Synthesis and evaluation of ursolic acid-based 1,2,4-triazolo[1,5-a]pyrimidines derivatives as anti-inflammatory agents

Here, two series of novel ursolic acid-based 1,2,4-triazolo[1,5-a]pyrimidines derivatives were synthesized and screened for their anti-inflammatory activity by evaluating their inhibition effect of using LPS-induced inflammatory response in RAW 264.7 macrophages in vitro; the effects of different concentrations of the compounds on the secretion of nitric oxide (NO) and inflammatory cytokines including TNF-α and IL-6 were evaluated. Their toxicity was also assessed in vitro. Results showed that the most prominent compound 3 could significantly decrease production of the above inflammatory factors. Docking study was performed for the representative compounds 3, UA, and Celecoxib to explain their interaction with cyclooxygenase-2 (COX-2) receptor active site. In vitro enzyme study implied that compound 3 exerted its anti-inflammatory activity through COX-2 inhibition.

     

Synthesis and molecular docking studies of novel pyrimidine derivatives as potential antibacterial agents

Molecular Diversity - The present work describes the in vitro antibacterial evaluation of some new pyrimidine derivatives. Twenty-two target compounds were designed, synthesized and preliminarily...     

固相微萃取-气相色谱-质谱联用测定水中痕量2-甲基异冰片和土臭素

1引言2-甲基异冰片(2-Methylisoborneol,MIB)和土臭素(Geosmin,GSM)主要由放线菌、真菌和蓝绿藻代谢产生,这两种物质是目前造成饮用水具有霉味和土味的主要原因,尽管其在样品中的含量极低,但人的嗅觉对其极为敏感,微量的这些物质便能感觉,有研究表明,人类对2-甲基异冰片和土臭素的嗅阈值分别为10和30 ng/L[1]。目前,吹扫捕集(PT)和固