110202-78-3Relevant academic research and scientific papers
Anacardic acid derivatives as inhibitors of glyceraldehyde-3-phosphate dehydrogenase from Trypanosoma cruzi
Pereira, Junia M.,Severino, Richele P.,Vieira, Paulo C.,Fernandes, Joao B.,da Silva, M. Fatima G.F.,Zottis, Aderson,Andricopulo, Adriano D.,Oliva, Glaucius,Correa, Arlene G.
, p. 8889 - 8895 (2008/12/23)
Chagas' disease, a parasitic infection caused by the flagellate protozoan Trypanosoma cruzi, is a major public health problem affecting millions of individuals in Latin America. On the basis of the essential role in the life cycle of T. cruzi, the glycolytic enzyme glyceraldehyde-3-phosphate dehydrogenase (GAPDH) has been considered an attractive target for the development of novel antitrypanosomatid agents. In the present work, we describe the inhibitory effects of a small library of natural and synthetic anacardic acid derivatives against the target enzyme. The most potent inhibitors, 6-n-pentadecyl- (1) and 6-n-dodecylsalicilic acids (10e), have IC50 values of 28 and 55 μM, respectively. The inhibition was not reversed or prevented by the addition of Triton X-100, indicating that aggregate-based inhibition did not occur. In addition, detailed mechanistic characterization of the effects of these compounds on the T. cruzi GAPDH-catalyzed reaction showed clear noncompetitive inhibition with respect to both substrate and cofactor.
Synthetic studies of thiazoline and thiazolidine-containing natural products - 1. Phosphorus pentachloride-mediated thiazoline construction reaction
Ino, Akira,Murabayashi, Akira
, p. 10271 - 10282 (2007/10/03)
Phosphorus pentachloride effectively mediates the cyclization of N- acylcysteamine derivatives giving rise to thiazoline rings. Using this method, sterically hindered thiazoline analogs could be constructed and thus segment A (the left half) of micacocidin, a unique antimycoplasma antibiotic, was synthesized efficiently.
SYNTHESES OF ANACARDIC ACIDS AND GINKGOIC ACID
Yamagiwa, Yoshiro,Ohashi, Kinji,Sakamoto, Yoshitaka,Hirakawa, Shinji,Kamikawa, Tadao,Kubo, Isao
, p. 3387 - 3394 (2007/10/02)
Syntheses of two anacardic acids , inhibitors of prostaglandin synthetase and of the growth of certain insects, and ginkgoic acid via directive metallation is reported.
Prostaglandin Synthetase Inhibitors from the African Medicinal Plant
Kubo, Isao,Kim, Mujo,Komatsu, Sakae,Yamagiwa, Yoshiro,Ohashi, Kinji,et al.
, p. 1101 - 1104 (2007/10/02)
Two prostaglandin synthetase inhibitory anacardic acids were isolated from O. mucronata.The structures of these inhibitors were established by spectroscopic means.Efficient syntheses of these two via directive metallation were reported.
