当前位置: X-MOL 学术Chem. Heterocycl. Comp. › 论文详情
Our official English website, www.x-mol.net, welcomes your feedback! (Note: you will need to create a separate account there.)
Electrophilic reactions as methods of modification of pyrrolobenzimidazolones and pyrroloquinazolinones
Chemistry of Heterocyclic Compounds ( IF 1.4 ) Pub Date : 2020-08-22 , DOI: 10.1007/s10593-020-02751-z
Vyacheslav S. Grinev , Alevtina Yu. Egorova

The publication presents a number of modifications based on electrophilic reactions of previously synthesized biologically active benzannulated pyrrolo[1,2-a]imidazolones and pyrrolo[2,1-b]quinazolinones, which make it possible to widely change the physicochemical properties of molecules. Quantitative assessments of the lipophilicity of all synthesized compounds were carried out, on the basis of which conclusions were made regarding the advisability of introducing alkyl and trifluoroacetyl groups to increase the bioavailability of compounds by increasing their lipophilicity to 40%.


中文翻译:

亲电反应作为吡咯并苯并咪唑酮和吡咯并喹唑啉酮的改性方法

该出版物提出了基于先前合成的具有生物活性的苯并环吡咯并[1,2-a]咪唑啉酮和吡咯并[2,1-b]喹唑啉酮的亲电反应的许多修饰,这些修饰使广泛改变分子的理化性质成为可能。对所有合成化合物的亲脂性进行了定量评估,在此基础上得出了有关引入烷基和三氟乙酰基以通过将其亲脂性提高至40%来提高化合物生物利用度的结论。
更新日期:2020-08-22
down
wechat
bug