ChemInform Abstract: Thiadiazole Derivatives as Potential Anticonvulsant Agents.

Mullick, Pooja; Khan, Shahrukh Rafi; Verma, Surajpal; Alam, Ozair

doi:10.1002/chin.201129129

Cited by 1 publication

(1 citation statement)

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“…Thus, sulphonamides reported mainly as antibacterial agents [7,8], are also functioning as insu lin releasing stimulants [9] and anti inflammatory [10] and cytotoxic [11] agents. 1,2,4 Triazines documented as anti HIV, anti H5N1 virus agents [12][13][14] are also antiproleferative [15,16] agents acting on VEGFR tyrosine kinases [17] as well as anti tuberculosis [18], anti anxiety, anti inflammatory agents [19,20], potent antidepression and antianxiety agents [21], and anti breast cancer candidates [22]. Finally, thiophenes are well known as inhibitors of BACE1 preventing β amyloid plaques formation in Alzheimer's disease [23,24] and Plasmo dium falciparum differentiation [25], anti HIV [26], antiproleferative [27,28], anti inflammatory [29][30][31], antibacterial [32], and antiprotozoal [33] agents.…”

Section: Introductionmentioning

confidence: 99%

Synthesis, reactions, and biological activity of some triazine derivatives containing sulfa drug moieties

et al. 2015

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Thienyl-triazine-sulphonamide conjugates were prepared from their precursor amines using triethyl orthoformate or ethyl chloroformate as cross coupling reagents. The progress of these reactions was investigated by spectral (IR, NMR, MS) and microanalytical techniques. The synthesized compounds were in vitro screened for antibacterial, antifungal, antioxidant, and anticancer activity. 4-[({[3-Mercapto-5-oxo-6-[2-(2-thienyl)yinyl]-1,2,4-triazin- 4(5H)-yl]imino}methyl)amino]-benzenesulfonamide turned out to be a powerful antibacterial agent, while all the compounds prepared were inactive against fungal species tested. 4-{[({8-Cyano-4-oxo-3-[2-(2-thienyl)vinyl- 4H,8H-[1,2,4]triazino[3,4-b][1,3,4]thiadiazin-7-yl}amino)(ethoxy)methyl]amino}benzenesulfonamide displayed in vitro promising cytotoxicity against Ehrlich ascites carcinoma cell line with concurrent attenuation of malonodinitrile and it was unique among other compounds being unable to increase glutathione S-transferase and reduced glutathione S-transferase activities. This compound exhibited also good antioxidant properties that together with its cytotoxicity nominated it for further investigation in cancer research.

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