Synthesis and hypoglycemic activity of sulfonamido-1,3,4-thiadiazoles

Recently a series of 2-amino-5-sulfanyl-1,3,4-thiadiazole derivatives bearing different substituents were synthesized and screened pharmacologically in order to evaluate their central nervous system activity. The purpose of this study was to evaluate the effects of the title compounds on CNS activity by varying the substituents in the thiadiazole moiety. It was found that some of these compounds possess marked antidepressant and anxiolytic properties comparable in efficiency to the reference drugs Imipramine and Diazepam. The most potent compound 3k was further investigated to complete its pharmacological profile with respect to undesired side effects. Behavioral results showed that 3k is a very promising compound, characterized by a mixed antidepressant-anxiolytic activity accompanied by a therapeutic dose range that is essentially 2 orders of magnitude less than that at which side effects such as sedation and amnesia are evident.

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“…TLC was performed on silica gel plates. Compounds 3a-d,f,g,i,k,l,m and 5a,g,l,n [6][7][8][9][10][11][12] are known.…”

Section: Methodsmentioning

confidence: 99%

Synthesis of 2-Amino-5-sulfanyl-1,3,4-thiadiazole Derivatives and Evaluation of Their Antidepressant and Anxiolytic Activity

Clerici

Pocar²,

Guido³

et al. 2001

J. Med. Chem.

222

124

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“…They have been reported to selectively inhibit several therapeutic receptors and enzymes, extending their applications in modern drug design. Further, there are reports in the literature about the antidiabetic activity of the derivatives containing thiadiazole ring system [7].…”

Section: Introductionmentioning

confidence: 99%

Synthesis of novel 5-{[2-(4-fluorobenzyl)-6-arylimidazo[2,1-b] [1,3,4]thiadiazol-5-yl]methylene}thiazolidine-2,4-diones as potent Antidiabetic agents

Badiger¹

2015

IJSEA

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“…Microbial infections cause pain and inflammation. In the current study, we have focused on thiadiazoles due to its versatile biological profile such as hypoglycemic (Avetisyan et al, 1981), anticancer (Parkanyi et al 1992), anti-inflammatory (Boschelli et al, 1993;Labanauskas et al, 2001;Schenone et al, 2001), anti-asthmatic (Bhattacharya et al, 2005), antihypertensive (Vio et al, 1989), antidepressant (Clerici et al, 2001), anxiolytic (Clerici et al, 2001), fungicidal (Chen and Hen, 2000; and antituberculosis (Foroumadi et al, 2001). On the other hand, esters of 1,1-cyclopropane dicarboxylic acid were found to possess important insecticidal activity (Ronald and Leland 1998).…”

Section: Introductionmentioning

confidence: 99%

Synthesis and Pharmacological Evaluation: Antimicrobial, Anti-Inflammatory, Analgesic, Ulcerogenic Properties of Several Bis-Heterocyclic Derivatives

Kumar¹,

Panwar²

2015

Indonesian J. Pharm.

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In Medicinal chemistry, heterocyclic derivatives contributed the largest classical division of organic chemistry. Thiadiazole compounds have been known for many biological activities such as hypoglycemic, anticancer, anti-inflammatory, anti-asthmatic, antihypertensive etc. On this research, several 1,1-bis [2-{2-(5-(arylidene)imino-1,3,4-thiadiazol-2-yl) methyl amino}-1,3,4-thiadiazo-5-yl] cyclopropane 5(a-h) have been synthesized from cyclopropane dicarboxylic acid comprising thiadiazole moieties. All the synthesized compounds have been characterized by elemental (C,H,N) and spectral (I.R., 1 H-NMR, Mass) analysis. Furthermore, all synthesized compounds were screened for their antifungal, antimicrobial, anti-inflammatory, analgesic, ulcerogenic and toxic activities. The Compound 5f, 3-chlorophenyl substituted was found the most potent in antimicrobial spectrum against all the used microbes. On the other hand, compound 5g, 4-hydroxy-3-methoxy phenyl substituted was found the most potent in antiinflammatory, analgesic, and ulcerogenic activities which further evaluated for lesser toxicity test.

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Synthesis and hypoglycemic activity of sulfonamido-1,3,4-thiadiazoles

Cited by 7 publications

References 2 publications

Synthesis of 2-Amino-5-sulfanyl-1,3,4-thiadiazole Derivatives and Evaluation of Their Antidepressant and Anxiolytic Activity

Synthesis of 2-Amino-5-sulfanyl-1,3,4-thiadiazole Derivatives and Evaluation of Their Antidepressant and Anxiolytic Activity

Synthesis of novel 5-{[2-(4-fluorobenzyl)-6-arylimidazo[2,1-b] [1,3,4]thiadiazol-5-yl]methylene}thiazolidine-2,4-diones as potent Antidiabetic agents

Synthesis and Pharmacological Evaluation: Antimicrobial, Anti-Inflammatory, Analgesic, Ulcerogenic Properties of Several Bis-Heterocyclic Derivatives

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