- TRICYCLIC COMPOUNDS AND THEIR USE
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Tricyclic compounds and their use are provided. More specifically, tricyclic compounds, pharmaceutical compositions containing them, methods for preparing them, and their use in therapy are also provided.
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Page/Page column 90; 91
(2020/12/29)
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- Novel triazole derivative with anti-inflammatory and anti-hyperglycemic activity and method for preparing the same
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The present invention relates to a novel triazole derivative having anti-inflammatory and anti-diabetic activities, to a production method thereof, and to a pharmaceutical composition for preventing or treating inflammatory diseases and diabetic diseases, comprising the same. The novel triazole derivative according to the present invention has excellent inhibitory activity of type II collagen and COX-2 and exhibits anti-inflammatory activity, and thus can be used as a pharmaceutical composition for the preventing or treating inflammatory diseases. In addition, anti-diabetic activity is showed due to excellent inhibitory activities of alpha-glucosidase and alpha-amylase, thereby being able to be used as a pharmaceutical composition for preventing or treating diabetes diseases.COPYRIGHT KIPO 2017
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Paragraph 0074; 0075; 0078
(2017/08/23)
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- Synthesis and Biological Evaluation of New (-)-Gossypol-Derived Schiff Bases and Hydrazones
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A series of 14 new (-)-gossypol Schiff bases and hydrazones have been synthesized via an in situ procedure in high yields. Structural data showed that all target compounds exist as the enamine tautomer. Bioassays showed that several compounds exhibited cytotoxic effects against three human cancer cell lines. Compound 8a showed the greatest cytotoxic effect against hepatocellular carcinoma (HepG2), lung carcinoma (LU-1), and breast cancer (MCF-7) cell lines with IC50 values of 20.93, 13.58, and 9.40 μM, respectively. However, in an antibacterial test, compounds 8a and 8b inhibited Staphylococcus aureus and Bacillus cereus and compound 8e inhibited only Staphylococcus aureus at the same MIC values of 1024 μg/ml.
- Vu, Vu Van,Nhung, Trinh Thi,Thanh, Nguyen Thi,Chinh, Luu Van,Tien, Vu Dinh,Thuy, Vu Thu,Thi Thao, Do,Nam, Nguyen Hai,Koeckritz, Angela,Vu, Tran Khac
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- Synthesis, structural elucidation and bioevaluation of 4-amino-1,2,4-triazole-3-thione's Schiff base derivatives
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In this study, a series of ten triazole Schiff base derivatives 6a-j were synthesized through microwave assisted imine formation by reacting substituted amino triazole 5 with different substituted aldehydes. All the synthesized compounds were evaluated fo
- Rafiq, Muhammad,Saleem, Muhammad,Hanif, Muhammad,Kang, Sung Kwon,Seo, Sung-Yum,Lee, Ki Hwan
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p. 161 - 171
(2016/03/12)
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- Acetylcholinesterase inhibition activity of some quinolinyl substituted triazolothiadiazole derivatives
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A series of aralkanoic acids was converted into aralkanoic acid hydrazides through their esters formation. The aralkanoic acid hydrazides upon treatment with carbon disulfide and methanolic potassium hydroxide yielded potassium dithiocarbazinate salts, which on refluxing with aqueous hydrazine hydrate yielded 5-aralkyl-4-amino-3-mercapto-1,2,4-triazoles. The target compounds, 3-aralkyl-6-(substitutedquinolinyl) [1,2,4]triazolo[3,4-b][1,3,4]thiadiazoles, were synthesized by condensing various quinolinyl substituted carboxylic acids with 5-aralkyl-4-amino-3-mercapto-1,2,4-triazoles in phosphorus oxychloride. The structures of the newly synthesized triazolothiadiazoles were characterized by IR, 1H NMR, 13C NMR, and elemental analysis studies. The structure of one of the 5-aralkyl-4-amino-3-mercapto-1,2,4-triazoles was unambiguously deduced by single crystal X-ray diffraction analysis. All the synthesized compounds were screened for their acetylcholinesterase inhibition activities. Four of the triazolothiadiazoles exhibited excellent acetylcholinesterase inhibition activities as compared to the reference inhibitor.
