- Design, synthesis, biological evaluation, and computational studies of novel thiazolo-pyrazole hybrids as promising selective COX-2 inhibitors: Implementation of apoptotic genes expression for ulcerogenic liability assessment
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A novel series of thiazolo-pyrazole hybrids has been prepared and assessed for their in vitro COX-1/COX-2 inhibitory activity. Compound 6c exhibited the most selective COX-2 inhibition profile (SI of 264) not far of Celecoxib (2 9 4). In-vivo anti-inflamm
- Marzouk, Adel A.,Taher, Ehab S.,Shaykoon, Montaser Sh. A.,Lan, Ping,Abd-Allah, Walaa Hamada,Aboregela, Adel M.,El-Behairy, Mohammed Farrag
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- Synthesis, characterization, free-radical scavenging capacity and antioxidant activity of novel series of hydrazone, 1,3,4-oxadiazole and 1,2,4-triazole derived from 3,5-dimethyl-1H-pyrazole
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Background: Pyrazole is an important class of heterocyclic compound, has been shown to exhibit diverse biological and pharmacological activities such as anti-inflammatory, anti-cancer, antioxidant, etc. Methods: In this study, a series of novel 3,5-dimeth
- Karrouchi, Khalid,Fettach, Saad,Radi, Smaail,Yousfi, El Bekkaye,Taoufik, Jamal,Mabkhot, Yahia Nasser,Alterary, Seham,Faouzi, My El Abbes,Ansar, Muhammed
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p. 712 - 720
(2019/08/26)
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- Synthesis and anti-inflammatory activity of some pyrazole derivatives
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A novel series of pyrazoles containing benzenesulfonamides, 1,3,4-oxadiazole-2-thiones, 4-substituted-1,2,4-triazole-3-thiones, and 2-substituted-1,3,4-thiadiazoles has been synthesized. Anti-inflammatory activity of some synthesized compounds was evaluated in vivo utilizing a standard acute carrageenan-induced paw edema method. The most active anti-inflammatory agents 3, 8f, and 10f were evaluated for ulcerogenic liability in rats compared to indomethacin and celecoxib as reference standards. Molecular modeling studies were initiated herein to validate the attained pharmacological data and provide understandable evidence for the observed anti-inflammatory behavior.
- El-Moghazy, Samir M.,Barsoum, Flora F.,Abdel-Rahman, Hamdy M.,Marzouk, Adel A.
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p. 1722 - 1733,12
(2020/07/30)
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- Synthesis, dimeric crystal structure, and fungicidal activity of 1-(4-methylphenyl)-2-(5-((3,5-dimethyl-1H-pyrazol-1-yl)methyl)-4-phenyl-4H-1,2, 4-triazol-3-ylthio)ethanone
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A new triazole compound, C46H46N10O 2S2, has been synthesized, and the crystal structure was determined by a single crystal X-ray diffraction study. The fungicidal activity of the title compound was determined, and the results showed that it displays moderate fungicidal activity. Supplemental materials are available for this article. Go to the publisher's online edition of Phosphorus, Sulfur, and Silicon and the Related Elements to view the free supplemental file. Copyright Taylor & Francis Group, LLC.
- Liu, Xing-Hai,Tan, Cheng-Xia,Weng, Jian-Quan
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experimental part
p. 558 - 564
(2011/05/15)
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- Synthesis and biological activities of novel bis-heterocyclic pyrrodiazole derivatives
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Novel structures of bis-heterocyclic pyrrodiazole derivatives containing pyrazole were designed and synthesized. The title compounds were characterized by 1H NMR, IR, MS, and elemental analysis. Biological activities of three intermediate compounds and 25 pyrrodiazole derivatives were tested in vivo and in vitro. Some of the title compounds exhibited certain herbicidal activities against barnyardgrass and rape.
- He, Feng-Qi,Liu, Xing-Hai,Wang, Bao-Lei,Li, Zheng-Ming
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- Synthesis and biological activity of hydrazone derivatives containing pyrazole
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Twelve novel hydrazone derivatives containing pyrazole rings have been prepared by condensing substituted-benzaldehyde with 2-(3,5-dimethyl-1H-pyrazol- 1-yl)acetohydrazide under microwave irradiation. Their structures were characterised by 1H NMR, IR, MS and elemental analysis. The preliminary biological activity tests showed that some of the compounds showed moderate fungicidal activity.
- Yang, Xiao-Dong
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experimental part
p. 489 - 491
(2009/04/06)
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- Modified Procedure for the Preparation of 5-Nitro-2-furylmethylene Diacetate and Its Use in the Synthesis of Some Novel (5-Nitro-2-furyl)azomethines via 5-Nitro-2-furaldehyde
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A modified two-step procedure for the preparation of 5-nitro-2-furylmethylene diacetate (3) by nitration of 2-furaldehyde (1) or 2-furylmethylene diacetate (4) with acetyl nitrate via 2-acetoxy-5-nitro-2,5-dihydro-2-furylmethylene diacetate (2), or 1,1,5-triacetoxy-2-hydroxy-5-nitro-3-penten (5) and 1,1,5-triacetoxy-2-hydroxy-5-nitro-2,4-pentadiene (6), has been developed.Acid hydrolysis of 3 yields 5-nitro-2-furaldehyde (7) which is used in the carbonylamine condensation with various hydrazines (9-11, 14, 17, 19, 21, 24, 25, 28, 29, 32, 34, 36, 38, 39, 41 and 44-54) prepared by known methods, in order to obtain some novel potentially pharmaceutically active (5-nitro-2-furyl)azomethines.
- Vlaovic, Djordje,Milic, Bozidar Lj.,Mackenzie, Kenneth
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p. 1201 - 1218
(2007/10/02)
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- Antidiabetic activity of some 1-substituted 3,5-dimethylpyrazoles
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Several new 1-substituted 3,5-dimethylpyrazoles were prepared for testing as hypoglycemic agents. A number of these containing para-substituted 1-carbonylphenylurea and para-substituted 1-carbamoylbenzenesulfonylurea derivatives were found to possess potent hypoglycemic activity.
- Soliman,Darwish
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p. 1659 - 1663
(2007/10/02)
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