- Antitubercular activities of the novel synthesized 1,2,4-triazole derivatives
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1,2,4-Triazoles exert antimycobacterial activity by inhibiting the cell wall biosynthesis. In an attempt to developing lead compounds exhibiting antitubercular activities, a series of 1,2,4-triazole derivatives were synthesized by introducing various substitutes into a scaffold and the antitubercular activity was evaluated. The most potent compounds 3e and 8d showed their minimum inhibitory concentrations against Mycobacterium tuberculosis as 12.5 ??M. The results indicate that those compounds can be considered as leads for further development of new 1,2,4-triazole type candidates with high antitubercular activities.
- Oh, Taegwon,Hayat, Aisal,Yoo, Euna,Cho, Sang-Nae,Sheen, Yhun Yhung,Kim, Dae-Kee,Choo, Hea-Young Park
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- Histone deacetylase activators: N-acetylthioureas serve as highly potent and isozyme selective activators for human histone deacetylase-8 on a fluorescent substrate
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We report, for the first time, that certain N-acetylthiourea derivatives serve as highly potent and isozyme selective activators for the recombinant form of human histone deacetylase-8 in the assay system containing Fluor-de-Lys as a fluorescent substrate. The experimental data reveals that such activating feature is manifested via decrease in the Km value of the enzyme's substrate and increase in the catalytic turnover rate of the enzyme.
- Singh, Raushan K.,Mandal, Tanmay,Balsubramanian, Narayanaganesh,Viaene, Tajae,Leedahl, Travis,Sule, Nitesh,Cook, Gregory,Srivastava
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supporting information; experimental part
p. 5920 - 5923
(2011/10/18)
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- Clobenpropit analogs as dual activity ligands for the histamine H3 and H4 receptors: Synthesis, pharmacological evaluation, and cross-target QSAR studies
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Previous studies have demonstrated that clobenpropit (N-(4-chlorobenzyl)-S-[3-(4(5)-imidazolyl)propyl]isothiourea) binds to both the human histamine H3 receptor (H3R) and H4 receptor (H4R). In this paper, we describe the synthesis and pharmacological characterization of a series of clobenpropit analogs, which vary in the functional group adjacent to the isothiourea moiety in order to study structural requirements for H3R and H4R ligands. The compounds show moderate to high affinity for both the human H3R and H4R. Furthermore, the changes in the functional group attached to the isothiourea moiety modulate the intrinsic activity of the ligands at the H4R, ranging from neutral antagonism to full agonism. QSAR models have been generated in order to explain the H3R and H4R affinities.
- Lim, Herman D.,Istyastono, Enade P.,van de Stolpe, Andrea,Romeo, Giuseppe,Gobbi, Silvia,Schepers, Marjo,Lahaye, Roger,Menge, Wiro M.B.P.,Zuiderveld, Obbe P.,Jongejan, Aldo,Smits, Rogier A.,Bakker, Remko A.,Haaksma, Eric E.J.,Leurs, Rob,de Esch, Iwan J.P.
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experimental part
p. 3987 - 3994
(2009/10/02)
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