2763-93-1Relevant academic research and scientific papers
Design, synthesis, and herbicidal activities of novel 2-cyanoacrylates containing isoxazole moieties
Liu, Yuxiu,Cui, Zhipeng,Liu, Bin,Cai, Baoli,Li, Yonghong,Wang, Qingmin
experimental part, p. 2685 - 2689 (2011/07/07)
A series of novel 2-cyanoacrylates containing an isoxazole moiety were designed and synthesized. Their structures were characterized by 1H NMR and elemental analysis (or high-resolution mass spectrometry). Their herbicidal activities against four species were evaluated, and the results indicated that some of the title compounds showed excellent herbicidal activities against rape and amaranth pigweed in postemergence treatment even at a dose of 75 g/ha.
Synthesis and pharmacological profile of a series of 2,5-substituted-N,N-dimethyltryptamine derivatives as novel antagonists for the vascular 5-HT1B-like receptor
Moloney, Gerard P.,Martin, Graeme R.,Mathews, Neil,Hobbs, Heather,Dodsworth, Susan,Sang, Pang Yih,Knight, Cameron,Maxwell, Miles,Glen, Robert C.
, p. 2713 - 2723 (2007/10/03)
The coronary 5-HT1B-like receptor has been implicated in vasospasm and it is postulated that a 5-HT1B-like antagonist may block the detrimental action of 5-HT whilst not interfering with normal blood vessel function. The synthesis and pharmacological profile of a novel series of 2-(N-heteroaryl)carboxamido-5-substituted-N,N-dimethyltryptamine derivatives as silent (as judged by the inability of angiotensin II to unmask 5-HT1B-like receptor mediated agonist activity in the rabbit femoral artery), competitive and selective 5-HT1B-like receptor antagonists is described. Modifications to the 2-carboxamido sidechain as well as the 5-ethylene linked heterocycle are explored. N-Furfuryl-5-[2-(N-phthalimido)ethyl]-3-[2-(dimethylamino)ethyl]-1H-indole-2- carboxamide (34) was discovered which fulfilled our in vitro selection criteria and which had a favourable pharmacokinetic profile. Compound 34 showed good affinity (pKB = 7.38) for the vascular 5-HT1B-like receptor and greater than 125 fold selectivity over α1-adrenoceptor affinity. The selectivity of 34 and related compounds for the 5-HT1B-like receptor over other receptor subtypes is discussed and a mode of binding for this class of compound to a pharmacophore model is proposed. The Royal Society of Chemistry 1999.
BROMONITRILE OXIDE CYCLOADDITIONS IN WATER
Rohloff, John C.,Robinson, James III,Gardner, John O.
, p. 3113 - 3116 (2007/10/02)
Bromonitrile oxide can be generated homogeneously in water at acidic pH, allowing efficient cycloaddition with water soluble olefins and acetylenes.Allylammonium salts react with high regioselectivity and without the need for N-group protection. Keyword: Acivicin; transglutaminase; cysteine; 4,5-dihydroisoxazole; dibromonoformaldoxime.
An improved synthesis of muscimol
Pevarello,Varasi
, p. 1939 - 1948 (2007/10/02)
A regiospecific 1,3-dipolar cycloaddition/elimination is the key-step of a convenient, gram-scale synthesis of the GABA-agonist muscimol (1).
