This report describes the synthesis of new cyclic imides obtained from the reaction between aniline and dichloromaleic anhydride with further chlorosulphonation as well as the reaction between different amines and 4-methoxyphenol for the synthesis of imidobenzenesulphonyl derivatives. These compounds were tested as antinociceptive agents using the writhing test on mice. Some compounds, when intraperitoneally injected, proved to be potent and dose-related antinociceptives, being several times more active than many known reference drugs.
3D-QSAR/CoMFA IN IMIDIC COMPOUNDS WITH ANTINOCICEPTIVE ACTIVITY. Imide compounds have shown biological activity. These compounds can be easily synthesized with good yields. The objective of this paper was the rational planning of imides and sulfonamides with antinociceptive activity using the 3D-QSAR/CoMFA approach. The studies were performed using two data sets. The first set consisted of 39 cyclic imides while the second set consisted of 39 imides and 15 sulfonamides. The 3D-QSAR/ CoMFA models have shown that the steric effect is important for the antinociceptive activity of imide and sulphonamide compounds. Ten new compounds with improved potential antinociceptive activity have been proposed by de novo design leapfrog simulations.
Background: Organic synthesis has contributed significantly to the development of new drugs. Cyclic imides are organic functions that demonstrate therapeutic potential, due to their easy attainment and good yields. The development of new drugs often requires the creation of a library of compounds for further biological tests. However, organic syntheses are known to be mostly delayed. The use of microwave radiation in organic synthesis has increased in the last years, several studies in the area showed advantages such as decrease or total absence of solvents, increase of yield and mainly reduction of reaction time. The reaction conditions used to obtain 3,4-dichloro-1phenyl-1 H -pyrrole-2,5-dione, on dielectric heating at reflux, from dichloromaleic anhydride and aniline, using acetic acid as a catalyst, ethanol as solvent , yielded good results, yielding from 39.56 to 70.21% and time from 15 to 20 minutes. The literature records yield for this synthesis of 70%, under heating and reflux for 2 hours. Therefore, the dielectric heating was more efficient when compared to traditional heating.
Antinociceptive Properties of Chloromaleinimides and Their Sulfonyl Derivatives. -A variety of new chloromaleimides [cf. (V), (IXa)] and corresponding sulfonyl derivatives [cf. (VIII), (IXb,c)] are synthesized and evaluated for their antinociceptive activities. Some of them, when intraperitoneally injected, prove to be potent and dose-related antinociceptives, being several times more active than many known reference drugs. -(WALTER, M. E.; MORA, C.; MUNDSTOCK, K.; DE SOUZA, M. M.; DE OLIVEIRA PINHEIRO, A.; YUNES, R. A.; NUNES*, R.
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