46124-27-0Relevant academic research and scientific papers
Structure-activity relationship study of the bacterial actin-like protein MreB inhibitors: Effects of substitution of benzyl group in S-benzylisothiourea
Iwai, Noritaka,Fujii, Takuya,Nagura, Hirokatsu,Wachi, Masaaki,Kitazume, Tomoya
, p. 246 - 248 (2008/03/13)
We comprehensively investigated the effects of substitution of the benzyl group in S-benzylisothiourea derivatives on antibacterial activity, because we found previously that some substitutions enhanced it. A 2,4-Cl 2-derivative was found to be the most effective compound, it was stronger than the original one in Gram-negative rod shaped-bacteria such as Escherichia coli and Salmonella typhimurium.
Antibiotics targeting MreB
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Page/Page column 11, (2008/06/13)
The identification of MreB as essential for bacterial chromosome segregation provides a new target for antibiotic action. The MreB function is useful in the development of screening assays for new antibiotics, which may use, for example, genetic mutants i
Structure-activity relationship of S-benzylisothiourea derivatives to induce spherical cells in Escherichia coli
Iwai, Noritaka,Ebata, Takuma,Nagura, Hirokatsu,Kitazume, Tomoya,Nagai, Kazuo,Wachi, Masaaki
, p. 2265 - 2269 (2007/10/03)
We have previously reported that a novel S-benzylisothiourea derivative, S-(3,4-dichlorobenzyl)isothiourea, tentatively named A22, induced spherical cells in Escherichia coli. To elucidate the structural element(s) required for inducing these spherical ce
Synthesis and Biological Activity of trans-(+/-)-N-Methyl-2-(3-pirydyl)-2-tetrahydrothiopyrancarbothioamide 1-Oxide (RP 49356) and Analogues: A New Class of Potassium Channel Opener
Brown, Thomas J.,Chapman, Robert F.,Cook, David C.,Hart, Terance W.,McLay, Iain M.,et al.
, p. 3613 - 3624 (2007/10/02)
The synthesis and biological activity of trans-(+/-)-N-methyl-2-(3-pyridyl)-2-tetrahydrothiopyrancarbothioamide 1-oxide (8a, RP 49356) and analoques is reported.These compounds constitute a new structural class of K+-channel opener.The effects of changes in the pyridyl group, thioamide, and thiane ring on in vitro K+-channel opening activity are discussed.A 3-pyridyl or 3-quinolyl group, a small N-alkyl thioamide function, and a thiane oxide ring, in which the sulfoxide is in a trans relationship to thioamide, are preferred for activity.Selected compounds were tested intravenously in the normotensive anaesthetized rat for hypotensive effects, and the activities reflect their in vitro K+-channel opening activity.This led to further evaluation of compound 8a and the selection of the (-)-enantiomer 8b (RP 52891) for development as an antihypertensive and antianginal agent.
