Rational Design of Potent Non-Nucleoside Inhibitors of HIV-1 Reverse Transcriptase was written by Chong, Pek;Sebahar, Paul;Youngman, Michael;Garrido, Dulce;Zhang, Huichang;Stewart, Eugene L.;Nolte, Robert T.;Wang, Liping;Ferris, Robert G.;Edelstein, Mark;Weaver, Kurt;Mathis, Amanda;Peat, Andrew. And the article was included in Journal of Medicinal Chemistry in 2012.Category: chlorides-buliding-blocks The following contents are mentioned in the article:
A new series of non-nucleoside reverse transcriptase inhibitors based on an imidazole-amide biarylether scaffold has been identified and shown to possess potent antiviral activity against HIV-1, including the NNRTI-resistant Y188L mutated virus. X-ray crystallog. of inhibitors bound to reverse transcriptase, including a structure of the Y188L RT protein, was used extensively to help identify and optimize the key hydrogen-bonding motif. This led directly to the design of compound (I) that exhibits remarkable antiviral activity (EC50 < 1 nM) against a wide range of NNRTI-resistant viruses and a favorable pharmacokinetic profile across multiple species. This study involved multiple reactions and reactants, such as 2-Chloro-4-sulfamoylbenzoic acid (cas: 53250-84-3Category: chlorides-buliding-blocks).
2-Chloro-4-sulfamoylbenzoic acid (cas: 53250-84-3) 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. Aryl chlorides may be prepared by the Friedel-Crafts halogenation, using chlorine and a Lewis acid catalyst.Category: chlorides-buliding-blocks
Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics