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

Küçük Resim Yok

Tarih

2021

Dergi Başlığı

Dergi ISSN

Cilt Başlığı

Yayıncı

Maik Nauka/Interperiodica/Springer

Erişim Hakkı

info:eu-repo/semantics/closedAccess

Özet

2,3-Dialkynylthiophene derivatives were synthesized by using regio- and stereocontrolled Pd-catalyzed Sonogashira coupling and desilylation reactions. The synthesized compounds were analyzed in silico for their pharmacokinetic parameters, general toxicity, and drug scores. In particular, 3-ethynyl-2-(phenylethynyl)thiophene and 3-ethynyl-2-[(4-methylphenyl)ethynyl]thiophene were found to have relatively high drug scores and low toxicities. The antioxidant activity of the title compounds were evaluated by five different assays. 3-Ethynyl-2-(naphthalen-1-ylethynyl)thiophene displayed significant reducing and free radical scavenging activities.

Açıklama

Anahtar Kelimeler

thiophene, coupling reactions, heteroaromatic compounds, ADME, antioxidants

Kaynak

Russian Journal of Organic Chemistry

WoS Q Değeri

Q4

Scopus Q Değeri

Q4

Cilt

57

Sayı

1

Künye