Design,synthesis and anti-influenza A virus activity of novel 2,4-disubstituted quinazoline derivatives |
| |
| Institution: | 1. Department of Pharmaceutical Chemistry, Dr. Rajendra Gode College of Pharmacy, Malkapur, MS, 443101, India;2. Department of Pharmacology, Shri R. D. Bhakt College of Pharmacy, Jalna, Maharashtra, 431203, India;3. Department of Pharmaceutical Chemistry, R. C. Patel Institute of Pharmaceutical Education and Research, Shirpur 425405, MS, India;4. Department of Pharmaceutical Chemistry, H. R. Patel Institute of Pharmaceutical Education and Research, Shirpur 425405, MS, India |
| |
| Abstract: | Four 2,4-disubstituted quinazoline series containing various amide moieties were designed and synthesized as new anti-influenza A virus agents using the strategies of bio-isosterism and scaffold hopping. Many of them exhibit potent in vitro anti-influenza A virus activity and low cytotoxicity (CC50: >100 μM). Particularly, compounds 10a5 and 17a show better activity (IC50: 3.70–4.19 μM) and higher selective index (SI: >27.03, >23.87, respectively) against influenza A/WSN/33 virus (H1N1), opening a new direction for quinazoline derivatives in anti-influenza A virus field. |
| |
| Keywords: | Quinazoline derivatives Design Synthesis Anti-influenza A virus activity |
| 本文献已被 ScienceDirect 等数据库收录！ |
|
