伪2 Adrenoceptor Agonists as Potential Analgesic Agents. 3. Imidazolylmethylthiophenes was written by Boyd, Robert E.;Rasmussen, C. Royce;Press, Jeffery B.;Raffa, Robert B.;Codd, Ellen E.;Connelly, Charlene D.;Li, Quan S.;Martinez, Rebecca P.;Lewis, Martin A.;Almond, Harold R.;Reitz, Allen B.. And the article was included in Journal of Medicinal Chemistry in 2001.COA of Formula: C5H2Cl2O2S This article mentions the following:
A series of imidazolylmethylthiophenes has been prepared and evaluated as ligands for the 伪2 adrenoceptor. These compounds were tested in two animal models that are predictive of analgesic activity in humans. The 3-thienyl compounds were generally the most potent, particularly those with substitution in the 4-position. A subset of the most active compounds was further evaluated for adverse cardiovascular effects in the anesthetized rat model. In addition to excellent binding at the 伪2D adrenoceptor, the 4-bromo analogs I [R = H, Me] were very active in the rat abdominal irritant test (RAIT) with ED50 doses of 0.38 and 0.31 mg/kg, resp. A pharmacophore model based on the biol. activity of the present series, dexmedetomidine and its conformationally restrained analogs was constructed. In the experiment, the researchers used many compounds, for example, 2,5-Dichlorothiophene-3-carboxylic acid (cas: 36157-41-2COA of Formula: C5H2Cl2O2S).
2,5-Dichlorothiophene-3-carboxylic acid (cas: 36157-41-2) belongs to organic chlorides. Organochlorines stimulate the central nervous system and cause convulsions, tremor, nausea, and mental confusion. Examples are dichlorodiphenyltrichloroethane (DDT), chlordane, lindane, endosulfan, and dieldrin. Alkyl chlorides readily react with amines to give substituted amines. Alkyl chlorides are substituted by softer halides such as the iodide in the Finkelstein reaction.COA of Formula: C5H2Cl2O2S
Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics