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

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

doi:10.1021/jm00161a024

Cited by 116 publications

(49 citation statements)

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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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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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“…5-Phenyl-1,3,4-thiadiazole is familiar group of bioactive compounds with numerous pharmacological activities 4 . Various pharmacological activities reported for 1,3,4-thiadiazole analogues are anticancer [5][6][7] antimicrobial [8][9][10] , antitubercular 11,12 , anti-inflammatory 13 , analgesic 14 , anticonvulsant 15 , antihypertensive 16 , diuretic 17 , local anesthetic 18 and antioxidant activities 19 .Hence, it is envisaged to synthesize 1,3,4-thiadiazole analogs and screened them for antimicrobial and anticancer activities.…”

Section: Introductionmentioning

confidence: 99%

Synthesis, Antimicrobial and Anticancer Activities of 5-(4-Substituted-Phenyl)-1,3,4- Thiadiazole-2-Amines

2017

Rasayan J Chem

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A series of 5-(4-substituted phenyl)-1,3,4-thiadiazole-2-amines (4a-h) were prepared from dehydrocyclization of 4-substituted benzoyl thiosemicarbazides (3a-h) using concentrated sulphuric acid. The chemical structures of compounds were elucidated by Infra-red, NMR, Mass spectral and elemental analyses. Antibacterial activities of these compounds against Staphylococcus aureus, Bacillus substilis, Eschereria coli and Pseudomonas aeruginosa using Ciprofloxacin while antifungal activities against Aspergillus niger and Candida albicans using Fluconazole as standard drugs were performed. Minimum inhibitory concentrations and anticancer activity of potent compounds was determined. The results indicate that compounds 4(a), 4(b) and 4(c) possess significant antibacterial activity whereas compounds 4(f) and 4(g) possess significant antifungal activity among the series of synthesized thiadiazoles comparing with standard drugs. Further, the results of anticancer studies on breast cancer cell line suggested that some potent antimicrobials i.e. 4(c), 4(f) and 4(g) associated with moderate to good anticancer activity. Thus, it may be found that synthesized compounds have good antibacterial activity and moderate antifungal activity. However, these compounds could be further screened for the antibacterial activities against a battery of bacteria to achieve their broad spectrum profile and also used to screen cytotoxic effect against other cancer cell lines.

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“…[5][6][7][8][9] Thiosemicarbazones have been reported to exhibit antituberculosis activity. 10,11 In addition, 1,3-thiazoles, 1,3,4-thiadiazoles and their derivatives exhibit various biological activities such as antituberculosis, 11 antimicrobial, 12 anti-inflammatory, 13 antiviral, anticonvulsant, 14 antihypertensive, 15 local anesthetic, 16 anticancer, 17 hypoglycemic, 18 and cytotoxic activities, among others. 19 1,3,4-Thiadiazoles and related compounds are of great interest in chemistry owing to their bioactivity of certain plant growth regulating effects as well as antimicrobial activity.…”

Section: Introductionmentioning

confidence: 99%

Synthesis, spectroscopic studies and characterizations of some new bis thiosemicarbazones and their cyclization reactions

Er¹,

Ünver²,

Sancak³

et al. 2009

Arkivoc

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The reaction of trans-1,4-dichloro-2-butene 1 with selected phenols affords (E)-1,4-bis(aryloxy)-2-butenes 2a-d which are converted into bis-thiosemicarbazones 3a-h via the reactions with thiosemicarbazide and 4-methyl thiosemicarbazide, respectively. Similarly, 4-methyl-5-ethoxycarbonyl-2,3-dihydro-1,3-thiazoles 4a-h are synthesized via the reaction of bisthiosemicarbazones 3a-h with ethyl 2-chloroacetoacetate. trans-1,4-Dithiocyanato-2-butene 5 is obtained from the reaction of KSCN and trans-1,4-dichloro-2-butene 1. Furthermore, the bis-2-amino-1,3,4-thiadiazoles 6k and l are obtained from the reaction of trans-1,4-dithiocyanato-2-butene 5 with thiosemicarbazide and 4-methyl thiosemicarbazide, respectively. These compounds are characterized by elemental analyses, infrared, 1 H-, 13 C-NMR and mass spectrometry. Finally, the microbial features of all compounds are determined. Some of them exhibited microbial activities at low level, and the electronic absorption spectra of the compounds 3b,d,f and h are measured in organic solvents (MeOH, DMF, DMSO and 1,4-dioxane) with various polarities.

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

Cited by 116 publications

References 0 publications

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

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

Synthesis, Antimicrobial and Anticancer Activities of 5-(4-Substituted-Phenyl)-1,3,4- Thiadiazole-2-Amines

Synthesis, spectroscopic studies and characterizations of some new bis thiosemicarbazones and their cyclization reactions

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