التفاصيل البيبلوغرافية
| العنوان: |
The azulene scaffold from a medicinal chemist's perspective : Physicochemical and in vitro parameters relevant for drug discovery |
| المؤلفون: |
Leino, Teppo O., Sieger, Peter, Yli-Kauhaluoma, Jari, Wallén, Erik A.A., Kley, Jörg T. |
| بيانات النشر: |
Elsevier |
| سنة النشر: |
2022 |
| المجموعة: |
JYX - Jyväskylä University Digital Archive / Jyväskylän yliopiston julkaisuarkisto |
| مصطلحات موضوعية: |
Indole, Naphthalene, Photostability, Scaffold hopping, atsuleeni, lääkesuunnittelu, aromaattiset yhdisteet, lääkekemia, biologinen aktiivisuus |
| الوصف: |
Azulene is a bicyclic scaffold rarely applied in medicinal chemistry. Here we report physicochemical and in vitro parameters relevant for drug discovery for a series of diversely substituted azulenes. We synthesized and characterized several scaffold hopping series of analogously substituted azulenes, indoles and naphthalenes. This enabled a comparison of azulene with the more common scaffolds indole and naphthalene. Our data indicates that undesirably low photostability of azulenes is restricted to certain substitution patterns. Generally, we conclude that azulene is an underused lipophilic bicycle and should be considered as a valuable complement to the collection of medicinal chemistry scaffolds. ; peerReviewed |
| نوع الوثيقة: |
article in journal/newspaper |
| وصف الملف: |
application/pdf; fulltext |
| اللغة: |
English |
| تدمد: |
0223-5234 |
| العلاقة: |
European Journal of Medicinal Chemistry; 237; 330800; Research Council of Finland; Suomen Akatemia; Leino, T. O., Sieger, P., Yli-Kauhaluoma, J., Wallén, E. A., & Kley, J. T. (2022). The azulene scaffold from a medicinal chemist's perspective : Physicochemical and in vitro parameters relevant for drug discovery. European Journal of Medicinal Chemistry , 237 , Article 114374. https://doi.org/10.1016/j.ejmech.2022.114374Test; CONVID_118852176; URN:NBN:fi:jyu-202204262374; http://urn.fi/URN:NBN:fi:jyu-202204262374Test |
| الإتاحة: |
http://urn.fi/URN:NBN:fi:jyu-202204262374Test |
| حقوق: |
CC BY 4.0 ; © 2022 the Authors ; openAccess ; https://creativecommons.org/licenses/by/4.0Test/ |
| رقم الانضمام: |
edsbas.BB487E83 |
| قاعدة البيانات: |
BASE |
