73870-25-4Relevant articles and documents
Peptidomimetic Vinyl Heterocyclic Inhibitors of Cruzain Effect Antitrypanosomal Activity
Chenna, Bala C.,Li, Linfeng,Mellott, Drake M.,Zhai, Xiang,Siqueira-Neto, Jair L.,Calvet Alvarez, Claudia,Bernatchez, Jean A.,Desormeaux, Emily,Alvarez Hernandez, Elizabeth,Gomez, Jana,McKerrow, James H.,Cruz-Reyes, Jorge,Meek, Thomas D.
, p. 3298 - 3316 (2020/04/08)
Cruzain, an essential cysteine protease of the parasitic protozoan, Trypanosoma cruzi, is an important drug target for Chagas disease. We describe here a new series of reversible but time-dependent inhibitors of cruzain, composed of a dipeptide scaffold appended to vinyl heterocycles meant to provide replacements for the irreversible reactive "warheads" of vinyl sulfone inactivators of cruzain. Peptidomimetic vinyl heterocyclic inhibitors (PVHIs) containing Cbz-Phe-Phe/homoPhe scaffolds with vinyl-2-pyrimidine, vinyl-2-pyridine, and vinyl-2-(N-methyl)-pyridine groups conferred reversible, time-dependent inhibition of cruzain (Ki? = 0.1-0.4 μM). These cruzain inhibitors exhibited moderate to excellent selectivity versus human cathepsins B, L, and S and showed no apparent toxicity to human cells but were effective in cell cultures of Trypanosoma brucei brucei (EC50 = 1-15 μM) and eliminated T. cruzi in infected murine cardiomyoblasts (EC50 = 5-8 μM). PVHIs represent a new class of cruzain inhibitors that could progress to viable candidate compounds to treat Chagas disease and human sleeping sickness.
Br?nsted acid-catalysed conjugate addition of photochemically generated α-amino radicals to alkenylpyridines
Hepburn, Hamish B.,Melchiorre, Paolo
supporting information, p. 3520 - 3523 (2016/03/04)
The conjugate addition of α-amino radicals to alkenylpyridines has been accomplished by the synergistic merger of Br?nsted acid and visible light photoredox catalysis. Key to reaction development was the protonation of the alkenylpyridines that transientl
MERCAPTOACYL DERIVATIVES OF VARIOUS 4-SUBSTITUTED PROLINES
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, (2008/06/13)
This invention is directed to compounds of the formula STR1 and various intermediates therefore. The final products possess useful hypotensive activity.
SYNTHESIS OF CAROTENOID ANALOGUES HAVING PYRIDINE, FURAN, AND TIOPHENE RINGS AS TERMINAL GROUPS
Brahmana, Hemat R.,Katsuyama, Kazuki,Inanaga, Junji,Katsuki, Tsutomi,Yamaguchi, Masaru
, p. 1695 - 1696 (2007/10/02)
Heteroaromatic carotenoid analogues having 2-pyridyl, 3-pyridyl, 2-furyl, 3-furyl, 2-thienyl, and 3-thienyl groups at both the ends of tetramethyloctadecanonaene chain, were synthesized and their spectral properties were examined.
Two Step Redox Systems, XXVII. - Vinylogous Bipyridyls and Biquinolyls; Syntheses and UV/VIS-Spectra
Carsky, Petr,Huenig, Siegfried,Stemmler, Ingo,Scheutzow, Dieter
, p. 291 - 304 (2007/10/02)
The vinylogous 2,2'-, 2,4'- and 4,4'-bipyridyls 1(n=2,3), 2(n=2) and 3(n=2,3) together with the corresponding 2,2'-, 2,4'- and 4,4'-biquinolyls 4(n=2,3), 5(n=2) and 6(n=2,3) are synthesized, partly by different routes.Their UV/VIS spectra are described.