Synthesis of new 2,5-Disubstituted-1,3,4-thiadiazoles and preliminary evaluation of anticonvulsant and antimicrobial activities

Dogan, H. N.; Duran, Arzu; Rollas, Sevım; Şener, Göksel; Uysal, Meral Keyer; Gülen, Dumrul

doi:10.1016/s0968-0896(02)00143-8

Cited by 247 publications

(123 citation statements)

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“…On the other hand, thiadiazole moiety was also found to possess significant anticonvulsant activity (6,7). In continuation of our previous research on benzothiazoles, we report here the synthesis and anticonvulsant activity of several N-(5-chloro-6-substituted-benzothiazol-2-yl)-N'-(substituted phenyl)- [1,3,4]thiadiazole-2,5-diamines.…”

mentioning

confidence: 69%

Synthesis and preliminary screening of benzothiazol-2-yl thiadiazole derivatives for anticonvulsant activity

Siddiqui¹,

Rana²,

Khan³

et al. 2009

Acta Pharmaceutica

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The term epilepsy is a collective term that includes disorders of the brain function characterized by the periodic and unpredictable occurrence of seizures. Epilepsies are common and frequently devastating and affect around 1-2 % of the world population (1).Current drug therapy for epilepsy suffers from a number of disadvantages, including the fact that the convulsions of approximately 25 % of epileptics are inadequately controlled by medication (2). In recent years, the field of antiepileptic drug development has become quite dynamic, affording many promising research opportunities.In our previous study (3-5), we designed aryl-substituted semicarbazones with benzothiazole moiety, in which we made some modifications in the structure of semicarbazones. The lipophilic aryl ring was replaced with a versatile heterocyclic molecule ben- Various,4]thiadiazole-2,5-diamines (5a-t) were designed and synthesized starting from substituted acetophenones. Structures of all the compounds were confirmed on the basis of spectral and elemental analyses. All the newly synthesized compounds were screened for their anticonvulsant activity and were compared with the standard drug phenytoin sodium. Interestingly, all the compounds showed protections against seizures in the range 50-100 % indicative of the promising nature of the compounds against seizure spread. Compounds 5b and 5c showed complete protection against MES induced seizures.

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confidence: 69%

Synthesis and preliminary screening of benzothiazol-2-yl thiadiazole derivatives for anticonvulsant activity

Siddiqui¹,

Rana²,

Khan³

et al. 2009

Acta Pharmaceutica

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“…1,3,4-Thiadiazoles have been screened for their antibacterial and antifungal activities [1][2][3][4], anti-inflammatory [5], anti-tuberculosis [6] and anticancer [7] activity. Also, pyrazoles and annelated pyrazoles have long been known to exhibit diverse biological activities [8,9,[10][11][12][13].…”

Section: Introductionmentioning

confidence: 99%

Reactions with hydrazonoyl halides 65: Synthesis of some new 1,3,4-thiadiazoles and triazolino[4,3-a]pyrimidines containing pyrazole moiety

2011

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“…Some compounds bearing a 1,2,4-triazole and 1,3,4-thiadiazole structure have been reported to have antimicrobial activity [4][5][6][7][8]. In addition, many compounds carrying a phthalazinone ring have been reported to have diverse biological activities such as antimicrobial [9,10], antihypertensive [11], analgesic and anti-inflammatory activities [12].…”

Section: Introductionmentioning

confidence: 99%

Synthesis and antimicrobial activity of new 1,2,4-triazole and 1,3,4-thiadiazole derivatives

Önkol

Dogruer

Uzun

et al. 2008

Journal of Enzyme Inhibition and Medicinal Chemistry

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In this study, new 3-[(1(2H)-phthalazinone-2-yl(methyl/ethyl]-4-aryl-1,2,4-triazole-5-thione and 2-[[1(2H)-phthalazinone-2-yl]methyl/ethyl]-5-arylamino-1,3,4-thiadiazole derivatives were synthesized. Antimicrobial properties of the title compounds were investigated against two Gram (þ) bacteria (S. aureus, B. subtilis), two Gram (2 ) bacteria (P. aeruginosa, E. coli) and two yeast-like fungi (C. albicans and C. parapsilosis) using the broth microdilution method. Generally the compounds were found to be active against B. subtilis and the fungi. Derivatives carrying a 1,3,4-thiadiazole ring generally showed higher antimicrobial activity against B. subtilis and the fungi when compared to other synthesized compounds.

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Synthesis of new 2,5-Disubstituted-1,3,4-thiadiazoles and preliminary evaluation of anticonvulsant and antimicrobial activities

Cited by 247 publications

References 5 publications

Synthesis and preliminary screening of benzothiazol-2-yl thiadiazole derivatives for anticonvulsant activity

Synthesis and preliminary screening of benzothiazol-2-yl thiadiazole derivatives for anticonvulsant activity

Reactions with hydrazonoyl halides 65: Synthesis of some new 1,3,4-thiadiazoles and triazolino[4,3-a]pyrimidines containing pyrazole moiety

Synthesis and antimicrobial activity of new 1,2,4-triazole and 1,3,4-thiadiazole derivatives

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