ChemInform Abstract: Synthesis and Evaluation of Some Novel 1,3,4‐Thiadiazoles for Antidiabetic Activity.

Pattan, Shashikant R; Kittur, B. S.; Sastry, B. S.; Jadav, S G; Thakur, Dinesh K.; Madamwar, S. A.; Shinde, Hemlata V

doi:10.1002/chin.201130132

Cited by 10 publications

(11 citation statements)

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“…Figure 1 shows scheme 1 [11] of synthesis for compound TD1 to TD6. Figure 2 shows scheme 2 for synthesis of compound TD7 [12].…”

Section: Experimental Methodsmentioning

confidence: 99%

“…In vivo study was carried out on alloxan induced diabetes rat model for all the synthesized molecules using glibenclamide, a second generation sulphonylurea as standard since it was used as a reference standard compound in the study of reference analogous compounds [11,12]. Molecular docking studies were performed by using Glide v5.6 (Schrodinger, LLC) [13].…”

Section: Chemistrymentioning

confidence: 99%

“…These binding residues were used as reference guide. Several thiadiazole compounds have been reported for their antidiabetic effect by acting as agonist at PPAR gamma [11,12]. Docking was performed selectively on reported thiadiazole analogues Tables 1 and 2 This study helped in understanding possible orientations and conformation of thiadiazole compounds and their resulting position and binding interaction in the pocket.…”

Section: Chemistrymentioning

confidence: 99%

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Design and Synthesis of Thiadiazole Derivatives as Antidiabetic Agents

Datar¹

2014

Med chem

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Thiadiazole compounds have versatile activities such as anti-microbial, anti-inflammatory, anticancer, etc. Present study involves design of thiadiazole compounds as antidiabetic agent using docking studies. The designed molecules were synthesized and subjected to antidiabetic activity by in vitro and in vivo method. Compound TD7 was found to show potent antidiabetic activity in alloxan induced diabetes rat model. Molecular docking revealed that synthesized derivatives and target proteins were actively involved in binding and had significant correlation with biological activity.

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“…Figure 1 shows scheme 1 [11] of synthesis for compound TD1 to TD6. Figure 2 shows scheme 2 for synthesis of compound TD7 [12].…”

Section: Experimental Methodsmentioning

confidence: 99%

Section: Chemistrymentioning

confidence: 99%

Section: Chemistrymentioning

confidence: 99%

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Design and Synthesis of Thiadiazole Derivatives as Antidiabetic Agents

Datar¹

2014

Med chem

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“…Thionation of N,N'-acylhydrazines with the use of a fluorous Lawesson's reagent leads to 1,3,4-thiadiazoles in high yields. The isolation of the final products is achieved in most cases by a simple filtration 48 .…”

Section: Scheme 18mentioning

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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“…2010; Cressier et al, 2009), antibacterial (Foroumadi et al, 2007;Dubey et al, 2012), antidepressant (Yusuf et al, 2008;Clerici and Pocar, 2001), antidiabetic (Pattn et al, 2011;Lee et al, 2010), antifungal (Liu et al, 2008;Xu et al, 2013), anticonvulsant (Siddiqui et al, 2013;Sharma et al, 2014), and antiinflammatory effects (Dekhane et al, 2011;Amir et al, 2007). In particular, a few of differently substituted 1,3,4-thiadiazoles have been found to exhibited anticancer activities (Hamama et al, 2013;Hosseinzadeh et al, 2013;Zhao et al, 2013;Kumar et al, 2010Kumar et al, , 2011.…”

Section: Introductionmentioning

confidence: 99%

Synthesis and in vitro antiproliferative activity of novel benzisoselenazolone derivatives

et al. 2014

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A series of novel benzisoselenazolone derivatives bearing 1,3,4-thiadiazole moiety were designed, synthesized and evaluated for their in vitro antiproliferative activities against human cancer cell lines SMMC-7721, MCF-7, A549, and normal cell lines L929 by CCK-8 assay.The bioassay results demonstrated that most of the tested compounds showed potent antitumor activities, and some compounds exhibited better effects than positive control ebselen and ethaselen against various cancer cell lines. Among these compounds, compound 7l showed significant antiproliferative activity against SMMC-7721 cells, with IC 50 values of 2.18 lM. Compound 7j exhibited the best inhibitory effect against MCF-7 cells, with IC 50 values of 2.89 lM. Compounds 7e and 7i displayed highly effective antitumor activities against A549 cells, with IC 50 values of 2.33 and 2.33 lM, respectively. Furthermore, most of the tested compounds showed weak cytotoxic effect against the normal cell lines L929. The pharmacological results suggest that the substituents of benzoylmethylthio-moiety at position-2 on 1,3,4-thiadiazole are vital for modulating antiproliferative activities against various tumor cell lines.

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ChemInform Abstract: Synthesis and Evaluation of Some Novel 1,3,4‐Thiadiazoles for Antidiabetic Activity.

Cited by 10 publications

References 0 publications

Design and Synthesis of Thiadiazole Derivatives as Antidiabetic Agents

Design and Synthesis of Thiadiazole Derivatives as Antidiabetic Agents

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

Synthesis and in vitro antiproliferative activity of novel benzisoselenazolone derivatives

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