Search

Your search keyword '"Phuong, Thao Tran"' showing total 4 results
Start Over Author "Phuong, Thao Tran" Journal bioorganic & medicinal chemistry letters
4 results on '"Phuong, Thao Tran"'

1. Inhibitory effects of compounds from Styrax obassia on NO production

Author

Jeong Ah Kim, Phuong-Thao Tran, Manh Hung Tran, Byung Sun Min, Jeong-Hyung Lee, Mi Hee Woo, Hyeong-Kyu Lee, and Thao Quyen Cao

Subjects
Lipopolysaccharide, Stereochemistry, Clinical Biochemistry, Nitric Oxide Synthase Type II, Pharmaceutical Science, Anisoles, Nitric Oxide, Biochemistry, Styrax, Cell Line, Nitric oxide, Terpene, Mice, chemistry.chemical_compound, Triterpene, Drug Discovery, Animals, Benzofuran, Molecular Biology, Benzofurans, chemistry.chemical_classification, Cyclooxygenase 2 Inhibitors, biology, Anti-Inflammatory Agents, Non-Steroidal, Organic Chemistry, biology.organism_classification, Triterpenes, Styrax obassia, chemistry, Cyclooxygenase 2, Cell culture, Plant Bark, Molecular Medicine
Abstract

Two new benzofurans, 2-(3,4-dimethoxyphenyl)-5-(1,3-dihydroxypropyl)-7-methoxybenzofuran (1) and 2-(3,4-methylenedioxyphenyl)-5-(3-hydroxymethyletoxy-1-hydroxypropyl)-7-methoxybenzofuran (2), a new triterpene, 3β, 6β, 21β-trihydroxyolean-12-ene (3), and eleven known compounds were isolated from the stem bark of Styrax obassia. The structures of the isolated compounds were established by extensive spectroscopic analyses, including 1D and 2D NMR and HRMS. Their anti-inflammatory activities were evaluated against lipopolysaccharide (LPS)-induced nitric oxide (NO) production in RAW264.7 macrophages. Compound 1 was shown to reduce LPS-induced iNOS expression in a dose-dependent manner. In addition, pretreating cells with 1 significantly suppressed their LPS-induced expression of COX-2 protein.

Published
2015

2. α-Substituted 2-(3-fluoro-4-methylsulfonamidophenyl)acetamides as potent TRPV1 antagonists

Author

Minghua Cui, Mannkyu Hong, Phuong-Thao Tran, Ho Shin Kim, Jeewoo Lee, Hannelore Stockhausen, Sun Choi, Gregor Bahrenberg, Changhoon Kim, Van Hoa Ngo, Sungeun Kim, Van-Hai Hoang, Jihyae Ann, Robert Frank-Foltyn, Peter M. Blumberg, Sunhye Hong, and Thomas Christoph

Subjects
Stereochemistry, Clinical Biochemistry, Substituent, TRPV1, TRPV Cation Channels, Pharmaceutical Science, CHO Cells, Biochemistry, Article, Structure-Activity Relationship, chemistry.chemical_compound, Cricetulus, Cricetinae, Acetamides, Drug Discovery, Animals, Potency, Molecular Biology, Molecular Structure, Organic Chemistry, Propanamide, chemistry, Docking (molecular), Capsaicin, Molecular Medicine, Antagonism, Acetamide
Abstract

A series of α-substituted acetamide derivatives of previously reported 2-(3-fluoro-4-methylsulfonamidophenyl)propanamide leads (1, 2) were investigated for antagonism of hTRPV1 activation by capsaicin. Compound 34, which possesses an α-m-tolyl substituent, showed highly potent and selective antagonism of capsaicin with Ki(CAP) = 0.1 nM. It thus reflected a 3-fold improvement in potency over parent 1. Docking analysis using our homology model indicated that the high potency of 34 might be attributed to a specific hydrophobic interaction of the m-tolyl group with the receptor.

Published
2015

3. 2-Aryl substituted pyridine C-region analogues of 2-(3-fluoro-4-methylsulfonylaminophenyl)propanamides as highly potent TRPV1 antagonists

Author

Mi Yeon Kim, Minghua Cui, Myeong Seop Kim, Sun Choi, Jeewoo Lee, Jieun Byun, HyungChul Ryu, Robert Frank-Foltyn, Ho Shin Kim, Babette Yvonne Koegel, Karam Son, Thomas Christoph, Sven Frormann, Van-Hai Hoang, Sejin Seo, Pankaz K. Sharma, Peter M. Blumberg, Jihyae Ann, Phuong-Thao Tran, and Gregor Bahrenberg

Subjects
Molecular model, Pyridines, Stereochemistry, Clinical Biochemistry, TRPV1, TRPV Cation Channels, Pharmaceutical Science, Biochemistry, Article, Structure-Activity Relationship, chemistry.chemical_compound, Stereospecificity, Drug Discovery, Pyridine, Humans, Potency, Homology modeling, Molecular Biology, Alkyl, chemistry.chemical_classification, Dose-Response Relationship, Drug, Molecular Structure, Organic Chemistry, chemistry, Docking (molecular), Molecular Medicine
Abstract

A series of 2-alkyl/alkenyl pyridine C-region derivatives of 2-(3-fluoro-4-methylsulfonylaminophenyl)propanamides were investigated as hTRPV1 antagonists. Multiple compounds showed excellent and stereospecific TRPV1 antagonism with better potency than previous lead 2. Among them, compound 15f demonstrated a strong analgesic profile in a rat neuropathic pain model and blocked capsaicin-induced hypothermia in a dose-dependent manner. Docking analysis of (S)-15f with our hTRPV1 homology model provided insight into its specific binding mode.

Published
2014

4. α-Methylated simplified resiniferatoxin (sRTX) thiourea analogues as potent and stereospecific TRPV1 antagonists

Author

Mi-Kyoung Jin, Van-Hai Hoang, Sang-Uk Kang, Jeewoo Lee, Ju-Ok Lim, Ho Shin Kim, Vladimir A. Pavlyukovets, Tae-Hwan Ha, Phuong-Thao Tran, Peter M. Blumberg, Jihyae Ann, and Larry V. Pearce

Subjects
Stereochemistry, Clinical Biochemistry, TRPV1, Resiniferatoxin, TRPV Cation Channels, Pharmaceutical Science, CHO Cells, Methylation, Biochemistry, Article, Structure-Activity Relationship, chemistry.chemical_compound, Cricetulus, Stereospecificity, Cricetinae, Drug Discovery, Animals, Humans, Receptor, Molecular Biology, Molecular Structure, Organic Chemistry, Thiourea, Stereoisomerism, Rats, chemistry, Molecular Medicine, Diterpenes, Antagonism, Protein Binding
Abstract

A series of α-methylated analogues of the potent sRTX thiourea antagonists were investigated as rTRPV1 ligands in order to examine the effect of α-methylation on receptor activity. The SAR analysis indicated that activity was stereospecific with the (R)-configuration of the newly formed chiral center providing high binding affinity and potent antagonism while the configuration of the C-region was not significant.

Published
2014

Catalog

Books, media, physical & digital resources
See catalog results