Synthesis of novel amide and urea derivatives of thiazol-2-ethylamines and their activity against Trypanosoma brucei rhodesiense was written by Patrick, Donald A.;Wenzler, Tanja;Yang, Sihyung;Weiser, Patrick T.;Wang, Michael Zhuo;Brun, Reto;Tidwell, Richard R.. And the article was included in Bioorganic & Medicinal Chemistry in 2016.COA of Formula: C8H4ClNO This article mentions the following:
2-(2-Benzamido)ethyl-4-phenylthiazole I was one of 1035 mols. (grouped into 115 distinct scaffolds) found to be inhibitory to Trypanosoma brucei, the pathogen causing human African trypanosomiasis, at concentrations below 3.6 μM and nontoxic to mammalian (Huh7) cells in a phenotypic high-throughput screen of a 700,000 compound library performed by the Genomics Institute of the Novartis Research Foundation (GNF). Compound I and 72 analogs were synthesized in this laboratory by one of two general pathways. These plus 10 com. available analogs were tested against T. brucei rhodesiense STIB900 and L6 rat myoblast cells (for cytotoxicity) in vitro. Forty-four derivatives were more potent than I, including eight with IC50 values below 100 nM. The most potent and most selective for the parasite was the urea analog 2-(2-piperidin-1-ylamido)ethyl-4-(3-fluorophenyl)thiazole II (IC50 = 9 nM, SI > 18,000). None of 33 compounds tested were able to cure mice infected with the parasite; however, seven compounds caused temporary reductions of parasitemia (â?7%) but with subsequent relapses. The lack of in vivo efficacy was at least partially due to their poor metabolic stability, as demonstrated by the short half-lives of 15 analogs against mouse and human liver microsomes. In the experiment, the researchers used many compounds, for example, 3-Cyanobenzoyl chloride (cas: 1711-11-1COA of Formula: C8H4ClNO).
3-Cyanobenzoyl chloride (cas: 1711-11-1) belongs to organic chlorides. Organic chlorides can cause corrosion in pipelines, valves and condensers, and cause catalyst poisoning. The hydrocarbon processing industry (HPI) and others are affected by damage caused by these substances. 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: C8H4ClNO
Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics