94041-14-2Relevant academic research and scientific papers
Thiocarbamates as non-nucleoside HIV-1 reverse transcriptase inhibitors. Part 2: Parallel synthesis, molecular modelling and structure-activity relationship studies on analogues of O-(2-phenylethyl)-N-phenylthiocarbamate
Cesarini, Sara,Spallarossa, Andrea,Ranise, Angelo,Bruno, Olga,La Colla, Paolo,Secci, Barbara,Collu, Gabriella,Loddo, Roberta
, p. 4173 - 4185 (2008/09/21)
To acquire further insight into the structure-activity relationship (SAR) of the thiocarbamates (TCs) described in the preceding work, 57 analogues of the lead compound O-(2-phenylethyl)-N-phenylthiocarbamate I were prepared by parallel solution-phase synthesis. We varied the 2-phenylethyl moiety (mono-substitution on the phenyl ring and modification of the ethyl linker), keeping constant the N-phenyl ring substitutions which have given the best results in the previous series. Most of the new TCs inhibited wild-type HIV-1 at micro- and nanomolar concentrations in MT-4 cell-based assays. Some TCs were also active at micromolar concentrations against the Y181C and/or K103N/Y181C resistant mutants. The SARs were rationalized by docking simulations.
Reaction of 2,4-Bis-(4-methoxyphenyl)-1,3,2,4-dithiadiphosphetane 2,4-Disulphide with Urea Derivatives, Carbamates and Thiocarbamates
El-Barbary, A. A.,Lawesson, S. O.
, p. 655 - 657 (2007/10/02)
Thiation of a series of urea derivatives, carbamates and thiocarbamates has been carried out by treatment with 2,4-bis-(4-methoxyphenyl)-1,3,2,4-dithiadiphosphetane 2,4-disulphide (1) under different conditions.Some of the products have been screened for their bactericidal activity.
