Varano F, Catarzi D, Colotta V, Cecchi L, Filacchioni G, Galli A, Costagli C
Dipartimento di Scienze Farmaceutiche, Università di Firenze, Italy.
Arch Pharm (Weinheim). 1996 Dec;329(12):529-34. doi: 10.1002/ardp.19963291204.
Some 2-arylpyrazolo[1,5-c][1,3]benzoxazin-5-ones 1 and 5- oxopyrazolo[1,5-c][1,3]benzoxazin-2-carboxylates 2 were prepared and biologically evaluated for their binding at benzodiazepine receptor (BZR) in rat cortical membranes. Structure-activity relationship studies suggest that, although proton donor d and proton acceptor a1 are both optional pharmacophoric descriptors, at least one of them must be present for good BZR affinity. When the proton donor d is not present, the heteroatom acceptor a1 is necessary either in the tricyclic core or in the appended substituent at the C-2 to obtain sub-micromolar BZR affinity.
制备了一些2-芳基吡唑并[1,5-c][1,3]苯并恶嗪-5-酮1和5-氧代吡唑并[1,5-c][1,3]苯并恶嗪-2-羧酸酯2，并对其在大鼠皮质膜中与苯二氮䓬受体（BZR）的结合进行了生物学评价。构效关系研究表明，虽然质子供体d和质子受体a1都是可选的药效团描述符，但为了获得良好的BZR亲和力，它们中至少必须有一个存在。当不存在质子供体d时，杂原子受体a1在三环核心或C-2位的附加取代基中是必要的，以获得亚微摩尔级的BZR亲和力。
