Entity

Time filter

Source Type


Wang H.,Southwest University | Yan J.-F.,Chengdu DiAo Pharmaceutical Group Co. | Song X.-L.,Southwest University | Fan L.,Southwest University | And 4 more authors.
Bioorganic and Medicinal Chemistry | Year: 2012

We wish to report the further design and improved synthesis that resulted in two series of target molecules, TM-1 and TM-2, with remarkably simplified structures containing β-amino ketone of discrete nabumetone moiety. These were obtained via a 'one-pot, two-step, three-component' protocol of Mannich reaction with yield up to 97%. A total of 28 out of 31 new compounds were characterized using 1H NMR, 13C NMR, ESI MS and HRMS techniques. Studies on their antidiabetic activities, screened in vitro at 10 μg mL -1 level, indicate that TM-2 possesses peroxisome proliferator-activated receptor activation and α-glucosidase inhibition activity significantly stronger than that of TM-1, and also that of the series B compounds that were previously synthesized by the group. Analysis of the structure-activity relationship points to the sulfanilamide unit as the most probable potent group of β-amino ketone and, on the basis of which, a tangible strategy is presented for the development of new antidiabetic drugs. © 2011 Elsevier Ltd. All rights reserved. Source


Li M.-S.,CAS Chengdu Institute of Organic Chemistry | Li M.-S.,University of Chinese Academy of Sciences | Zhang Q.,CAS Chengdu Institute of Biology | Hu D.-Y.,CAS Chengdu Institute of Organic Chemistry | And 6 more authors.
Tetrahedron Letters | Year: 2016

A simple and catalyst-free method has been developed for the construction of β-hydroxyphosphine oxides through direct difunctionalization of alkenes with H-phosphine oxides and dioxygen under mild conditions. Preliminary mechanistic studies indicated that the hydroxyl oxygen atom of β-hydroxyphosphine oxide originated from the dioxygen and the present reaction might involve a radical process. © 2016 Elsevier Ltd. Source


Zhang K.,Southwest University | Yan J.-F.,Chengdu DiAo Pharmaceutical Group Co. | Tang X.-M.,Southwest University | Liu H.-P.,Southwest University | And 3 more authors.
Yaoxue Xuebao | Year: 2011

Twenty five new β-aminoalcohols containing nabumetone moiety were prepared via the reduction of potassium borohydride with a convenient and efficient procedure, starting from β-aminoketones that have been synthesized by our group. Their chemical structures were determined by IR, MS, 1H NMR, 13C NMR, HR-MS and antidiabetic activities were screened in vitro. Preliminary results revealed that the antidiabetic activity of most β-aminoalcohols were better than that of the corresponding β-aminoketones. Although most compounds showed weak antidiabetic activity, the α-glucosidase inhibitory activity of compounds 5hd1 and 5id2 reached 74.37% and 90.15%, respectively, which were superior to the positive control. The relative peroxisome proliferator-activated receptor response element (PPRE) activity of five compounds were more than 60%, among them compound 5ca possessed the highest activity (112.59%). As lead molecules of antidiabetic agents, compounds 5hd1, 5id2 and 5ca deserve further study. Source


Patent
Chengdu Diao Pharmaceutical Group Co. | Date: 2015-08-13

Disclosed are a phthalic hydrazide (phthalazine ketone) compound, and a pharmaceutical composition comprising the same. As a DNA repair enzyme poly (ADP-ribozyme) polymerase inhibitor, the compound and the pharmaceutical composition can effectively treat diseases involving PARP enzymatic activity, including cancer, neural degenerative diseases, inflammation and the like.


Patent
Chengdu Diao Pharmaceutical Group Co. | Date: 2012-12-03

Disclosed are a phthalic hydrazide (phthalazine ketone) compound, and a pharmaceutical composition comprising the same. As a DNA repair enzyme poly (ADP-ribozyme) polymerase inhibitor, the compound and the pharmaceutical composition can effectively treat diseases involving PARP enzymatic activity, including cancer, neural degenerative diseases, inflammation and the like.

Discover hidden collaborations