145383-01-3Relevant articles and documents
ANTIVIRAL COMPOUNDS AND USE THEREOF
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Page/Page column 36-38, (2019/10/04)
The present invention relates to compounds of formula (I), their use as medicaments, in particular as broad spectrum antiviral agents, their combination with a further antiviral agent and relative pharmaceutical compositions. In particular, the compounds of the invention are useful in the treatment of a disease caused by an enveloped virus.
Structural requirement(s) of N-phenylthioureas and benzaldehyde thiosemicarbazones as inhibitors of melanogenesis in melanoma B 16 cells
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
supporting information; experimental part, p. 2991 - 2993 (2010/08/06)
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.
Clobenpropit analogs as dual activity ligands for the histamine H3 and H4 receptors: Synthesis, pharmacological evaluation, and cross-target QSAR studies
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.
experimental part, p. 3987 - 3994 (2009/10/02)
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.
Isothiourea analogues of histamine as potent agonists or antagonists of the histamine H3-receptor
Van der Goot,Schepers,Sterk,Timmerman
, p. 511 - 517 (2007/10/02)
The synthesis and H3-activity of a series of isothiourea analogues of histamine have been described. It has been shown that S-[2-(4(5)-imidazolyl)ethylisothiourea (VUF 8325) is a potent H3-agonist measured as the electrically evoked contraction of the guinea-pig ileum. Upon methylation of the imidazole system or the isothiourea moiety a decrease in affinity was observed leading to either weak agonists or weak antagonists. Introduction of N-(phenylalkyl) substituents at the isothiourea part gives rise to highly potent H3-antagonists. Particularly the 4-chlorobenzyl group appeared to be favourable in the series described resulting in a histamine H3-antagonist with a pA2-value of 9.9.
