827-51-0Relevant articles and documents
Synthesis and pharmacological evaluation of 2,3-dialkylindoles, 'in vitro' inhibitors of thrombin-induced platelet aggregation
Arcari,Aveta,Brandt,Cecchetelli,Corsi,Solinas
, p. 405 - 425 (2007/10/02)
A series of 2,3-dialkylindoles (1-5) have been prepared and tested as antithrombotic agents. The whole class showed in vitro interesting activity in the inhibition of thrombin-induced aggregation. Among these compounds some ones showed activity comparable to standards also in the inhibition of collagen-induced aggregation. Owing to a very fast metabolic degradation through a beta-oxidative mechanism, a drastic decrease of activity in several tests ex vivo or in vivo was observed.
An efficient, one-pot synthesis of 3-alkyl or aryl sydnoneimines
Beal,Turnbull
, p. 673 - 676 (2007/10/02)
In a 'one-pot' process, a variety of 3-alkyl and 3-aryl sydnoneimine hydrochlorides can be prepared in high yield, under mild conditions, by nitrosation of the corresponding aminoacetonitrile with isoamyl nitrite in diethyl ether followed by cyclization w
A Model for Metabolic Activation of Dialkylnitrosoamines. Oxidative Dealkylation 2-(N-Nitrosoalkylamino)acetonitriles by a Flavin Mimic in Aqueous Solution
Yano, Yumihiko,Yokoyama, Takeshi,Ikuta, Masato,Yoshida, Kitaro
, p. 5606 - 5610 (2007/10/02)
It is found for the first time that a flavin mimic, benzodipteridine (BDP), reacts with 2-(N-nitrosoalkylamino)acetonitriles via oxidative dealkylation to yield the corresponding alcohols (ROH) and the 2-e-reduced BDP in aqueous acetonitrile.Kinetic studies reveal that the rates are first order with respect to and ->, respectively.Kinetic isotope effects (kH/kD) for RN(NO)CD2CN (R = Me, n-Bu, Ph, and PhCH2) are found to be 2.2-4.2, indicating that deprotonation is involved in the rate-determining step.The mechanism of the oxidative dealkylation of the nitrosoamines by the flavin mimic is discussed.
