TY - JOUR T1 - Structural Modifications of Benzimidazoles via Multi-Step Synthesis and Their Impact on Sirtuin-Inhibitory Activity. AU - Yoon,Yeong Keng, AU - Choon,Tan Soo, Y1 - 2015/11/30/ PY - 2015/09/19/received PY - 2015/11/02/revised PY - 2015/11/06/accepted PY - 2015/12/1/entrez PY - 2015/12/1/pubmed PY - 2017/1/7/medline KW - Benzimidazole KW - Molecular docking KW - SAR KW - Sirtuin SP - 1 EP - 8 JF - Archiv der Pharmazie JO - Arch Pharm (Weinheim) VL - 349 IS - 1 N2 - Benzimidazole derivatives have been shown to possess sirtuin-inhibitory activity. In the continuous search for potent sirtuin inhibitors, systematic changes on the terminal benzene ring were performed on previously identified benzimidazole-based sirtuin inhibitors, to further investigate their structure-activity relationships. It was demonstrated that the sirtuin activities of these novel compounds followed the trend where meta-substituted compounds possessed markedly weaker potency than ortho- and para-substituted compounds, with the exception of halogenated substituents. Molecular docking studies were carried out to rationalize these observations. Apart from this, the methods used to synthesize the interesting compounds are also discussed. SN - 1521-4184 UR - https://www.unboundmedicine.com/medline/citation/26616218/Structural_Modifications_of_Benzimidazoles_via_Multi_Step_Synthesis_and_Their_Impact_on_Sirtuin_Inhibitory_Activity_ DB - PRIME DP - Unbound Medicine ER -