62985-28-8Relevant academic research and scientific papers
Chemoselective phosphine-catalyzed cascade annulations between two different activated alkenes: Highly diastereoselective syntheses of polysubstituted cyclohexanes and cyclopentenes
Cai, Lingchao,Zhang, Bo,Wu, Guiping,Song, Haibin,He, Zhengjie
, p. 1045 - 1047 (2011)
Chemoselective phosphine-catalyzed cascade [2 + 2 + 2] and [2 + 2 + 1] annulations between two molecules of 2-arylmethylidene cyanoacetates or malononitriles and one molecule of α,β-unsaturated ketones have been developed. Under the nucleophilic catalysis
Synthesis, evaluation of insecticidal activity, and crystal analysis of cis-nitenpyram analogs bearing 1,4-dihydropyridine
Sun, Chuanwen,Liu, Tianyan,Ding, Li,Chen, Yanxia,Zhang, Wanggeng
, p. 1003 - 1012 (2013/07/26)
A new series of nitenpyram analogs were designed by introducing 1,4-dihydropyridine to fix the pharmacophore (-C=C-NO2) into the cis-configuration, as confirmed by X-ray diffraction. Crystal structure analysis showed that there was a homoconjugation effect on these cis-nitenpyram analogs, and a huge conjugated system comprising the 1,4-dihydropyridine scaffold and the ester group at the 3 position. Preliminary bioassays showed that most of the target compounds exhibit good insecticidal activities (>80 %) at 100 mg/dm3 against Aphis medicagini, while a 4-fluorophenyl cis-nitenpyram analog afforded the best activity, with >90 % mortality at 20 mg/dm3. These excellent insecticidal activities imply that this huge conjugated system results in an enhanced π-π interaction between the molecule and amino acid residues in receptors. Further studies on the mode of action of one of these cis-nitenpyram analogs and structural modifications are in progress.
Synthesis and histamine H2 agonistic activity of arpromidine analogues: replacement of the pheniramine-like moiety by non-heterocyclic groups
Buschauer, A,Friese-Kimmel A,Baumann, G,Schunack, W
, p. 321 - 330 (2007/10/02)
Analogues of the potent histamine H2 agonist arpromidine, characterized by non-hetrocyclic groups (phenyl, cyclohexyl, alkyl) instead of the pheniramine-like portion, were prepared and tested for their H2 agonistic and H1 antagonistic activity in the isolated guiea pig right atrium and ileum, respectively.In the diphenylpropylguanidine series an increase in H2 agonistic potency resulted from mono- or difluorination at one or both phenyl rings in the meta and/or para position (pD2 7.75 vs pD2 = 7.15 for the unsubstituted parent compound).Compounds chlorinated atboth phenyl rings were considerably less potent.Highest combined H2 agonistic/H1 antagonistic potency was found in the 4-fluorophenyl series.The arpromidine analogue with cyclohexyl and methyl group instead of phenyl and pyridine ring proved to be 30 times more potent than histamine in the atrium.The H1 antagonistic potency in cyclohexyl compounds was lower than in the diaryl series.Thus, aromatic rings appear not to be required for high H2 agonistic potency but are useful for combined H2 agonistic/H1 antagonistic activity. histamine / H2 receptor / H2 agonist / arpromidine / impromidine / H1 antagonist / antihistamine
