Pyrrolidine-5,5-trans-lactams. 2. The use of X-ray crystal structure data in the optimization of P3 and P4 substituents.
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Andrews DM, Chaignot H, Coomber BA, Good AC, Hind SL, Johnson MR, Jones PS, Mills G, Robinson JE, Skarzynski T, Slater MJ, Somers DO
Pyrrolidine-5,5-trans-lactams. 2. The use of X-ray crystal structure data in the optimization of P3 and P4 substituents.
Org Lett. 2002 Dec 12;4(25):4479-82.
- PubMed ID
- 12465917 [ View in PubMed]
- Abstract
[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.