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

Behzad Jafari, Saquib Jalil, Sumera Zaib, Jamshed Iqbal, Sayfidin Shahobidinovich Safarov, Muattar Khalikova, Muzafar D. Isobaev, Ali Munshi, Qamar Rahman, Meirambek Ospanov

7 more authors

Nazym S. Yelibayeva, Nazken Kelzhanova, Zharylkasyn A. Abilov, Mirgul Zh. Turmukhanova, Sergey Kalugin, Peter Ehlers, Peter Langer

2019

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DOI 10.1002/slct.201902245

Data confidence 70 medium

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Abstract

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.