Synthesis, antibacterial properties and 2D-QSAR studies of quinolone-triazole conjugates

Hassan M. Faidallah; Adel S. Girgis; Anand D. Tiwari; Hitesh H. Honkanadavar; Sean J. Thomas; Ahmed Samir; Atef Kalmouch; Khalid A. Alamry; Khalid A. Khan; Tarek S. Ibrahim; Amany M.M. AL-Mahmoudy; Abdullah M. Asiri; Siva S. Panda

doi:10.1016/j.ejmech.2017.10.042

Synthesis, antibacterial properties and 2D-QSAR studies of quinolone-triazole conjugates

Hassan M. Faidallah, Adel S. Girgis, Anand D. Tiwari, Hitesh H. Honkanadavar, Sean J. Thomas, Ahmed Samir, Atef Kalmouch, Khalid A. Alamry, Khalid A. Khan, Tarek S. Ibrahim, Amany M.M. AL-Mahmoudy, Abdullah M. Asiri, Siva S. Panda

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52 Scopus citations

Abstract

A set of 1,2,3-triazole incorporated quinolone antibiotic conjugates 10–15, 17–19 were synthesized via microwave assisted click chemistry technique. Some of the aryl-substituted conjugates 17–19 show promising antibacterial properties against the tested Gram-positive (S. aureus and S. pyogenes) and Gram-negative bacteria (S. typhi) with potency higher than that of the parent antibiotics 1–3. 2D-QSAR modeling supports the observed biological properties.

Original language	English (US)
Pages (from-to)	1524-1534
Number of pages	11
Journal	European Journal of Medicinal Chemistry
Volume	143
DOIs	https://doi.org/10.1016/j.ejmech.2017.10.042
State	Published - Jan 1 2018

Keywords

1,2,3-Triazole
Antibacterial
Conjugate
QSAR
Quinolone

ASJC Scopus subject areas

Pharmacology
Drug Discovery
Organic Chemistry

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10.1016/j.ejmech.2017.10.042

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Faidallah, H. M., Girgis, A. S., Tiwari, A. D., Honkanadavar, H. H., Thomas, S. J., Samir, A., Kalmouch, A., Alamry, K. A., Khan, K. A., Ibrahim, T. S., AL-Mahmoudy, A. M. M., Asiri, A. M., & Panda, S. S. (2018). Synthesis, antibacterial properties and 2D-QSAR studies of quinolone-triazole conjugates. European Journal of Medicinal Chemistry, 143, 1524-1534. https://doi.org/10.1016/j.ejmech.2017.10.042

Faidallah, HM, Girgis, AS, Tiwari, AD, Honkanadavar, HH, Thomas, SJ, Samir, A, Kalmouch, A, Alamry, KA, Khan, KA, Ibrahim, TS, AL-Mahmoudy, AMM, Asiri, AM & Panda, SS 2018, 'Synthesis, antibacterial properties and 2D-QSAR studies of quinolone-triazole conjugates', European Journal of Medicinal Chemistry, vol. 143, pp. 1524-1534. https://doi.org/10.1016/j.ejmech.2017.10.042

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abstract = "A set of 1,2,3-triazole incorporated quinolone antibiotic conjugates 10–15, 17–19 were synthesized via microwave assisted click chemistry technique. Some of the aryl-substituted conjugates 17–19 show promising antibacterial properties against the tested Gram-positive (S. aureus and S. pyogenes) and Gram-negative bacteria (S. typhi) with potency higher than that of the parent antibiotics 1–3. 2D-QSAR modeling supports the observed biological properties.",

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author = "Faidallah, {Hassan M.} and Girgis, {Adel S.} and Tiwari, {Anand D.} and Honkanadavar, {Hitesh H.} and Thomas, {Sean J.} and Ahmed Samir and Atef Kalmouch and Alamry, {Khalid A.} and Khan, {Khalid A.} and Ibrahim, {Tarek S.} and AL-Mahmoudy, {Amany M.M.} and Asiri, {Abdullah M.} and Panda, {Siva S.}",

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year = "2018",

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doi = "10.1016/j.ejmech.2017.10.042",

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AU - Faidallah, Hassan M.

AU - Girgis, Adel S.

AU - Tiwari, Anand D.

AU - Honkanadavar, Hitesh H.

AU - Thomas, Sean J.

AU - Samir, Ahmed

AU - Kalmouch, Atef

AU - Alamry, Khalid A.

AU - Khan, Khalid A.

AU - Ibrahim, Tarek S.

AU - AL-Mahmoudy, Amany M.M.

AU - Asiri, Abdullah M.

AU - Panda, Siva S.

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AB - A set of 1,2,3-triazole incorporated quinolone antibiotic conjugates 10–15, 17–19 were synthesized via microwave assisted click chemistry technique. Some of the aryl-substituted conjugates 17–19 show promising antibacterial properties against the tested Gram-positive (S. aureus and S. pyogenes) and Gram-negative bacteria (S. typhi) with potency higher than that of the parent antibiotics 1–3. 2D-QSAR modeling supports the observed biological properties.

KW - 1,2,3-Triazole

KW - Antibacterial

KW - Conjugate

KW - QSAR

KW - Quinolone

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JO - European Journal of Medicinal Chemistry

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Synthesis, antibacterial properties and 2D-QSAR studies of quinolone-triazole conjugates

Abstract

Keywords

ASJC Scopus subject areas

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