61445-93-0Relevant academic research and scientific papers
Spectroscopic study of a symmetrical bis-crown fluoroionophore of the diphenylpentadienone series
Marcotte, Nathalie,Fery-Forgues, Suzanne,Lavabre, Dominique,Marguet, Sylvie,Pivovarenko, Vasyl G.
, p. 3163 - 3170 (1999)
A new fluoroionophore bearing two crown ethers on the conjugated system, 1,5-bis[4N-(aza-15-crown-5)-phenyl]-1,4-pentadien-3-one (II), was synthesized together with model compound I where the crown ethers are replaced by diethylamino groups. The behavior
Synthesis of tetracyclic oxindoles and evaluation of their α-glucosidase inhibitory and glucose consumption-promoting activity
Dodd, Robert H.,Hao, Lei,Ma, Ying,Ma, Yujiao,Sun, Hua,Yu, Peng,Zhang, Xinying,Zhang, Yinan,Zhao, Lianbo
supporting information, (2020/05/27)
A series of tetracyclic oxindole derivatives was synthesized by asymmetric 1, 3-dipole reaction in 2–4 steps in 57–86% overall yields. These compounds were evaluated for α-glucosidase inhibitory and glucose consumption-promoting activity in vitro. Compound 4l competitively and reversibly inhibited α-glucosidase (IC50 = 3.64 μM) with activity 14-fold higher than that of acarbose. Docking analysis substantiated these findings. In addition, compound 4l exhibited significant glucose consumption promoting activity at 1 μM.
Effects of novel diarylpentanoid analogues of curcumin on secretory phospholipase A2, cyclooxygenases, lipo-oxygenase, and microsomal prostaglandin e synthase-1
Ahmad, Waqas,Kumolosasi, Endang,Jantan, Ibrahim,Bukhari, Syed N. A.,Jasamai, Malina
, p. 670 - 681 (2014/06/09)
Arachidonic acid and its metabolites have generated a heightened interest due to their significant role in inflammation. Inhibiting the enzymes involved in arachidonic acid metabolism has been considered as the synergistic anti-inflammatory effect. A series of novel curcumin diarylpentanoid analogues were synthesized and evaluated for their inhibitory effects on activity of secretory phospholipase A2, cyclooxygenases, soybean lipo-oxygenase as well as microsomal prostaglandin E synthase-1. Among the curcumin analogues, compounds 3, 6, 9, 12, and 17 exhibited strong inhibition of secretory phospholipase A2 activity, with IC50 values ranging from 5.89 to 11.02 μm. Seven curcumin analogues 1, 3, 6, 7, 9, 11, and 12 showed inhibition of cyclooxygenases-2 with IC50 values in the range of 46.11 to 94.86 μm, which were lower than that of curcumin. Compounds 3, 6, 7, 12, and 17 showed strong inhibition of lipo-oxygenase enzyme activity. Preliminary screening of diarylpentanoid curcumin analogues for microsomal prostaglandin E synthase-1 activity revealed that four diarylpentanoid curcumin analogues 5, 6, 7, and 13 demonstrated higher inhibition of microsomal prostaglandin E synthase-1 activity with IC50 ranging from 2.41 to 4.48 μm, which was less than that of curcumin. The present results suggest that some of these diarylpentanoid analogues were able to inhibit the activity of these enzymes. This raises the possibility that diarylpentanoid analogues of curcumin might serve as useful starting point for the design of improved anti-inflammatory agents. A series of novel diarylpentanoid analogues of curcumin was synthesized by direct coupling of the appropriate aromatic aldehyde with three ketones, namely cyclohexanone, acetone, and cyclopentanone, under base-catalyzed Claisen-Schmidt condensation reaction. These analogues were screened for their inhibitory effects on the activity of secretory phospholipase A2 (sPLA2), cyclooxygenases, soybean lipo-oxygenase as well as microsomal prostaglandin E synthase-1 using in vitro assays.
Synthesis and anti-inflammatory evaluation of novel mono-carbonyl analogues of curcumin in LPS-stimulated RAW 264.7 macrophages
Zhao, Chengguang,Cai, Yuepiao,He, Xuzhi,Li, Jianling,Zhang, Li,Wu, Jianzhang,Zhao, Yunjie,Yang, Shulin,Li, Xiaokun,Li, Wulan,Liang, Guang
experimental part, p. 5773 - 5780 (2011/02/22)
Curcumin is a multifunctional natural product with regulatory effects on inflammation. However, a major limitation for the application of curcumin is its poor bioavailability. We previously demonstrated that the mono-carbonyl analogues of curcumin possess
Analogs of Michler's ketone for two-photon absorption initiation of polymerization in the near infrared: Synthesis and photophysical properties
Lemercier, Gilles,Martineau, Cecile,Mulatier, Jean-Christophe,Wang, Irene,Stephan, Olivier,Baldeck, Patrice,Andraud, Chantal
, p. 1606 - 1613 (2007/10/03)
We present the synthesis of substituted ketones, conjugated analogs of Michler's ketone. These molecules exhibit broadband TPA properties between 700 and 1100 nm due to a charge transfer from the terminal amino groups to the central ketone function and wi
