Naslov
Synthesis and biological activity of hydroxy- substituted N-benzimidazole carboxamides

Autori
Beč, Anja ; Kralj, Marijeta ; Zlatić, Katarina ; Starčević, Kristina ; Bertoša, Branimir ; Hranjec, Marijana

Vrsta, podvrsta i kategorija rada
Sažeci sa skupova, sažetak, znanstveni

Izvornik
8th EuChemS Chemistry Congress : book of abstracts / Silva, Artur M. S. ; Galvão, Adelino M. ; Machado, Bruno F. ; Faria, Joaquim L. - Lisabon : Sociedade Portuguesa de Química, 2022, 607-607

ISBN
978-989-8124-35-7

Skup
8th EuChemS Chemistry Congress (ECC8)

Mjesto i datum
Lisabon, Portugal, 28.08.2022. - 01.09.2022

Vrsta sudjelovanja
Poster

Vrsta recenzije
Međunarodna recenzija

Ključne riječi
benzimidazoles ; carboxamides ; antioxidants

Sažetak
It has been widely demonstrated that oxidative stress participates in all stages of chemical carcinogenesis. Since antioxidants are known by their function in protecting the human body against damage by reactive oxygen species (ROS) as well as by inhibiting ROS-relayed reactions, there has been tremendous and constant growing interest for the searching of novel natural or synthetic organic molecules as potential antioxidants. Being one of the well-known privileged building substructures in medicinal chemistry, benzimidazoles derivatives can be promising candidates as antioxidants. Among versatile pharmacological features, the most important ones for the rational design of novel bioactive compounds are antitumor, antimicrobial, antiviral, antioxidative and anti-inflammatory activities [1, 2]. All compounds were prepared by conventional reactions of organic synthesis as well as by microwave assisted reactions [3]. Targeted benzimidazole-2-carboxamides were synthesized by removal of methoxy protecting groups by using BBr3 in absolute dichloromethane at −75 °C, or by removal of benzyloxy protecting groups by Pd/C catalytic hydrogenation in methanol to afford the corresponding deprotected derivatives. All newly prepared compounds were screened for their antioxidant capacity using several spectroscopic methods as well as antiproliferative activity on several human cancer cells in vitro. To explore the antioxidative potency of benzimidazole-2- carboxamides we developed 3D-QSAR models and used them for computational prediction of antioxidative activity of the presented compounds.

Izvorni jezik
Engleski

Znanstvena područja
Kemija

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