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Permanent link (DOI): https://doi.org/10.7939/R3NC5SS1R

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Design and synthesis of arylthiophene-2-Carbaldehydes via suzuki-miyaura reactions and their biological evaluation Open Access

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Author or creator
Ali, Shaukat
Rasool, Nasir
Ullah, Aman
Nasim, Faiz-ul-Hassan
Yaqoob, Asma
Zubair, Muhammad
Rashid, Umer
Riaz, Muhammad
Additional contributors
Subject/Keyword
Antioxidant
Pd (0) Catalyzed Suzuki Coupling
Heamolytic
Antiurease
Thiophene
Antibacterial
Activities
Type of item
Journal Article (Published)
Language
English
Place
Time
Description
A series of various novel 4-arylthiophene-2-carbaldehyde compounds were synthesized in moderate to excellent yields via Suzuki-Miyaura cross-coupling with different arylboronic pinacol esters/acids. The synthesized products were screened for their antibacterial, haemolytic, antiurease, and nitric oxide (NO) scavenging capabilities and interestingly, almost all products turned out to have good activities. 3-(5-Formyl-thiophene-3-yl)-5-(trifloromethyl)benzonitrile (2d) revealed excellent antibacterial activity, showing an IC50 value of 29.7 µg/mL against Pseudomonas aeruginosa, compared to the standard drug streptomycin with an IC50 value 35.2 µg/mL and was also found to be the best NO scavenger, with an IC50 value of 45.6 µg/mL. Moreover, 4-(3-chloro-4-fluoro-phenyl)thiophene-2-carbaldehyde (2i) exhibited a superior haemolytic action and an outstanding urease inhibition, showing an IC50 value of 27.1 µg/mL.
Date created
2013
DOI
doi:10.7939/R3NC5SS1R
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Attribution 4.0 International
Citation for previous publication
Ali, S., Rasool, N., Ullah, A., Nasim, F., Yaqoob, A., Zubair, M., Rashid, U., & Riaz, M. (2013). Design and synthesis of arylthiophene-2-Carbaldehydes via suzuki-miyaura reactions and their biological evaluation. Molecules, 18(12), 14711-14725.  http://dx.doi.org/10.3390/molecules181214711

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