1257641-82-9Relevant academic research and scientific papers
Design and synthesis of rosiglitazone-ferulic acid-nitric oxide donor trihybrids for improving glucose tolerance
Liu, Jingchao,Huang, Zhangjian,Ma, Wenhuan,Peng, Sixun,Li, Yunman,Miranda, Katrina M.,Tian, Jide,Zhang, Yihua
, p. 650 - 665 (2018/11/27)
Glucose intolerance is associated with metabolic syndrome and type 2 diabetes mellitus (T2DM) while some new therapeutic drugs, such as rosiglitazone (Rosi), for T2DM can cause severe cardiovascular side effects. Herein we report the synthesis of Rosi-ferulic acid (FA)-nitric oxide (NO) donor trihybrids to improve glucose tolerance and minimize the side effects. In comparison with Rosi, the most active compound 21 exhibited better effects on improving glucose tolerance, which was associated with its NO production, antioxidant and anti-inflammatory activities. Furthermore, 21 displayed relatively high stability in the simulated gastrointestinal environments and human liver microsomes, and released Rosi in plasma. More importantly, 21, unlike Rosi, had little stimulatory effect on the membrane translocation of aquaporin-2 (AQP2) in kidney collecting duct epithelial cells. These, together with a better safety profile, suggest that the trihybrids, like 21, may be promising candidates for intervention of glucose intolerance-related metabolic syndrome and T2DM.
Design and synthesis of novel NO-donor-ferulic acid hybrids as potential antiatherosclerotic drug candidates a
Li, Nian-Guang,Wang, Rong,Shi, Zhi-Hao,Tang, Yu-Ping,Li, Bao-Quan,Wang, Zhen-Jiang,Song, Shu-Lin,Qian, Li-Hua,Wei, Li,Yang, Jian-Ping,Yao, Li-Juan,Xi, Jun-Zuan,Xu, Jia,Feng, Feng,Qian, Da-Wei,Duan, Jin-Ao
, p. 405 - 415 (2012/05/05)
Novel NO-donor-ferulic acid hybrids were designed and synthesized through a symbiotic approach using ferulic acid and three different NO-donating groups, such as nitric ester, 4-hydroxyl-3-phenylfuroxan, and 4-hydroxymethyl-3- phenylsulfonylfuroxan. Antioxidant, nitric oxide release, and vasodilator properties studies showed that the target phenylsulfonylfuroxan 14, especially 14c, while keeping the antioxidant activity, showed more NO release activity and vasodilating activity than isosorbide dinitrate (ISDN). Thus, 14c may be considered a novel potent anti-atherosclerosis drug candidate.
Design, synthesis and evaluation of nitric oxide releasing derivatives of 3-n-butylphthalide as antiplatelet and antithrombotic agents
Wang, Xuliang,Li, Yang,Zhao, Qian,Min, Zhenli,Zhang, Chao,Lai, Yisheng,Ji, Hui,Peng, Sixun,Zhang, Yihua
experimental part, p. 5670 - 5681 (2011/09/15)
Novel nitric oxide (NO) releasing derivatives (7a-7l) of 3-n-butylphthalide (NBP) were designed and synthesized. Compound 7e inhibited the adenosine diphosphate (ADP), thrombin (TH) and arachidonic acid (AA)-induced in vitro platelet aggregation, superior to NBP and aspirin, released moderate levels of NO, and improved aqueous solubility relative to NBP. Furthermore, 7e exhibited greater antithrombotic activity than NBP and aspirin in rats, and protected against collagen and adrenaline-induced thrombosis in mice. Therefore, NO-releasing NBP derivatives possessed potent antiplatelet aggregation and antithrombotic activity. Our findings may aid in the design of new therapeutic agents for the treatment of thrombosis-related ischemic stroke.
