- New phthalimide-benzamide-1,2,3-triazole hybrids; design, synthesis, α-glucosidase inhibition assay, and docking study
-
A new series of phthalimide-benzamide-1,2,3-triazole hybrids 8a–k as α-glucosidase inhibitors was designed and synthesized. The biological evaluation of compounds 8a–k against yeast α-glucosidase demonstrated that all they have excellent inhibitory activity in comparison with standard inhibitor acarbose. Among them, the most potent compound was compound 8d with inhibitory activity 18.5-fold more than acarbose. Kinetic study revealed that α-glucosidase inhibition of compound 8d was the competitive type. Furthermore, docking study suggested that compound 8d is more stable than acarbose in the active site of α-glucosidase.
- Ali Faramarzi, Mohammad,Biglar, Mahmoud,Emadi, Mehdi,Larijani, Bagher,Mahdavi, Mohammad,Mohammadi-Khanaposhtani, Maryam,Mojtabavi, Somayeh,Rahmani, Abbas,Sadat-Ebrahimi, Seyed Esmaeil,Yahya-Meymandi, Azadeh,jafari, Negar
-
-
Read Online
- Synthesis and anti-inflammatory intestinal activity of new glucocorticoid derivatives
-
Glucocorticoids (GCs) are used worldwide in the treatment of chronic inflammatory diseases. This study describes the synthesis of new glucocorticoid derivatives and evaluates anti-inflammatory activity in rat models with ulcerative colitis (UC). Six compounds (5a–f) were synthetized using the molecular hybridization strategy with yields of 40–80%. The compounds 5e and 5f showed a total regression of ulceration in 83.3% and 75% of treated animals, respectively. Moreover, 5e improved several clinical signs, such as weight gain and survival rates. The compounds 5a and 5c showed total regression of ulceration in 33.3% of the rats. This is higher than prednisolone. Glucocorticoid derivatives showed potential anti-inflammatory intestinal activity with regression of ulceration in colitis.
- Machado, Marcella Gabrielle Mendes,Scarim, Cauê Benito,de Andrade, Cleverton Roberto,dos Santos, Jean Leandro,Chin, Chung Man
-
-
Read Online
- Synthesis of phthalimides, isoindolin-1-ones and isoindolines bearing aminobenzoic acids as a new fluorescent compounds
-
Both experimental and theoretical methods were used in order to study the fluorescent properties of nine new compounds based on phthalimides, isoindolin-1-ones and isoindolines bearing aminobenzoic acids (2-aminobenzoic acid, 3-aminobenzoic acid and 4-aminobenzoic acid), which were obtained under mild reaction conditions. The photophysical properties of all the compounds were studied by electronic absorption and fluorescence spectroscopy in methanol solutions. All compounds exhibited fluorescence emission and high quantum yields. Additionally, it was found that the intramolecular charge in these donor-acceptor systems is significantly depending on electron-withdrawing substituents at the carboxylic acid position.
- Solis-Santos, Melchor,Ordó?ez, Mario,Ochoa-Terán, Adrián,Morales-Cueto, Rodrigo,Labastida-Galván, Victoria
-
-
- 1,3-dioxo-isoindoline benzamide compound and application thereof
-
The invention belongs to the technical field of diabetes treatment medicines and in particular relates to an N-(2-aminophenyl)-3-(1,3-dioxo-isoindoline-2-yl) benzamide compound, and a preparation andapplication thereof in preparing diabetes treatment medicines. The compound has a formula (1) shown in the description, in the formula, R is selected from hydrogen, fluorine, chlorine, bromine, methyl, ethyl, propyl, isopropyl, n-butyl, sec-butyl, isobutyl and tert-butyl, and X is selected from hydrogen or fluorine. The N-(2-aminophenyl)-3-(1,3-dioxo-isoindoline-2-yl) benzamide compound has a remarkable function of protecting pancreatic beta cells, and can be adopted to prepare novel diabetes treatment medicines.
- -
-
Paragraph 0061; 0062; 0065
(2019/11/28)
-
- Amide compounds for regulating WNT signal channel and application of compounds
-
The invention belongs to the technical field of medicine, and particularly relates to amide compounds for regulating a WNT signal channel and an application of the compounds. The compounds have a structure represented by a general formula I shown in the description.
- -
-
Paragraph 0216; 0218
(2019/07/11)
-
- Synthesis and SAR of novel, non-MPEP chemotype mGluR5 NAMs identified by functional HTS
-
This Letter describes the discovery and SAR of three novel series of mGluR5 non-competitive antagonists/negative allosteric modulators (NAMs) not based on manipulation of an MPEP/MTEP chemotype identified by a functional HTS approach. This work demonstrates fundamentally new mGluR5 NAM chemotypes with submicromolar potencies, and further examples of a mode of pharmacology 'switch' to provide PAMs with a non-MPEP scaffold.
- Zhou, Ya,Rodriguez, Alice L.,Williams, Richard,Weaver, C. David,Conn, P. Jeffrey,Lindsley, Craig W.
-
scheme or table
p. 6502 - 6506
(2010/05/17)
-
- Hypolipidemic Activity of Phthalimide Derivatives. 2. N-Phenylphthalimide and Derivatives
-
A series of substituted N-phenylphthalimide derivatives was synthesized and examined for their ability to lower serum cholesterol and triglyceride levels in mice at 20 (mg/kg)/day, ip.Of the newly synthesized compounds, the most potent compound, o-(N-phthalimido)acetophenone, lowered serum cholesterol 57percent after 16 days and lowered serum triglyceride levels 44percent after 14 days. o-(N-Phthalimido)acetophenone was observed to be active in both normogenic (normal blood lipids levels) and hyperlipidemic mice and normogenic rats.In the latter, the reduction of serum lipids was reversible.The mode of action of this compound appeared to be multiple, including blockage of the de novo synthesis of lipids and acceleration of the excretion of lipids.The lipoprotein fractions of rat blood were reduced significantly in cholesterol, triglyceride, and neutral lipid content after 14 days treatment with o-(N-phthalimido)acetophenone.
- Chapman, James M.,Voorstad, P. Josee,Cocolas, George H.,Hall, Iris H.
-
p. 237 - 243
(2007/10/02)
-