Synthesis and evaluation of new pyrazoline‐thiazole derivatives as monoamine oxidase inhibitors |
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| Authors: | Ulviye Acar evik,Derya Osmaniye,Begü m Nurpelin Sa lik,Serkan Levent,Betü l Kaya avu o lu,Yusuf
zkay,Zafer As&#x m Kaplancikli |
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| Affiliation: | Ulviye Acar Çevik,Derya Osmaniye,Begüm Nurpelin Sağlik,Serkan Levent,Betül Kaya Çavuşoğlu,Yusuf Özkay,Zafer Asım Kaplancikli |
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| Abstract: | A novel series of 1,3,5‐trisubstituted‐2‐pyrazoline derivatives ( 4a ‐ 4k ) was synthesized and their chemical structures characterized by 1H NMR, 13C NMR, and mass spectroscopy. These compounds were evaluated as inhibitors for of type A and type B monoamine oxidase (MAO) enzymes. The most common inhibitors of MAO enzymes used to treat depression and anxiety such as selegiline and moclobemide drugs were used as reference agents. A result of biological evaluation of these compounds revealed compounds 4c , 4d , and 4? as potent and selective MAO A inhibitors. The most active compound 4? , which is 2,4‐dimethoxy at phenyl ring, showed strong inhibitory activity at MAO A (IC50 of 0.0445 ± 0.0018μM). Furthermore, compounds 4c and 4d showed significant inhibition profile on MAO A with the IC50 values 0.1423 ± 0.0051μM and 0.2148 ± 0.0067μM, respectively. |
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