219611-74-2Relevant academic research and scientific papers
New phthalimide derivatives with potent analgesic activity: II
Antunes, Roberto,Batista, Hildson,Srivastava,Thomas,Araujo
, p. 3071 - 3076 (1998)
Seven new phthalimide derivatives (9a~g) with 1,2,4-oxadiazol-5-yl methyl group attached to nitrogen have been synthesized from N- phthaloylglycine 6 and arylamidoximes 7a~g. All of these showed potent analgesic effect with acetic acid induced 'writhing' test in mice. One of the better compounds (ID50 = 22 mg/Kg ip) has been found to be 9a which also demonstrates analgesic activity against inflammatory pain.
Isothiazolinone compound and corresponding application
-
, (2019/07/08)
The invention provides an isothiazolinone compound with an IDO inhibitory activity, and a preparing method and pharmaceutical application thereof. The invention particularly relates to a compound shown in a formula I, pharmaceutically acceptable salts thereof, isomers and prodrugs, wherein definitions of all groups are shown in the description. The invention further relates to compound drug preparations, drug compositions and the application of the compound drug preparations and the drug compositions in treating, relieving and/or preventing various relevant diseases caused by immunosuppressionsuch as tumors, virus infection or autoimmune diseases. The isothiazolinone compound has the excellent IDO inhibitory activity.
Synthesis, characterization and interaction mechanism of new oxadiazolo-phthalimides as peripheral analgesics. IV
Antunes, Roberto,Batista, Hildson,Srivastava, Rajendra M.,Thomas, George,Araújo, Clidenor C.,Longo, Ricardo L.,Magalh?es, Hélio,Le?o, Marcelo B.C.,Pav?o, Ant?nio C.
, p. 1 - 13 (2007/10/03)
The synthesis, characterization and spectroscopic studies of compounds 6a-g with analgesic activity is described. A new model of interaction between the drug and the enzyme is suggested. Application of the Resonance Valence Bond theory led us to propose, for the first time, an entirely new mechanism involving an electron transfer from the amino acid residue of the enzyme to the drug. Theoretical studies of various transition states involved in the interaction mechanism employing the semi-empirical molecular orbital calculations (AM1 method) have been carried out. This article also deals with an extensive study of the structure-activity relationships of seven oxadiazolo-phthalimides 6a-g.
