Modeling directed design and biological evaluation of quinazolinones as non-peptidic growth hormone secretagogues

  • Bioorg Med Chem Lett. 2000 Jan 3;10(1):5-8. doi: 10.1016/s0960-894x(99)00584-3.
Z Ye  1 ,  Y Gao ,  R K Bakshi ,  M H Chen ,  S P Rohrer ,  S D Feighner ,  S S Pong ,  A D Howard ,  A Blake ,  E T Birzin ,  L Locco ,  R M Parmar ,  W W Chan ,  J M Schaeffer ,  R G Smith ,  A A Patchett ,  R P Nargund
Affiliations
  • 1. Department of Medicinal Chemistry, Merck Research Laboratories, Rahway, NJ 07065, USA.
PMID: 10636230 DOI: 10.1016/s0960-894x(99)00584-3
Abstract

Quinazolinone derivatives were synthesized and evaluated as non-peptidic growth hormone secretagogues. Modeling guided design of quinazolinone compound 21 led to a potency enhancement of greater than 200-fold compared to human growth hormone secretagogue affinity of a screening lead 4.