10472-88-5Relevant articles and documents
Directed biosynthesis of 5'-fluoropactamycin in Streptomyces pactum
Adams,Rinehart
, p. 1456 - 1465 (1994)
A new pactamycin analogue, 5'-fluoropactamycin, was prepared by directed biosynthesis. Supplementation of the fermentation medium of Streptomyces pactum, var. pactum with 3-amino-5-fluorobenzoic acid, an analogue of 3-aminobenzoic acid, an advanced precursor in pactamycin biosynthesis, resulted in co-production of pactamycin and the new pactamycin analogue. A similar feeding experiment with 3-amino-5-methylbenzoic acid did not result in formation of the corresponding methylated pactamycin analogue, but only in inhibition of pactamycin production. Comparison of antimicrobial and cytotoxic activities of pactamycin and 5'-fluoropactamycin showed no significant differences.
Fluorine atom substituted benzo heterocycle based conjugated molecule material as well as preparation method and application thereof
-
Paragraph 0094; 0097; 0098; 0099, (2018/07/30)
The invention discloses a fluorine atom substituted benzo heterocycle based conjugated molecule material as well as a preparation method and application thereof. The conjugated molecule material is ofan acceptor-donor-acceptor type structure, wherein an a
Potent mGluR5 antagonists: Pyridyl and thiazolyl-ethynyl-3,5-disubstituted- phenyl series
Alagille, David,Dacosta, Herve,Chen, Yelin,Hemstapat, Kamondanai,Rodriguez, Alice,Baldwin, Ronald M.,Conn, Jeffrey P.,Tamagnan, Gilles D.
supporting information; experimental part, p. 3243 - 3247 (2011/07/07)
We report the synthesis of four series of 3,5-disubstituted-phenyl ligands targeting the metabotropic glutamate receptor subtype 5: (2-methylthiazol-4-yl) ethynyl (1a-j,), (6-methylpyridin-2-yl)ethynyl (2a-j), (5-methylpyridin-2-yl) ethynyl (3a-j,), and (pyridin-2-yl)ethynyl (4a-j,). The compounds were evaluated for antagonism of glutamate-mediated mobilization of internal calcium in an mGluR5 in vitro assay. All compounds were found to be full antagonists and exhibited low nanomolar to subnanomolar activity.