- Synthesis and biological evaluations of some new oxadiazole–piperidine hybrid derivatives as antioxidant agents
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A series of some new 1,3,4-oxadiazole-2-thiol derivatives (6a-h) containing cyclic secondary amine such as piperidine ring was expeditiously synthesized by alkylation of 1,3,4-oxadiazol-2-thiol derivatives with chloroethyl piperidine hydrochloride. The 1,3,4-oxadiazole-2-thiols were effectively synthesized by cyclization reaction of acid hydrazide derivatives with carbon disulfide. The target compounds 6a-h were preliminarily screened for in vitro antioxidant activities using various in vitro antioxidant assays including 2,2′-diphenyl-1-picrylhydrazyl, nitric oxide, and hydrogen peroxide methods. The results showed that the compounds exhibited promising antioxidant property in the three methods at 50, 75, and 100 μM. Among the tested compounds, the compounds 6a and 6b having chloro substituent in the benzene ring displayed greater radical scavenging activity.
- Al-Ghorbani, Mohammed M. Abdullah
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p. 379 - 384
(2018/09/29)
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- A new conjugated polymer-based combination probe for ATP detection using a multisite-binding and FRET strategy
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A new conjugated polymer-based ratiometric combination probe was constructed for adenosine triphosphate detection by taking advantage of a multisite-binding and fluorescence resonance energy transfer strategy. The method is rapid and highly selective, whi
- Zhao, Qi,Zhang, Ziqi,Tang, Yanli
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p. 9414 - 9417
(2017/08/29)
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- Regioselective Alkoxycarbonylation of Allyl Phenyl Ethers Catalyzed by Pd/dppb under Syngas Conditions
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A simple and regioselective synthesis of phenoxy esters and phenylthio esters is reported. The products are obtained by selective alkoxycarbonylation catalyzed by Pd2(dba)3, 1,4-bis(diphenylphisphino)butane (dppb), and syngas (CO/H2) in chloroform/alcohol. This methodology affords bifunctional products in good yield with excellent n-selectivity and without the need to use additives.
- Amézquita-Valencia, Manuel,Alper, Howard
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p. 3860 - 3867
(2016/05/24)
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- Synthesis of oxadiazole-morpholine derivatives and manifestation of the repressed CD31 Microvessel Density (MVD) as tumoral angiogenic parameters in Dalton's Lymphoma
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A series of oxadiazole derivatives possessing morpholine 6a-l were synthesized by nucleophilic substitution reaction of key intermediates [1,3,4]-oxadiazole-2-thiol derivatives 5a-l with 4-(2-chloroethyl) morpholine. Compounds 6a-l were evaluated for their in vitro and in vivo antitumor potential in Dalton's Lymphoma Ascites (DLA) tumor cells. Among 6a-l series, compound 6a with concentration ~8.5 μM have shown extensive cytotoxicity in vitro and 85% reduction in tumor volume in vivo, attributing an excellent anti-proliferative capability towards the cancer cells. Compound 6a has extensively inhibited the Microvessel Density (MVD) or tumoral neovasculature which was evident from the CD31 immuno staining and peritoneal H&E staining. The major reason for the antiproliferative activity of compound 6a was due to the repression of tumor vasculature.
- Al-Ghorbani, Mohammed,Vigneshwaran,Ranganatha, V. Lakshmi,Prabhakar,Khanum, Shaukath Ara
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p. 136 - 146
(2015/06/02)
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- Conformationally Restricted Tetrahydro-1-benzoxepin Analogs of Hallucinogenic Phenethylamines
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Tetrahydro-1-benzoxepin analogs of prototypical 4-substituted-2,5-dimethoxyphenylisopropylamines were prepared as agents having restricted conformational mobility in the 2-alkoxy group and alkylamine sidechain. The derivatives were evaluated for their abi
- Monte, Aaron P.,Marona-Lewicka, Danuta,Cozzi, Nicholas V.,Nelson, David L.,Nichols, David E.
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p. 651 - 663
(2007/10/03)
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