Tosh, Dilip K. et al. published their research in European Journal of Medicinal Chemistry in 2022 | CAS: 4298-52-6

2-Ethynylthiophene (cas: 4298-52-6) belongs to benzothiophene derivatives. Benzothiophene scaffolds are of great importance due to its increased presence in bioactive molecules. It has been used as a raw material for the synthesis of biologically active structures and is found in pharmaceuticals such as leukotriene synthesis inhibitors and antifungals, as well as in many natural products.Name: 2-Ethynylthiophene

A3 adenosine receptor agonists containing dopamine moieties for enhanced inter-species affinity was written by Tosh, Dilip K.;Salmaso, Veronica;Campbell, Ryan G.;Rao, Harsha;Bitant, Amelia;Pottie, Eline;Stove, Christophe P.;Liu, Naili;Gavrilova, Oksana;Gao, Zhan-Guo;Auchampach, John A.;Jacobson, Kenneth A.. And the article was included in European Journal of Medicinal Chemistry in 2022.Name: 2-Ethynylthiophene This article mentions the following:

Following our study of 4′-truncated (N)-methanocarba-adenosine derivatives that displayed unusually high mouse (m) A3AR affinity, we incorporated dopamine-related N6 substituents in the full agonist 5′-methylamide series. N6-(2-(4-Hydroxy-3-methoxy-phenyl)ethyl) derivative MRS7618 I displayed Ki (nM) 0.563 at hA3AR (∼20,000-fold selective) and 1.54 at mA3AR. 2-Alkyl ethers maintained A3 affinity, but with less selectivity than 2-alkynes. Parallel functional assays of G protein-dependent and β-arrestin 2 (βarr2)-dependent pathways indicate these are full agonists but not biased. Through use of computational modeling, we hypothesized that Ph OH/OMe groups interact with polar residues, particularly Gln261, on the mA3AR extracellular loops as the basis for the affinity enhancement. Although the pharmacokinetic indicated facile clearance of parent O-Me catechol nucleosides, prolonged mA3AR activation in vivo was observed in a hypothermia model, suggested potential formation of active metabolites through demethylation. Selected analogs induced mouse hypothermia following i.p. injection, indicative of peripheral A3AR agonism in vivo. In the experiment, the researchers used many compounds, for example, 2-Ethynylthiophene (cas: 4298-52-6Name: 2-Ethynylthiophene).

2-Ethynylthiophene (cas: 4298-52-6) belongs to benzothiophene derivatives. Benzothiophene scaffolds are of great importance due to its increased presence in bioactive molecules. It has been used as a raw material for the synthesis of biologically active structures and is found in pharmaceuticals such as leukotriene synthesis inhibitors and antifungals, as well as in many natural products.Name: 2-Ethynylthiophene

Referemce:
Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem