484698-81-9Relevant academic research and scientific papers
Pyrrolidine-5,5-trans-lactams. 4. Incorporation of a P3/P4 Urea Leads to Potent Intracellular Inhibitors of Hepatitis C Virus NS3/4A Protease
Slater, Martin J.,Amphlett, Elizabeth M.,Andrews, David M.,Bamborough, Paul,Carey, Seb J.,Johnson, Martin R.,Jones, Paul S.,Mills, Gail,Parry, Nigel R.,Somers, Donald O'N.,Stewart, Alan J.,Skarzynski, Tadeusz
, p. 4627 - 4630 (2007/10/03)
(Matrix presented) In this, the first of two Letters, we describe how a P3/P4 urea linking unit was used to greatly enhance the biochemical and replicon potency of inhibitors based upon the pyrrolidine-5,5-trans-lactam template. Compound 7b demonstrated a
Pyrrolidine-5,5-trans-lactams. 2. The Use of X-ray Crystal Structure Data in the Optimization of P3 and P4 Substituents
Andrews, David M.,Chaignot, Helene,Coomber, Barry A.,Good, Andrew C.,Hind, S. Lucy,Johnson, Martin R.,Jones, Paul S.,Mills, Gail,Robinson, J. Ed,Skarzynski, Tadeusz,Slater, Martin J.,Somers, Donald O'N
, p. 4479 - 4482 (2007/10/03)
(Matrix Presented) In this, the second of two letters, we describe the elaboration of the pyrrolidine-5,5-trans-lactam template to delineate the requirements for optimal substitution of the pyrrolidine and lactam nitrogen atoms. Central to the strategy is the use of rapid iterative synthesis in conjunction with X-ray crystal structure determination of ligand-protein complexes.
