Publication Abstract from PubMed
[reaction: see text] 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.
Pyrrolidine-5,5-trans-lactams. 2. The use of X-ray crystal structure data in the optimization of P3 and P4 substituents.,Andrews DM, Chaignot H, Coomber BA, Good AC, Hind SL, Johnson MR, Jones PS, Mills G, Robinson JE, Skarzynski T, Slater MJ, Somers DO Org Lett. 2002 Dec 12;4(25):4479-82. PMID:12465917[1]
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.
