors

Gumus,

D'Agostino,

Puca

et al. 2024

Archiv der Pharmazie

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The eradication of Helicobacter pylori, the etiologic agent of gastric ulcer and adenocarcinoma, is a big concern in clinics due to the increasing drug resistance phenomena and the limited number of efficacious treatment options. The exploitation of the H. pylori carbonic anhydrases (HpCAs) as promising pharmacological targets has been validated by the antibacterial activity of previously reported CA inhibitors due to the role of these enzymes in the bacterium survival in the gastric mucosa. The development of new HpCA inhibitors seems to be on the way to filling the existing antibiotics gap. Due to the recent evidence on the ability of the coumarin scaffold to inhibit microbial α‐CAs, a large library of derivatives has been developed by means of a pH‐regulated cyclization reaction of coumarin‐bearing acyl thiosemicarbazide intermediates. The obtained 1,3,4‐thiadiazoles (10–18a,b) and 1,2,4‐triazole‐3‐thiones (19–26a,b) were found to strongly and selectively inhibit HpαCA and computational studies were fundamental to gaining an understanding of the interaction networks governing the enzyme–inhibitor complex. Antibacterial evaluations on H. pylori ATCC 43504 highlighted some compounds that maintained potency on a resistant clinical isolate. Also, their combinations with metronidazole decreased both the minimal inhibitory concentration and minimal bactericidal concentration values of the antibiotic, with no synergistic effect.

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Cyclization of acyl thiosemicarbazides led to new Helicobacter pylori α‐carbonic anhydrase inhibitors

Gumus,

D'Agostino,

Puca

et al. 2024

Archiv der Pharmazie

View full text Add to dashboard Cite

show abstract

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New nitazoxanide derivatives: design, synthesis, biological evaluation, and molecular docking studies as antibacterial and antimycobacterial agents

Abstract: Multifunctional nitazoxanide derivatives were designed, synthesized and screened as multitarget antibacterial and mycobacterial agents.

Cited by 1 publication

References 81 publications

Cyclization of acyl thiosemicarbazides led to new Helicobacter pylori α‐carbonic anhydrase inhibitors

Cyclization of acyl thiosemicarbazides led to new Helicobacter pylori α‐carbonic anhydrase inhibitors

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