39870-05-8Relevant articles and documents
Synthesis and evaluation of the 2-aminothiazoles as anti-tubercular agents
Kesicki, Edward A.,Bailey, Mai A.,Ovechkina, Yulia,Early, Julie V.,Alling, Torey,Bowman, Julie,Zuniga, Edison S.,Dalai, Suryakanta,Kumar, Naresh,Masquelin, Thierry,Hipskind, Philip A.,Odingo, Joshua O.,Parish, Tanya
, (2016/06/01)
The 2-aminothiazole series has anti-bacterial activity against the important global pathogen Mycobacterium tuberculosis. We explored the nature of the activity by designing and synthesizing a large number of analogs and testing these for activity against M. tuberculosis, as well as eukaryotic cells. We determined that the C-2 position of the thiazole can accommodate a range of lipophilic substitutions, while both the C-4 position and the thiazole core are sensitive to change. The series has good activity against M. tuberculosis growth with sub-micromolar minimum inhibitory concentrations being achieved. A representative analog was selective for mycobacterial species over other bacteria and was rapidly bactericidal against replicating M. tuberculosis. The mode of action does not appear to involve iron chelation. We conclude that this series has potential for further development as novel antitubercular agents.
PYRIMIDYLPYRROLE DERIVATIVES ACTIVE AS KINASE INHIBITORS
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Page/Page column 24, (2010/02/10)
Pyrimidylpyrrole derivatives of formula (1) and pharmaceutically acceptable salts thereof, as defined in the specification, process for their preparation and pharmaceutical compositions comprising them are disclosed; the compounds of the invention may be
Substituent Effects on Photochemical Hydrogen Abstraction in 2-Acylpyridines, 2-Acylpyrazines, and 4-Acylpyrimidines
Rao, C. Janakiram,Agosta, William C.
, p. 2125 - 2131 (2007/10/02)
Stern-Volmer quenching of the photochemistry of 1c indicates that N- and O-abstraction (eqs 1 and 2, respectively) are quenched at different rates (Figure 1).For quenching of 2c kqτ is 157 M-1 and for 3c, 64 M-1.When 1c is sensitized with triplet sensitizers of increasing ET,N-abstraction increases (Table 1).These data indicate that N- and O-abstraction in 1c take place from distiguishable triplet states.Survey of Φp's of ring-substituted ketones 1b-d, 6d, 7a,b,d, 8b, 9b,d, 10b, and 11d demonstartes the effect of substitution on the competition between N- and O-abstraction (Table 2).For methyl- and dicyano-substituted ketones, the results can be understood simply in terms of shifts in ET of the n?* and ??* states of the heterocycle.The photochemistry of all these ketones requires consideration of interactions among three triplet states.
