- Synthesis, characterization, and investigation of the antioxidant activity of some 1,2,4-benzothiadiazine-1,1-dioxides bearing sulfonylthioureas moieties
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A series of 1,2,4-benzothiadiazine-1,1-dioxides bearing a sulfonylthiourea moiety were synthesized, characterized, and screened for their antioxidant activity, using six antioxidant analytical assays comparatively to reference compounds, ascorbic acid and quercetin. The results indicated that several compounds demonstrated strong antioxidant activity in DPPH, ABTS, H2O2, and lipid peroxidation assays where some of them were either as active as or more active than reference compounds. However, all compounds were largely less active than references compounds in the reducing power assay. The results indicated that the thiourea moiety probably played a crucial role in the antioxidant activity of the target compounds, as a thiolate ion. The most favorable R1 groups were the hydrogen atom and methyl group, followed by phenyl and benzyl groups, whereas the most favorable R2 group was iPr, followed by the phenyl and methyl groups. The combination of benzothiadiazine ring with sulfonylthiourea moieties led to valuable new antioxidants, which could be used in the treatment or the prevention of certain diseases or in the field of cosmetics, which needs further investigations in the future.
- Harrouche, Kamel,Lahouel, Asma,Belghobsi, Mebrouk,Pirotte, Bernard,Khelili, Smail
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p. 824 - 832
(2019/11/28)
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- CHLOROTHIAZIDE, CHLOROTHIAZIDE SALTS AND PHARMACEUTICAL COMPOSITIONS THEREOF
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The present invention relates to an improved process for the preparation of Chlorothiazide and pharmaceutically acceptable salts thereof. The present invention relates to novel polymorphs of Chlorothiazide and Chlorothiazide salts, in particular Chlorothiazide sodium. The present invention further relates to pharmaceutical compositions comprising Chlorothiazide and Chlorothiazide salts, in particular Chlorothiazide sodium and process for preparation thereof.
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Page/Page column 9
(2011/11/06)
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- Synthesis and pharmacological evaluation of 1,2,4-benzothiadiazin-1,1- dioxides bearing 5- or 7-sulfonylurea moieties
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A series of substituted benzothiadiazin-1,1-dioxides bearing sulfonylurea moieties in position 5 or 7 has been synthesized. The most powerful vasodilator compound was 18a, obtained by substitution of a sulfonylurea moiety on position 7 of the diazoxide skeleton by means of a SO2 group. Interestingly, 18a and 18b were found inactive on insulin secretion at 50 μM and likely devoid of adverse effect on glycemia, suggesting a special therapeutic potential for these compounds.
- Khelili, Smail,Faury, Gilles,Nicolle, Edwige,Verdetti, Jean,Leclerc, Gerard
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p. 457 - 470
(2007/10/03)
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