喹唑啉类：3型和4型磷酸二酯酶联合抑制剂。
Quinazolines: combined type 3 and 4 phosphodiesterase inhibitors.
作者信息
Charpiot B, Brun J, Donze I, Naef R, Stefani M, Mueller T
机构信息
Research, Novartis Pharma AG, Basle, Switzerland.
出版信息
Bioorg Med Chem Lett. 1998 Oct 20;8(20):2891-6. doi: 10.1016/s0960-894x(98)00508-3.
A series of quinazolines has been prepared and evaluated for its ability to inhibit cyclic AMP phosphodiesterase type 3, type 4A, 4B and 4D. The most potent inhibitors showed IC50 values in the nanomolar range for type 3 and type 4 isoforms and bind with high affinity to the [3H]rolipram binding site. These quinazolines represent a new family of potent mixed PDE 3/4 inhibitors and are expected to have a therapeutic potential.
已制备了一系列喹唑啉，并对其抑制3型、4A型、4B型和4D型环磷酸腺苷磷酸二酯酶的能力进行了评估。最有效的抑制剂对3型和4型同工酶的IC50值在纳摩尔范围内，并与[3H]咯利普兰结合位点具有高亲和力。这些喹唑啉代表了一类新的强效3/4型磷酸二酯酶混合抑制剂，有望具有治疗潜力。
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