Respiratory syncytial virus fusion inhibitors. Part 6: an examination of the effect of structural variation of the benzimidazol-2-one heterocycle moiety |
| |
Authors: | Combrink Keith D Gulgeze H Belgin Thuring Jan W Yu Kuo-Long Civiello Rita L Zhang Yi Pearce Bradley C Yin Zhiwei Langley David R Kadow Kathleen F Cianci Christopher W Li Zhufang Clarke Junius Genovesi Eugene V Medina Ivette Lamb Lucinda Yang Zheng Zadjura Lisa Krystal Mark Meanwell Nicholas A |
| |
Institution: | Department of Chemistry, Bristol-Myers Squibb Research and Development, 5 Research Parkway, Wallingford, CT 06492, USA. |
| |
Abstract: | The effect of structural variation of the benzimidazol-2-one ring of RSV fusion inhibitors related to BMS-433771 (1) was examined in conjunction with side chain modifications and the introduction of an aminomethyl substituent at the 5-position of the core benzimidazole moiety. Replacement of the benzimidazol-2-one moiety with benzoxazole, oxindole, quinoline-2-one, quinazolin-2,4-dione and benzothiazine derivatives provided a series of potent RSV fusion inhibitors 4. However, the intrinsic potency of 6,6-fused ring systems was generally less than that of comparably substituted 5,6-fused heterocycles of the type found in BMS-433771 (1). The introduction of an aminomethyl substituent to the benzimidazole ring enhanced antiviral activity in the 6,6-fused ring systems. |
| |
Keywords: | |
本文献已被 ScienceDirect PubMed 等数据库收录! |
|