28036-91-1Relevant academic research and scientific papers
Some Novel Mannich Bases of 5-(3,4-Dichlorophenyl)-1,3,4-oxadiazole-2(3H)-one and Their Anti-Inflammatory Activity
Koksal, Meric,Ozkan-Dagliyan, Irem,Ozyazici, Tugce,Kadioglu, Beril,Sipahi, Hande,Bozkurt, Ayhan,Bilge, Suleyman S.
, (2017)
Non-steroidal anti-inflammatory drugs (NSAIDs), which are widely used for the treatment of rheumatic arthritis, pain, and many different types of inflammatory disorders, cause serious gastrointestinal (GI) side effects. The free carboxylic acid group exis
Synthesis, spectral characterization, and biological studies of 3,5-disubstituted-1,3,4-oxadiazole-2(3H)-thione derivatives
?zyazici, Tug?e,Sahin, Fikrettin,K?ksal, Meri?
, p. 749 - 760 (2021/07/26)
The reaction of 3,4-dichlorophenyl-1,3,4-oxadiazole-2(3H)-thione with piperidine derivatives via Mannich reaction was used to generate eleven novel compounds in moderate to good yields. Synthesized molecules were characterized according to their structure
Discovery of highly potent tubulin polymerization inhibitors: Design, synthesis, and structure-activity relationships of novel 2,7-diaryl-[1,2,4]triazolo[1,5-a]pyrimidines
Huo, Xian-Sen,Jian, Xie-Er,Ou-Yang, Jie,Chen, Lin,Yang, Fang,Lv, Dong-Xin,You, Wen-Wei,Rao, Jin-Jun,Zhao, Pei-Liang
, (2021/05/10)
By removing 5-methyl and 6-acetyl groups in our previously reported compound 3, we designed a series of novel 2,7-diaryl-[1,2,4]triazolo[1,5-a]pyrimidine derivatives as potential tubulin polymerization inhibitors. Among them, compound 5e displayed low nanomolar antiproliferative efficacy on HeLa cells which was 166-fold higher than the lead analogue 3. Interestingly, 5e displayed significant selectivity in inhibiting cancer cells over HEK-293 (normal human embryonic kidney cells). In addition, 5e dose-dependently arrested HeLa in G2/M phase through the alterations of the expression levels of p-cdc2 and cyclin B1, and caused HeLa cells apoptosis by regulation of expressions of cleaved PARP. Further evidence demonstrated that 5e effectively inhibited tubulin polymerization and was 3-fold more powerful than positive control CA-4. Moreover, molecular docking analysis indicated that 5e overlapped well with CA-4 in the colchicine-binding site. These studies demonstrated that 2,7-diaryl-[1,2,4]triazolo[1,5-a]pyrimidine skeleton might be used as the leading unit to develop novel tubulin polymerization inhibitors as potential anticancer agents.
Synthesis and antituberculosis activity of new acylthiosemicarbazides designed by structural modification
Martínez, Roberto,Espitia-Pinzón, Clara I.,Silva Miranda, Mayra,Chávez-Santos, Rosa María,Pretelin-Castillo, Gustavo,Ramos-Orea, Aldahir,Hernández-Báez, ángela M.,Cotlame-Pérez, Sandra,Pedraza-Rodríguez, Rogelio
, p. 350 - 355 (2019/12/03)
Acylthiosemicarbazides 8a–n were designed by structural modification of lead Compound 7. The syntheses of 8a–n involve a five-step procedure starting from carboxylic acids. Compounds 8a–n were tested against three Mycobacterium tuberculosis strains to measure their inhibitory antituberculosis activities. These activities could be explained according to the presence or absence of the chlorine substituent in the aromatic ring of the amide joined to the thiosemicarbazide core. Thiosemicarbazide derivative 8n is a candidate for the development of novel antitubercular agents. Ongoing studies are focused on exploring the mechanism by which these compounds inhibit M. tuberculosis cell growth.
