Details

Autor(en) / Beteiligte

• Jafari, Behzad
• Jalil, Saquib
• Zaib, Sumera
• Iqbal, Jamshed
• Safarov, Sayfidin
• Khalikova, Muattar
• Isobaev, Muzafar
• Munshi, Ali
• Rahman, Qamar
• Ospanov, Meirambek
• Yelibayeva, Nazym
• Kelzhanova, Nazken
• Abilov, Zharylkasyn A.
• Turmukhanova, Mirgul Z.
• Kalugin, Sergey N.
• Ehlers, Peter
• Langer, Peter

Titel

Synthesis of 2‐Aryl‐12 H ‐benzothiazolo[2,3‐ b ]quinazolin‐12‐ones and Their Activity Against Monoamine Oxidases

Ist Teil von

• ChemistrySelect (Weinheim), 2019-10, Vol.4 (37), p.11071-11076

Erscheinungsjahr

2019

Quelle

Wiley Online Library All Journals

Beschreibungen/Notizen

• Abstract Benzothiazoloquinazolines are known to possess several interesting biological properties. Various arylated benzothiazoloquinazolines were synthesized from readily available 2 ‐ bromo ‐ 12 H ‐ benzothiazolo[2,3 ‐ b ]quinazolin ‐ 12 ‐ one by palladium catalysed Suzuki ‐ Miyaura reactions in 43 – 85% yield. Synthesized derivatives were analysed regarding their in vitro inhibition activity towards monoamine oxidases A and B and showed significant inhibitory values in the micromolar range. Molecular modelling as well as PAINS studies on the binding interaction of most potent inhibitors with both isoforms were studied to verify the experimental results.