Kelley J L, Linn J A, Selway J W
Division of Organic Chemistry, Burroughs Wellcome Co., Research Triangle Park, North Carolina 27709.
J Med Chem. 1990 May;33(5):1360-3. doi: 10.1021/jm00167a012.
A series of 6-anilino-9-benzyl-2-chloropurines was synthesized and tested for antirhinovirus activity. Most of the compounds were prepared by reaction of the appropriate aniline with 9-benzyl-2,6-dichloro-9H-purine. Structure-activity relationship studies revealed that compounds with small, lipophilic para substituents were good inhibitors of serotype 1B. Several compounds had good activity against four representative serotypes.
合成了一系列6-苯胺基-9-苄基-2-氯嘌呤,并对其抗鼻病毒活性进行了测试。大多数化合物是通过适当的苯胺与9-苄基-2,6-二氯-9H-嘌呤反应制备的。构效关系研究表明,具有小的亲脂性对位取代基的化合物是1B型血清型的良好抑制剂。几种化合物对四种代表性血清型具有良好的活性。