Daoud N. E., Çevik U. A., Gül Ü. D., Kaplancıklı Z. A.
MEDICINAL CHEMISTRY, cilt.22, ss.1-10, 2026 (SCI-Expanded, Scopus)
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Yayın Türü:
Makale / Tam Makale
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Cilt numarası:
22
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Basım Tarihi:
2026
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Doi Numarası:
10.2174/0115734064437065251129131536
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Dergi Adı:
MEDICINAL CHEMISTRY
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Derginin Tarandığı İndeksler:
Scopus, Science Citation Index Expanded (SCI-EXPANDED), Chemical Abstracts Core, EMBASE, MEDLINE
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Sayfa Sayıları:
ss.1-10
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Bilecik Şeyh Edebali Üniversitesi Adresli:
Evet
Özet
Introduction:
Infections caused by multidrug-resistant bacteria and fungi pose an increasing
global threat, underscoring the urgent need for new drugs with novel structures and mechanisms
of action.
Methods:
A new series of triazole–thiadiazole hybrid derivatives (7a-7i) was designed, synthesized,
and structurally characterized using 1H NMR and 13C NMR spectroscopy. The antimicrobial efficacy
of the synthesized compounds was evaluated in vitro against a panel of clinically significant,
resistant bacterial and fungal strains.
Results:
Compound 7a demonstrated the highest potency against E. coli with a MIC of 3.90 μg/mL,
followed by compound 7b (7.81 μg/mL) and compound 7e (31.25 μg/mL). Antifungal screening
revealed moderate activity against the resistant strains C. krusei ATCC 6258 and C. albicans ATCC
24433. Compound 7a inhibited C. krusei with an MIC of 62.5 μg/mL, while compounds 7e and 7h
exhibited MIC values of 125 μg/mL against both fungal strains.
Discussion:
Preliminary Structure–Activity Relationship (SAR) analysis suggests that small, hydrophobic
alkylamine substituents significantly enhance antimicrobial activity. In silico ADMET
profiling supported the biological findings, indicating that all compounds fall within acceptable
drug-likeness criteria. Among them, compound 7b emerged as the most promising lead, exhibiting
high oral absorption, good solubility, and permeability, and the lowest predicted cardiotoxicity risk.
Conclusion:
These results suggest that triazole-thiadiazole hybrids, particularly compound 7b,
represent a promising scaffold for the development of new antimicrobial agents.