21405-62-9Relevant academic research and scientific papers
Synthesis and insecticidal activity of mesoionic pyrido[1,2-α]pyrimidinone derivatives containing a neonicotinoid moiety
Pan, Jianke,Yu, Lu,Liu, Dengyue,Hu, Deyu
, (2018/05/30)
Mesoionic pyrido[1,2-α]pyrimidinone derivatives containing a neonicotinoid moiety were designed, synthesized, and evaluated for their insecticidal activity. Some of the title compounds showed remarkable insecticidal properties against Aphis craccivora. Compound I13 exhibited satisfactory insecticidal activity against A. craccivora. Meanwhile, label-free proteomics analysis of compound I13 treatment identified a total of 821 proteins. Of these, 35 proteins were up-regulated, whereas 108 proteins were down-regulated. Differential expressions of these proteins reflected a change in cellular structure and metabolism.
METHYLENE LINKED QUINOLINYL MODULATORS OF RORyt
-
Paragraph 0387; 0388; 0413; 0414, (2014/05/07)
The present invention comprises compounds of Formula I. wherein: R1, R2, R3, R4, R5, R6, R7, R8, and R9 are defined in the specification. The invention also comprises a method of treating or ameliorating a syndrome, disorder or disease, wherein said syndrome, disorder or disease is rheumatoid arthritis or psoriasis. The invention also comprises a method of modulating RORγt activity in a mammal by administration of a therapeutically effective amount of at least one compound of claim 1.
Pd(II)-catalyzed intramolecular amidoarylation of alkenes with molecular oxygen as sole oxidant
Yip, Kai-Tai,Yang, Dan
supporting information; experimental part, p. 2134 - 2137 (2011/06/19)
Stereoselective palladium-catalyzed synthesis of structurally versatile indoline derivatives, using molecular oxygen as the sole oxidant, is described. New C-N and C-C bonds form across an alkene in an intramolecular manner. The C-N bond-forming step proceeds via a syn-amidopalladation pathway. The moderate kinetic isotope effects (intramolecular KIE = 3.56) suggest that electrophilic aromatic substitution occurs in the arylation step.
SULFOXIMINE AND SULDODIIMINE MATRIX METALLOPROTEINASE INHIBITORS
-
, (2008/06/13)
Novel sulfoximine and sulfodiimine matrix metalloproteinase inhibitors of the formula, STR1 wherein: R 1 is selected from the group consisting of lower-alkyl, hydroxy lower-alkyl, amino lower-alkyl, carbamoyl lower-alkyl, lower-alkyl carbonyl, lower-alkyoxyalkyl, aralkyl and heteroaralkyl;X is NH or O;R 2 is selected from the group consisting of hydrogen, lower-alkyl and aralkyl;R 3 is selected from the group consisting of hydrogen, lower-alkyl, amino lower-alkyl, guanyl lower-alkyl, aralkyl and heteroaralkyl; andR 4 is selected from the group consisting of lower alkyl, aralkyl and--CH(R 5)--C(O)NH 2, wherein R 5 is selected from the group consisting of hydrogen, lower-alkyl, amino lower-alkyl, guanyl lower-alkyl, imidazoylalkyl, hydroxymethyl, 1-hydroxyethyl, mercapto lower-alkyl, and methylthio lower-alkyl;useful for modulating physiological functions or treating diseases and disease conditions associated with matrix metalloproteinase modulation.
ENKEPHALINASE ENZYME INHIBITING COMPOUNDS
-
, (2008/06/13)
Chiral 2-(2-benzyl-3-mercaptopropionylamino)-1-alkanol derivatives and chiral 2-(2-benzyl-3-mercaptopropionylamino)-4-methylthiobutyric acids are inhibitors of enkephalinase enzyme, reflecting their clinical utility as analgesics or anticonvulsant agents, or as therapy for disorders in which endogenous enkephalin levels are below normal.
Mesoionic Xanthine Analogues: Phosphodiesterase Inhibitory and Hypotensive Activity
Glennon, Richard A.,Rogers, Michael E.,Smith, J. Doyle,El-Said, M. K.,Egle, John L.
, p. 658 - 661 (2007/10/02)
Several mesoionic thiazolopyrimidines and mesoionic 1,3,4-thiadiazolopyrimidines were evaluated as inhibitors of cyclic-AMP phosphodiesterase.While small alkyl substituents at the 6 position have no significant effect on activity, phenyl and benzyl substituents enhance activity.Mesoionic structures such as 1 (R2 = H; R8 = Et) possess 20 to 40 times activity of theophylline when the R6 substituent is phenyl or 4-chlorobenzyl.Methyl and ethyl substitution at the 2 position essentially abolishes activity.Although plagued by solubility problems, several of the mesoionic derivatives were found to display weak hypotensive effects in vivo.