- Rafiq, Muhammad,Saleem, Muhammad,Hanif, Muhammad,Abbas, Qamar,Lee, Ki Hwan,Seo, Sung-Yum
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p. 170 - 177
(2015/04/14)
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- Synthesis, crystal structure, anti-inflammatory and anti-hyperglycemic activities of novel 3,4-disubstituted 1,2,4-triazol-5(4H)-one derivatives
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A new series of 3,4-disubstituted 1,2,4-triazol-5(4H)-one 5a-r, bearing various methoxyphenyl, fluorophenyl, tolyl and phenyl groups, was synthesized by the dehydrocyclization of hydrazinecarboxamides 4a-r by refluxing in a 2 N sodium hydroxide solution. Hydrazinecarboxamides 4a-r was synthesized via the condensation of the corresponding aralkanoic acid hydrazides, 3a-g, with fluoro-, tolyl- and methoxyphenylisocyanates. The newly synthesized compounds (5ar) were characterized by IR, 1H NMR and 13C NMR analyses. The structure of one compound 5a was determined by single crystal X-ray diffraction analysis. All of the synthesized compounds were screened for their anti-inflammatory and anti-diabetic (α-glucosidase and α-amylase inhibition) activity to identify new drugs that might be useful in preventing damage related to diabetes and inflammation. Compounds 5j, 5k and 5m decrease the expression of type II collagen in a dose dependent manner; similarly 5l decrease the COX-2 expression of rabbit articular chondrocytes in a dose dependent manner possessing potent anti-inflammatory potential while some of derivatives including 5c, 5e, 5g and 5h cause inflammation. Meanwhile, excellent α-glucosidase and moderate α-amylase inhibitory profiles against carbohydrate modulating enzymes were demonstrated by compounds 5b, 5f, 5k and 5q compared to the reference standard acarbose, and compounds 5g, 5h, 5i, 5j, 5l and 5o exhibited moderate to low enzyme inhibition potential among the series.
- Saleem, Muhammad,Yu, Seon-Mi,Rafiq, Muhammad,Kim, Song-Ja,Seo, Sung-Yum,Lee, Ki Hwan
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p. 810 - 823
(2015/04/14)
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- Synthesis and biological activities of some new 3,6-disubstituted 1,2,4-triazolo[3,4-b]1,3,4-thiadiazole derivatives
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A series of aromatic hydrazides 3a-j were prepared by refluxing esters 2a-j with hydrazine hydrate in methanol, which were prepared by the esterification of 1a-j. Acetohydrazides 3a-j upon treatment with carbon disulfide and methanolic potassium hydroxide yielded potassium dithiocarbazate salts 4a-j, which on refluxing with hydrazine hydrate yielded substituted 4-amino-5-aryl-3H-1,2,4-triazole-3-thiones 5a-j. The target compounds 6a-j were synthesized by condensing furan-3-carboxylic acid in the presence of polyphosphoric acid under reflux. The structures of newly synthesized compounds were characterized by IR, 1H NMR, 13C NMR, elemental analysis and mass spectrometric studies. All the synthesized compounds were screened for their urease, acetylcholine esterase inhibition, antioxidant and alkaline phosphatase inhibition activity. Almost all of the compounds 6a-j showed good to excellent activities against urease and acetylcholine esterase more than the reference drugs. Compounds 6f and 6g were more potent scavenger of free radicals than the reference n-propyl gallate. Compound 6b and 6h showed excellent activities of alkaline phosphatase as compare to the reference KH 2PO4.
- Rafiq, Muhammad,Saleem, Muhammad,Hanif, Muhammad,Maqsood, Muhammad Rizwan,Rama, Nasim Hasan,Lee, Ki-Hwan,Seo, Sung-Yum
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p. 3943 - 3949
(2013/08/23)
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- Some pyridyl- and thiophenyl- Substituted 1,2,4-triazolo[3,4-b]1,3,4- thiadiazole derivatives as potent antibacterial
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The target compounds 6-11a-e were synthesized by condensing 4-amino-5-aryl-3H-1,2,4-triazole-3-thiones 5a-f with various aromatic carboxylic acids in the presence of phosphorous oxychloride. The structures of newly synthesized compounds were characterized by IR, 1H NMR, 13C NMR, elemental analysis and mass spectrometric studies. All the synthesized compounds were screened for their antibacterial activity. Almost all the tested compounds were potent against four different strains of bacteria when compared with that of reference drug ciprofloxacin. Compounds 6c, 6e, 8d, 9b, 9e, 11a and 11b showed nearly equal or lower MIC values than standard drug, against all four tested bacterial strains but rest of the compounds showed excellent antibacterial activities.
- Maqsood, Muhammad Rizwan,Hanif, Muhammad,Rafiq, Muhammad,Saleem, Muhammad,Zaib, Sumera,Khan, Aftab Ahmed,Iqbal, Mazhar,Iqbal, Jamshed,Rama, Nasim Hasan,Seo, Sung-Yum,Lee, Ki-Hwan
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p. 4180 - 4184
(2013/08/23)
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