for synthesis of 1, 3, 4-Oxadiazole derivatives and ..
Synthesis and Pharmacological Evaluation of Some Novel 1,3,4-Oxadiazole Analogues as Anticonvulsant Agent.
Design, synthesis and biological evaluation of 1,3,4-oxadiazole.
N.C. Desai , Amit M. Dodiya, Synthesis, characterization and in vitro antimicrobial screening of quinoline nucleus containing 1,3,4-oxadiazole and 2- zetidinone derivatives, Journal of Saudi Chemical Society (2014) 18, 425431.
Rajesh A. Rane , Pavankumar Bangalore , Sheetal D. Borhade, Preeti K. Khandare, Synthesis and evaluation of novel 4-nitropyrrole-based 1,3,4- oxadiazole derivatives as antimicrobial and anti-tubercular agents, European Journal of Medicinal Chemistry 70 (2013) 49-58.
Singh P: Design, synthesis and biological evaluation of 1,3,4 ..
Navarrete-Va´zquez G et al.55 reported the synthesis of 4-(5-substituted-1,3,4-oxadiazol-2-yl)pyridine derivatives and evaluated for their in vitro antimycobacterial activity. Some compounds showed an interesting activity against Mycobacterium tuberculosis H37Rv and five clinical isolates (drug-sensitive and -resistant strains) [Figure 29].
Fliur Macaev et al 54 reported that a series of 5-aryl-2-thio-1,3,4-oxadiazole derivatives were synthesized and screened for their anti-mycobacterial activities against Mycobacterium tuberculosis H37Rv.
Maria Ispikoudi , Michalis Amvrazis , Christos Kontogiorgis, Alexandros E. Koumbis , Konstantinos E. Litinas , Dimitra Hadjipavlou-Litina , Konstantina C. Fylaktakidou, Convenient synthesis and biological profile of 5-amino-substituted 1,2,4-oxadiazole derivatives, European Journal of Medicinal Chemistry 45 (2010) 5635-5645.
Harish Kumar, Sadique A. Javed, Suroor A. Khan, Mohammad Amir, 1,3,4-Oxadiazole/thiadiazole and 1,2,4-triazole derivatives of biphenyl-4-yloxy acetic acid: Synthesis and preliminary evaluation of biological properties, European Journal of Medicinal Chemistry 43 (2008) 2688-2698.
The system can be applied to the screening and design of new ..
Cursos de Extensão na área de Design. Inscreva-se!
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Design, Synthesis an ..
Glycogen Synthase Kinase-3 (GSK-3)-Targeted Therapy …
Docking simulation was performed to position the title compounds into the telomerase structure active site to determine the probable binding model. Antiproliferative and enzyme assay results suggested that these compounds were potential antitumor agents. From the results, it could be concluded that some quinoline derivatives are good candidates for antitumor agents screening and research. The template quinoline with 1,3,4-oxadiazole moiety was suitable to reconstruct and design for development of more potential therapeutic drugs against cancer [Figure 8].
Molecules | April 2014 - Browse Articles
Fanny PB et al 36 reported the synthesis and biological evaluation of 5-nitro-2-furfuriliden derivatives and also evaluated the anti-Trypanosoma cruzi activity of 5-nitro-2-furfuriliden derivatives. All the synthesized active compounds were evaluated for the cytotoxicity assay of on J774 macrophages cell line and FN1 human fibroblast cells. The findings indicated that the anti-T. cruzi activity of the investigated compounds regarding the two series is strongly influenced by the physicochemical properties of the substituent group attached to the benzene ring and the cytotoxicity assay shown that some compounds have presented interesting selectivity indices [Figure 10].
Molecules, Volume 19, Issue 4 (April 2014), Pages 3851-5458
Shuai Z et al 37 have designed and synthesized a series of new 1,3,4-oxadiazole derivatives containing benzotriazole moiety as potential focal adhesion kinase (FAK) inhibitors. All the synthesized compounds were evaluated for their anticancer activity against MCF-7 (human breast cancer) and HT29 (human colorectal cancer) cell lines. Some compounds showed the potent inhibitory activity against MCF-7 and HT29 cell lines with IC50 values of 5.68 lg/ml and 10.21 lg/ml, respectively. All the compounds were also assayed for FAK inhibitory activity using the TRAP–PCR–ELISA assay and results showed that some compounds found to have potent FAK inhibitory activity with IC50 values of 1.2 ± 0.3 lM [Figure 11].
Gastrointestinal Toxicity of Nonsteroidal …
Juan S et al 34 have synthesized a series of quinoline derivatives and also evaluated their biological activities as potential telomerase inhibitors. Bioassay tests demonstrated that most of the compounds exhibited substantial broad-spectrum of antitumor activity against the three cancer cell lines (HepG2, SGC-7901 and MCF-7). Moreover, all the title compounds were assayed for telomerase inhibition using the TRAP-PCR-ELISA assay. Some compounds from the series displayed the most potent anticancer activities, which were comparable to the positive control.
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