19380-80-4Relevant academic research and scientific papers
Synthesis, biological evaluation, and metabolic stability of chlorogenic acid derivatives possessing thiazole as potent inhibitors of α-MSH-stimulated melanogenesis
Jo, Hyeju,Zhou, Yuanyuan,Viji, Mayavan,Choi, Minho,Lim, Jae Young,Sim, Jaeuk,Rhee, Jeongtae,Kim, Youngsoo,Seo, Seung-Yong,Kim, Wun-Jae,Hong, Jin Tae,Lee, Heesoon,Lee, Kiho,Jung, Jae-Kyung
supporting information, p. 4854 - 4857 (2017/10/06)
A series of catechol and dioxolane analogs containing thiazole CGA derivatives have been synthesized and evaluated for their inhibitory activity against α-MSH. The inhibitory activity was improved by replacing an α,β-unsaturated carbonyl of previously reported caffeamides with thiazole motif. Surprisingly, compound 7d, one of the derivatives of dioxolane analogs, displayed the most potent inhibitory activity with an IC50 of 0.90 μM. Further studies on metabolic stability and bioactivation potential were also accomplished.
Novel Chlorogenic Acid Derivatives and Anti-Inflammatory and Skin Whitening Composition Comprising the Same
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Paragraph 0163-0165, (2016/12/01)
The present invention relates to a novel chlorogenic acid derivative compound having an anti-inflammatory activity and a skin whitening activity, a use of the compound, and a manufacturing method of the compound. The compound of the present invention inhibits an NF- κB activation path, and inhibits an activity of α-melanocyte-stimulating hormone (α-MSH), thereby having the anti-inflammatory activity and the skin whitening activity. The compound of the present invention can be developed as a treating agent of inflammatory diseases and a skin whitening agent.
COMPOSITIONS AND METHODS FOR THE TREATMENT OF MALARIA
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Page/Page column 73; 74, (2014/10/15)
The present invention provides aminohydantoin anti-malarial agents. In some embodiments, these agents have the property of functions of targeting malarial aspartic proteases while at the same time having low activity against human BACE. Methods of employing such agents are also provided.
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.
