Al-Salahi Rashad, Geffken Detlef, Koellner Maria
Department of Pharmaceutical Chemistry, College of Pharmacy, King Saud University, Riyadh, Saudi Arabia.
Chem Pharm Bull (Tokyo). 2011;59(6):730-3. doi: 10.1248/cpb.59.730.
This research was carried out to study the pharmacological activity of a newly synthesized series of 2-alkoxy-[1,2,4]triazolo[1,5-a]quinazolin-5-ones as adenosine receptor antagonists. These compounds have been tested in radioligand binding assays on cloned Chinese hamster ovary (CHO) cells transfected with A(1), A(2A), A(2B) and A(3) receptors. In particular, among the triazoloquinazolines (1-11), the dialkoxy derivative (7b) was found to have the highest affinity at A(1) subtype receptor, and its radioligand binding activity together with 1,3-dipropyl-8-cyclopentylxanthine (DPCPX) was studied. Finally, the structure-activity relationship (SAR) studies on the titled compounds provide some new insights about steric hindrance and lipophilic requirements for anchoring to the adenosine receptors recognition site.
本研究旨在研究一系列新合成的2-烷氧基-[1,2,4]三唑并[1,5-a]喹唑啉-5-酮作为腺苷受体拮抗剂的药理活性。这些化合物已在转染了A(1)、A(2A)、A(2B)和A(3)受体的克隆中国仓鼠卵巢（CHO）细胞的放射性配体结合试验中进行了测试。特别是，在三唑并喹唑啉类化合物（1-11）中，发现二烷氧基衍生物（7b）对A(1)亚型受体具有最高亲和力，并研究了其放射性配体结合活性以及1,3-二丙基-8-环戊基黄嘌呤（DPCPX）。最后，对标题化合物的构效关系（SAR）研究为锚定到腺苷受体识别位点的空间位阻和亲脂性要求提供了一些新的见解。
