
Molecules p. 14711 - 14725 (2013)
Update date:2022-07-29
Topics:
Ali, Shaukat
Rasool, Nasir
Ullah, Aman
Nasim, Faiz-Ul-Hassan
Yaqoob, Asma
Zubair, Muhammad
Rashid, Umer
Riaz, Muhammad
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-Formylthiophene- 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-fluorophenyl) thiophene-2-carbaldehyde (2i) exhibited a superior haemolytic action and an outstanding urease inhibition, showing an IC50 value of 27.1 μg/mL.
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