- 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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- Structural requirement(s) of N-phenylthioureas and benzaldehyde thiosemicarbazones as inhibitors of melanogenesis in melanoma B 16 cells
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In order to define the structural requirements of phenylthiourea (PTU), a series of thiourea and thiosemicarbazone analogs were prepared and evaluated as inhibitors of melanogenesis in melanoma B16 cells. The most potent analog was 2-(4-tert-butylbenzylidene)hydrazinecarbothioamide (1u) with an IC50 value of 2.7 μM in inhibition of melanogenesis. The structure for potent inhibitory activity of these derivatives are required with the direct connection of π-planar structure to thiourea without steric hinderance in PTU derivatives and the hydrophobic substituent at para position in case of semicarbazones.
- Thanigaimalai,Le Hoang, Tuan Anh,Lee, Ki-Cheul,Bang, Seong-Cheol,Sharma, Vinay K.,Yun, Cheong-Yong,Roh, Eunmiri,Hwang, Bang-Yeon,Kim, Youngsoo,Jung, Sang-Hun
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supporting information; experimental part
p. 2991 - 2993
(2010/08/06)
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- Improved Procedures for the Preparation of Cycloalkyl-, Arylalkyl-, and Arylthioureas
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An improved procedure for the preparation of arylthioureas consists of the reaction of benzoyl isothiocyanate with anilines in acetone and debenzoylation of the resultant N-aryl-N'-benzoylthioureas with 5percent aqueous sodium hydroxide.Bicycloalkylthioureas and N-(arylalkyl)thioureas (e.g. 9H-9-fluorenylthiourea) are directly prepared from the corresponding isothiocyanates and ammonia.
- Rasmussen, C. R.,Villani, F. J.,Weaner, L. E.,Reynolds, B. E.,Hood, A. R.,et al.
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p. 456 - 459
(2007/10/02)
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