Substituted 1,3,4-thiadiazoles with anticonvulsant activity. 4. Amidines

Chapleo, Christopher B.; Myers, Peter L.; Smith, A. C. B.; Stillings, Michael R.; Tulloch, I.F.; Walter, D.S.

doi:10.1021/jm00396a004

Cited by 88 publications

(33 citation statements)

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“…Many substituted five-membered heterocycle pyrazoles, 1,2,4-triazoles and 1,3,4-thiadiazoles are known to posses a wide range of pharmacological activities, such as antibacterial [1][2][3], anticonvulsant [4][5][6], and antitubercular [7][8] activities. Moreover, the pyrazole nucleus ranks among those molecular structures related to potent analgesic activity [9][10].…”

Section: Introductionmentioning

confidence: 99%

Synthesis of Some Novel Azo Derivatives of 3,5‐Dimethly‐1‐(2‐hydroxyethyl)pyrazole as Potent Analgesic Agents

Oruç

Koçyığıt‐Kaymakcioğlu

Oral

et al. 2006

Archiv der Pharmazie

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A series of 1-(2-hydroxyethyl)-3,5-dimethylpyrazolylazo derivatives, incorporating thiosemicarbazide 2a-c, 1,3,4-thiadiazole 3a-c, and 1,2,4-triazole-3-thione 4a-c were synthesized. The structure of these novel synthesized compounds 2a-c, 3a-c, and 4a-c was confirmed by spectral analysis. All these compounds were screened for their analgesic activity. Hot-plate and tail-immersion tests were used for the determination of the analgesic activity. Morphine, an analgesic through both spinal and supraspinal pathways, was used as a standard test drug. All compounds were administered at a dose of 100 mg/kg i.p. Among the compounds, 2-(butylamino)-5-[((1-(2-hydroxyethyl)-3,5-dimethylpyrazole-4-yl)azo)phenyl]-1,3,4-thiadiazole 3a and 4-[((1-(2-hydroxyethyl)-3,5-dimethylpyrazole-4-yl)azo)phenyl]-4-(2-phenethyl)-2,4-dihydro-3H-1,2,4-triazole-3-thione 4c showed analgesic effects in both tests. Especially 4c exerted strong analgesia starting at 30 min after injection.

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Section: Introductionmentioning

confidence: 99%

Synthesis of Some Novel Azo Derivatives of 3,5‐Dimethly‐1‐(2‐hydroxyethyl)pyrazole as Potent Analgesic Agents

Oruç

Koçyığıt‐Kaymakcioğlu

Oral

et al. 2006

Archiv der Pharmazie

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“…During recent years there has been intense investigation of different classes of thiadiazole compounds, many of which known to possess interesting biological properties such as antimicrobial, antituberculosis, anti-inflammatory, anticonvulsants, antihypertensive [71][72][73][74][75][76] , antioxidant, anticancer and antifungal [77][78][79][80][81] activity. These compounds also exhibited significant antiinflammatory activity, which is comparable to that of celecoxib.…”

Section: Recent Advancement In the Therapeutic Potential Of Thiadiazomentioning

confidence: 99%

Chemistry, synthesis and progress report on biological activities of thiadiazole compounds - a review

Asif¹

2016

Mediterr.J.Chem.,

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Thiadiazoles are an important class of heterocyclic compounds that exhibit diverse applications in organic synthesis, pharmaceutical and biological applications. They are also useful as oxidation inhibitors, cyanine dyes, metal chelating agents, anti-corrosion agents. Researchers across the globe are working on this moiety due to their broad spectrum of applications of thiadiazole chemistry. This article provides information about developments, exploration, synthetic strategies, techniques for the synthesis of thiadiazoles and their diverse biological activities, structure-activity relationship of the compounds and physical properties. This article is an important tool for organic and medicinal chemists to develop newer thiadiazole compounds that could be better agents in terms of efficacy and safety.

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“…Furthermore, thiadiazoles possess antifungal, 6 antituberculosis, [7][8][9] anticancer, 10,11 antimicrobial, [12][13][14][15] anti-inflammatory, [16][17][18] antihypertensive, 19,20 local anesthetic, 21 anticonvulsant, [22][23][24] and antitrypanosomal 25 activities.…”

Section: Introductionmentioning

confidence: 99%

Synthesis and antituberculosis activity of 2-(aryl/alkylamino)-5-(4-aminophenyl)-1,3,4-thiadiazoles and their Schiff bases

Solak¹,

Rollas²

2006

Arkivoc

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A series of new Schiff bases were synthesized through the condensation reaction of 1,3,4-thiadiazoles containing a aromatic primary amine and 3-hydroxybenzaldehyde, salicylaldehyde, 5-nitrofurfuraldehyde or 3-nitrobenzaldehyde. The synthesized compounds screened for antituberculosis activity against Mycobacterium tuberculosis H 37 Rv using BACTEC 460 radiometric system. Among the tested compounds, 2-phenylamino-5-[4-(2-hydroxybenzylideneamino)phenyl]-1,3,4-thiadiazol (5a) showed the highest inhibitory activity (51%). The activities of the synthesized Schiff bases were compared with those of the starting 2-(aryl/alkylamino)-5-(4-aminophenyl)-1,3,4-thiadiazoles (4a-e). Some Schiff bases showed higher growth inhibition than the starting amines.

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Substituted 1,3,4-thiadiazoles with anticonvulsant activity. 4. Amidines

Cited by 88 publications

References 1 publication

Synthesis of Some Novel Azo Derivatives of 3,5‐Dimethly‐1‐(2‐hydroxyethyl)pyrazole as Potent Analgesic Agents

Synthesis of Some Novel Azo Derivatives of 3,5‐Dimethly‐1‐(2‐hydroxyethyl)pyrazole as Potent Analgesic Agents

Chemistry, synthesis and progress report on biological activities of thiadiazole compounds - a review

Synthesis and antituberculosis activity of 2-(aryl/alkylamino)-5-(4-aminophenyl)-1,3,4-thiadiazoles and their Schiff bases

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