135030-72-7Relevant academic research and scientific papers
Pyrrolidine inhibitors of human cytosolic phospholipase A2. Part 2: Synthesis of potent and crystallized 4-triphenylmethylthio derivative 'pyrrophenone'
Eno, Kaoru,Okuno, Takayuki,Nishi, Koichi,Murakami, Yasushi,Yamada, Katsutoshi,Nakamoto, Shozo,Ono, Takashi
, p. 587 - 590 (2007/10/03)
We synthesized a potent and crystallized human cytosolic phospholipase A2α inhibitor, pyrrophenone (6) which inhibits the isolated enzyme with an IC50 value of 4.2 nM. Pyrrophenone shows potent inhibition of arachidonic acid release, prostaglandin E2, thromboxane B2, and leukotriene B4 formation in human whole blood. The magnitudes of prostaglandin E2 and thromboxane B2 inhibition are the same as those of indomethacin.
Aryl-fused and hetaryl-fused-2,4-diazepine and 2,4-diazocine antiarrhythmic agents
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, (2008/06/13)
Aryl-fused- and hetaryl-fused-2,4-diazepines of formula XXXVI, benzodiazocines of formula XXX, benzodiazepines of formula II STR1 δ-aminoamides of formula III and aryldimethanamines of formula XXXVII STR2 wherein A is an aryl or hetaryl ring; R1 is hydrogen, alkyl, aryl or hetaryl; R2 is hydrogen, alkyl, substituted alkyl, or aryl; R3 is alkyl, aryl, aralkyl or heteroatom substituted alkyl or aralkyl; R4 is hydrogen or alkyl; R5 is hydrogen, alkyl, aryl or hetaryl; R6 is hydrogen, alkyl, alkoxy, halogen or a fused benzene ring; R9 is hydrogen, alkyl, or substituted alkyl; and R10 is hydrogen, alkyl, or substituted alkyl. The invention further relates to processes for the preparation of, pharmaceutical compositions containing, and methods of treating cardiac arrhythmia with the compounds of formulas XXXVI, XXX, II, III, and XXXVII.