NOVEL FUNCTIONALIZED PURINE-2,6-DIONES AND THEIR USE IN MEDICINE
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Page/Page column 51; 52; 56, (2019/02/13)
There is provided compounds of formula (I), or pharmaceutically-acceptable salts thereof, wherein R1 to R4 and X1 to X5 have meanings provided in the description, which compounds are useful in the treatment of c
Design, synthesis, insecticidal activity and 3D-QSR study for novel trifluoromethyl pyridine derivatives containing an 1,3,4-oxadiazole moiety
Xu,Wang,Luo,Yu,Guo,Fu,Zhao,Wu
, p. 6306 - 6314 (2018/02/19)
A series of trifluoromethyl pyridine derivatives containing 1,3,4-oxadiazole moiety was designed, synthesized and bio-assayed for their insecticidal activity. The result of bio-assays indicated the synthesized compounds exhibited good insecticidal activity against Mythimna separata and Plutella xylostella, most of the title compounds show 100% insecticidal activity at 500 mg L-1 and >80% activity at 250 mg L-1 against the two pests. Compounds E18 and E27 showed LC50 values of 38.5 and 30.8 mg L-1 against Mythimna separata, respectively, which were close to that of avermectin (29.6 mg L-1); compounds E5, E6, E9, E10, E15, E25, E26, and E27 showed 100% activity at 250 mg L-1, which were better than chlorpyrifos (87%). CoMFA and CoMSIA models with good predictability were proposed, which revealed the electron-withdrawing groups with an appropriate bulk at 2- and 4-positions of benzene ring could enhance insecticidal activity.
SUBSTITUTED PYRAZOLE COMPOUNDS AND METHODS OF USING THEM FOR TREATMENT OF HYPERPROLIFERATIVE DISEASES
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Paragraph 208, (2018/06/21)
Disclosed are compounds useful, for example, in methods of treating hyperproliferative disorders such as cancer, methods of arresting the cell cycle in cancer cells, methods of inhibiting glutathione synthesis in cancer cells, and associated compounds for
Efficient three-component synthesis of N-alkyl-3, 6-diaryl-[1, 2, 4]triazolo[4, 3-b][1, 2, 4]triazin-7-amines under solvent-free condition
Azimi, Sara,Soheilizad, Mehdi,Zonouzi, Afsaneh,Mahdavi, Mohammad
, p. 293 - 300 (2017/12/06)
A simple, efficient and environment-friendly approach is described for the synthesis of N-alkyl-3, 6-diaryl-[1, 2, 4]triazolo[4, 3-b][1, 2, 4]triazin-7-amines based on three-component reaction between 5-aryl-4H-1, 2, 4-triazole-3, 4-diamine, isocyanide and aldeyhde under solvent-free condition. The products are obtained in moderate to good yields and are in a state of high purity.
Azabicyalo derivative as well as preparation and application thereof
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Paragraph 0202; 0203; 0205, (2016/10/07)
The invention relates to an azabicyalo derivative as well as preparation and application thereof, and particularly discloses a compound with a structure shown in to the formula (A) or salt thereof acceptable in agricultural pharmacology. The compound in the formula (A) is described in the description in detail, and has an excellent killing effect on nematode.
Synthesis of new 2,5-di-substituted 1,3,4-oxadiazoles bearing 2,6-di-tert-butylphenol moieties and evaluation of their antioxidant activity
Shakir, Raied M.,Ariffin, Azhar,Abdulla, Mahmood Ameen
, p. 3436 - 3439 (2014/04/17)
Eleven new 2,6-di-tert-butyl-4-(5-Aryl-1,3,4-oxadiazol-2-yl)phenols 5a-k were synthesized by reacting aryl hydrazides with 3,5-di-tert butyl 4-hydroxybenzoic acid in the presence of phosphorus oxychloride. The resulting compounds were characterized based on their IR, 1H-NMR, 13C-NMR, and HRMS data. 2,2-Diphenyl-1-picrylhydrazide (DPPH) and ferric reducing antioxidant power (FRAP) assays were used to test the antioxidant properties of the compounds. Compounds 5f and 5j exhibited significant free-radical scavenging ability in both assays.
