Synthesis, Optimization, ADME Analysis, and Antioxidant Activity of 2-(Arylethynyl)-3-ethynylthiophenes

Kavak E., Algso M., Konus M., Yılmaz C., Lazoğlu A., Karaağaç S., ...Daha Fazla

Russian Journal of Organic Chemistry, cilt.57, sa.1, ss.91-99, 2021 (SCI-Expanded) identifier identifier

  • Yayın Türü: Makale / Tam Makale
  • Cilt numarası: 57 Sayı: 1
  • Basım Tarihi: 2021
  • Doi Numarası: 10.1134/s1070428021010139
  • Dergi Adı: Russian Journal of Organic Chemistry
  • Derginin Tarandığı İndeksler: Science Citation Index Expanded (SCI-EXPANDED), Scopus, Academic Search Premier, Chemical Abstracts Core
  • Sayfa Sayıları: ss.91-99
  • Anahtar Kelimeler: thiophene, coupling reactions, heteroaromatic compounds, ADME, antioxidants
  • Eskişehir Osmangazi Üniversitesi Adresli: Hayır

Özet

© 2021, Pleiades Publishing, Ltd.Abstract: 2,3-Dialkynylthiophene derivatives were synthesized by using regio- andstereocontrolled Pd-catalyzed Sonogashira coupling and desilylation reactions.The synthesized compounds were analyzed in silico for their pharmacokineticparameters, general toxicity, and drug scores. In particular,3-ethynyl-2-(phenylethynyl)thiophene and3-ethynyl-2-[(4-methylphenyl)ethynyl]thiophene were found to have relativelyhigh drug scores and low toxicities. The antioxidant activity of the titlecompounds were evaluated by five different assays.3-Ethynyl-2-(naphthalen-1-ylethynyl)thiophene displayed significant reducing andfree radical scavenging activities.