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Exploring the antimicrobial and cytotoxic potential of novel chloroquine analogues.
Islam, Shamsul; Shahzad, Sohail A; Ismail, Tariq; Sherani, Usman As; Khan, Kashif M; Fatima, Nighat; Khan, Shujaat A; Mannan, Abdul.
Afiliação
  • Islam S; Department of Pharmacy, COMSATS University Islamabad, Abbottabad Campus, Abbottabad, 22060, Pakistan.
  • Shahzad SA; Department of Chemistry, COMSATS University Islamabad, Abbottabad Campus, Abbottabad, 22060, Pakistan.
  • Ismail T; Department of Pharmacy, COMSATS University Islamabad, Abbottabad Campus, Abbottabad, 22060, Pakistan.
  • Sherani UA; Department of Pharmacy, COMSATS University Islamabad, Abbottabad Campus, Abbottabad, 22060, Pakistan.
  • Khan KM; Institute of Pharmaceutical Sciences, University of Veterinary & Animal Sciences, Lahore, 54000, Pakistan.
  • Fatima N; Department of Pharmacy, COMSATS University Islamabad, Abbottabad Campus, Abbottabad, 22060, Pakistan.
  • Khan SA; Department of Pharmacy, COMSATS University Islamabad, Abbottabad Campus, Abbottabad, 22060, Pakistan.
  • Mannan A; Department of Pharmacy, COMSATS University Islamabad, Abbottabad Campus, Abbottabad, 22060, Pakistan.
Future Med Chem ; 16(8): 737-749, 2024.
Article em En | MEDLINE | ID: mdl-38456272
ABSTRACT

Aim:

To synthesize novel chloroquine analogues and evaluate them for antimicrobial and cytotoxic potential.

Methods:

Novel analogues were synthesized from chloroquine by nucleophilic substitution reaction at the 4-amino position.

Results:

Analogue CS1 showed maximum antimicrobial potential (30.3 ± 0.15 mm zone) against Pseudomonas aeruginosa and produced a 19.2 ± 0.21 mm zone against Candida albicans, while CS0 produced no zone at the same concentration. Analogue CS9 has excellent cytotoxic potential (HeLa cell line), showing 100% inhibition (IC50 = 8.9 ± 1.2 µg/ml), compared with CS0 (61.9% inhibition at 30 µg/ml).

Conclusion:

These synthesized chloroquine analogues have excellent activity against different microbial strains and cervical cancer cell lines (HeLa) compared with their parent molecule.
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Texto completo: 1 Base de dados: MEDLINE Assunto principal: Pseudomonas aeruginosa / Candida albicans / Testes de Sensibilidade Microbiana / Cloroquina / Antineoplásicos Limite: Humans Idioma: En Ano de publicação: 2024 Tipo de documento: Article

Texto completo: 1 Base de dados: MEDLINE Assunto principal: Pseudomonas aeruginosa / Candida albicans / Testes de Sensibilidade Microbiana / Cloroquina / Antineoplásicos Limite: Humans Idioma: En Ano de publicação: 2024 Tipo de documento: Article