Mingji Dai,Samuel J Danishefsky
Mingji Dai
The feasibility of a hypervalent iodine-mediated oxidative dearomatization/cyclization to produce the oxabicyclo[3.2.1]octene of cortistatin A has been demonstrated through a model study. An interesting tandem cyclization via a Ritter inter...
SYNTHETIC APPROACHES TO 4,8-DIMETHYL-4'- (N-PYRIDINIUMMETHYL)- 4',5'-DIHYDROPSORALENS AND THEIR ACTIVITY AGAINST PAM 212 KERATINOCYTES [0.03%]
4,8-二甲基-4'-(N-吡啶鎓甲基)-4',5'-二氢刺槐素的合成及其对PAM 212角质形成细胞的活性研究
Marilyn S Whittemore,Ned D Heindel,Christophe D Guillon et al.
Marilyn S Whittemore et al.
Synthetic approaches to novel 4,8-dimethyl-4'-halomethyl-4',5'-dihydropsoralens as synthetic precursors to 4,8-dimethyl-4'-(N-pyridiniummethyl)-4',5'-dihydropsoralens are described. The compounds are potential therapeutic agents for improve...
SYNTHESIS OF PROBE MOLECULES, 6-(DIMETHYLAMINO)-2-PHENYLISOINDOLIN-1-ONES, FOR MECHANISTIC STUDIES OF FIREFLY LUCIFERASE INHIBITION [0.03%]
萤火虫荧光素酶抑制机理研究探针分子6-(二甲基氨基)-2-苯基异吲哚啉-1-酮的合成
Medha J Gunaratna,Bo Hao,Man Zhang et al.
Medha J Gunaratna et al.
Firefly luciferase is used in high-throughput screening based on the detection of chemiluminescence. It catalyzes an esterification reaction of luciferin with adenosine 5'-triphosphate (ATP) followed by decarbonylation with oxygen and conco...
SYNTHESIS OF 1,3,4-OXADIAZOLES AS SELECTIVE T-TYPE CALCIUM CHANNEL INHIBITORS [0.03%]
1,3,4-噁二唑作为选择性T型钙通道抑制剂的合成
Man Zhang,Bende Zou,Medha J Gunaratna et al.
Man Zhang et al.
Neuropathic pain, epilepsy, insomnia, and tremor disorder may arrive from an increase of intracellular Ca2+ concentration through a dysfunction of T-type Ca2+ channels. Thus, T-type calcium channels could be a target in drug discovery for t...
MULTICOMPONENT REACTIONS: SYNTHESIS OF SPIROCYCLIC TETRAHYDROPYRAN DERIVATIVES BY PRINS CYCLIZATION [0.03%]
Prins环化合成螺杂环四氢吡喃类化合物
Arun K Ghosh,Dongwoo Shin,Gary Schiltz
Arun K Ghosh
Substituted spirocyclic tetrahydropyranyl mesylates and tosylates have been synthesized in good yields using a Prins-type cyclization of various cyclic ketones, a homoallylic alcohol and either methanesulfonic or p-toluenesulfonic acid unde...
DE NOVO ASYMMETRIC APPROACH TO THE DISACCHARIDE PORTION OF SCH-47554 [0.03%]
从头合成不对称构建SCH-47554的双糖部分
Xiaomei Yu,Miaosheng Li,George A O&#x;Doherty
Xiaomei Yu
A method for the asymmetric synthesis of the disaccharide portion of SCH-47554 has been developed in 6 steps. The route is shorter than the reported route to a related disaccharide. The route involves the use of the Noyori reduction to esta...
A FISCHER INDOLIZATION STRATEGY TOWARD THE TOTAL SYNTHESIS OF (-)-GONIOMITINE [0.03%]
应用 Fischer 偏烃合成 (-)-Goniomitine 的全合成
Beau P Pritchett,Jun Kikuchi,Yoshitaka Numajiri et al.
Beau P Pritchett et al.
A Fischer indolization strategy toward the core of (-)-goniomitine is reported. Initial investigations into the Pd-catalyzed asymmetric allylic alkylation of dihydropyrido[1,2-a]indolone (DHPI) substrates are also discussed.
Kenneth A Jacobson,Kenneth L Kirk
Kenneth A Jacobson
John W. Daly was engaged in groundbreaking basic research for nearly 50 years at NIH in Bethesda, Maryland. A primary focus of his research included the discovery, structure elucidation, synthesis and pharmacology of alkaloids and other bio...
Bertil B Fredholm,Kenneth A Jacobson
Bertil B Fredholm
John Daly played an important role in defining adenosine receptors as an important target for drug discovery. His systematic work characterized the effects of adenosine analogues on cyclic AMP in the brain that were antagonized by methylxan...
EPIBATIDINE ANALOGS SYNTHESIZED FOR CHARACTERIZATION OF NICOTINIC PHARMACOPHORES-A REVIEW [0.03%]
用于表征烟碱药效团的埃吡巴丁类似物合成的研究进展综述
F Ivy Carroll
F Ivy Carroll
In 1992 Daly and co-workers reported the isolation of a new natural product, epibatidine. Future studies showed that epibatidine was an nAChR ligand with analgesic potency 200-400 times greater than that of morphine. However, its potential ...