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

Abstract Quinazolinone derivatives were synthesized and evaluated as non-peptidic growth hormone secretagogues. Modeling guided design of quinazolinone compound 21 Download high-res image (70KB) Download full-size image Scheme 2 . (a) DMAP, Et 3 N, DMF; (b) Gly-OMe ( 8 ), heat; (c) NaOH, H 2 O, THF; (d) NH 2 (CH 2 ) n NHBoc, HOBt, EDC, NMM; (e) PhB(OH) 2 , Pd(PPh 3 ) 4 , Na 2 CO 3 ; (f) HCl. led to a potency enhancement of greater than 200-fold compared to human growth hormone secretagogue affinity of a screening lead 4 .