Elucidating the Structure-Activity Relationships of the Vasorelaxation and Antioxidation Properties of Thionicotinic Acid Derivatives.docVIP

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Elucidating the Structure-Activity Relationships of the Vasorelaxation and Antioxidation Properties of Thionicotinic Acid Derivatives.doc

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Elucidating the Structure-Activity Relationships of the Vasorelaxation and Antioxidation Properties of Thionicotinic Acid Derivatives

Molecules 2010, 15, 198-214; doi:10.3390/moleculeOPEN ACCESS molecules ISSN 1420-3049 /journal/molecules Article Elucidating the Structure-Activity Relationships of the Vasorelaxation and Antioxidation Properties of Thionicotinic Acid Derivatives Supaluk Prachayasittikul 1,*, Orapin Wongsawatkul 2, Apilak Worachartcheewan 3, Chanin Nantasenamat 3, Somsak Ruchirawat 4 and Virapong Prachayasittikul 3,* 1 Department of Chemistry, Faculty of Science, Srinakharinwirot University, Bangkok 10110, Thailand 2 Department of Pharmacology, Faculty of Medicine, Srinakharinwirot University, Bangkok 10110, Thailand 3 Department of Clinical Microbiology, Faculty of Medical Technology, Mahidol University, Bangkok 10700, Thailand 4 Chulabhorn Research Institute and Chulabhorn Graduate Institute, Bangkok 10210, Thailand ? Authors to whom correspondence should be addressed; E-Mails: supaluk@swu.ac.th (S.P.); mtvpr@mahidol.ac.th (V.P.); Tel.: +662-664-1000 ext 8209 (S.P.); +662-441-4376 (V.P.); Fax: +662-259-2097 (S.P.); +662-441-4380 (V.P.). Received: 11 November 2009; in revised form: 29 December 2009 / Accepted: 4 January 2010 / Published: 6 January 2010 Abstract: Nicotinic acid, known as vitamin B3, is an effective lipid lowering drug and intense cutaneous vasodilator. This study reports the effect of 2-(1-adamantylthio)nicotinic acid (6) and its amide 7 and nitrile analog 8 on phenylephrine-induced contraction of rat thoracic aorta as well as antioxidative activity. It was found that the tested thionicotinic acid analogs 6-8 exerted maximal vasorelaxation in a dose-dependent manner, but their effects were less than acetylcholine (ACh)-induced nitric oxide (NO) vasorelaxation. The vasorelaxations were reduced, apparently, in both NG-nitro-L-arginine methyl ester (L-NAME) and indomethacin (INDO). Synergistic effects were observed in the presence of L-NAME plus INDO, leading to loss of vasorelaxation of both the ACh