Sulfonamide-1,3,5-triazine–thiazoles: discovery of a novel class of antidiabetic agents via inhibition of DPP-4

Gao, Hai-De; Liu, Peng; Yang, Yang; Gao, Fang

doi:10.1039/c6ra15948f

Cited by 45 publications

(31 citation statements)

References 18 publications

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“…Furthermore, the presence of additional aromaticity did not influence the activity. Moreover, molecular docking results indicated that, ligand 157 was efficiently docked into the active site of the catalytic triad of Ser 630, Asp 708 and His 740 encompassing both S1 and S2 pocket with CDOCKER interaction energy of 57.80 [91]. At last, Iqbal and co-workers have developed arylsulfonylspiroimidazolidine-2,4-dione hybrids as potent hypoglycemic and ALR2 agents.…”

Section: Anti-diabetic Activitymentioning

confidence: 99%

Pharmaceutical and medicinal significance of sulfur (SVI)-Containing motifs for drug discovery: A critical review

Zhao

Rakesh

Ravidar

et al. 2019

European Journal of Medicinal Chemistry

449

183

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a b s t r a c tSulfur (S VI ) based moieties, especially, the sulfonyl or sulfonamide based analogues have showed a variety of pharmacological properties, and its derivatives propose a high degree of structural diversity that has established useful for the finding of new therapeutic agents. The developments of new less toxic, low cost and highly active sulfonamides containing analogues are hot research topics in medicinal chemistry. Currently, more than 150 FDA approved Sulfur (S VI )-based drugs are available in the market, and they are widely used to treat various types of diseases with therapeutic power. This comprehensive review highlights the recent developments of sulfonyl or sulfonamides based compounds in huge range of therapeutic applications such as antimicrobial, anti-inflammatory, antiviral, anticonvulsant, antitubercular, antidiabetic, antileishmanial, carbonic anhydrase, antimalarial, anticancer and other medicinal agents. We believe that, this review article is useful to inspire new ideas for structural design and developments of less toxic and powerful Sulfur (S VI ) based drugs against the numerous death-causing diseases.

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Section: Anti-diabetic Activitymentioning

confidence: 99%

Pharmaceutical and medicinal significance of sulfur (SVI)-Containing motifs for drug discovery: A critical review

Zhao

Rakesh

Ravidar

et al. 2019

European Journal of Medicinal Chemistry

449

183

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“…[18][19][20] However, GLP-1 exerts a short in vivo active duration due to the dipeptidyl peptidase IV (DPP-IV) digestion and rapid renal ltration, which severely limit its application in diabetes therapies. [21][22][23] According to our previous research, 24 the strategy to obtain the extended half-lives of peptide drugs was performed by fusing the peptide drugs with a lipidated the heptapeptide tags exerting high affinity for HSA. In order to develop the GLP-1 receptor agonist with prolonged active duration, we reoptimized the previous tags and fused the tag to the mutated GLP-1(7-37) via a thrombin-cleavable linker to construct novel GLP-1R agonist pro-drugs.…”

Section: Introductionmentioning

confidence: 99%

Design and evaluation of novel thrombin-based GLP-1 analogs with peptidic albumin binding domain for the controlled release of GLP-1

et al. 2020

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“…In this regard, derivatives of 1,3,5‐triazine have received considerable attention . 1,3,5‐Triazines have various pharmacological activities, such as antibacterial, antifungal, antimalarial, antidiabetic and anticystic fibrosis effects. Moreover, 1,3,5‐triazine exerts anticancer effects by inhibiting PI3K/mTOR, Rad6 ubiquitin conjugating enzyme and human epidermal growth factor receptor tyrosine kinases (EGFR‐TKs) …”

Section: Introductionmentioning

confidence: 99%

Novel 1,3,5‐triazine derivatives exert potent anti‐cervical cancer effects by modulating Bax, Bcl2 and Caspases expression

Wang

et al. 2017

Chem Biol Drug Des

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This study aimed to develop novel 1,3,5-triazine derivatives as potent anti-cervical cancer agents. The compounds were synthesized in short steps with an excellent yield and characterized via various spectroscopic and analytical methods. A structure-activity relationship study suggested that electron-withdrawing substituents showed greater anticancer activity than electron-donating groups. Compound 7p (p-fluoro) showed the highest activity against cervical cancer cells. In a nude mouse xenograft model inoculated with HeLa cells, 7p showed dose-dependent inhibition of cervical tumour growth. Histopathological examination of excised tumour-bearing tissues showed that 7p improved the microstructure in a dose-dependent manner. Compound 7p also increased the proportions of HeLa cells in G0/G1 and S-phase and significantly decreased that of G2/M-phase. The effects of 7p on C-caspase-3, C-caspase-9, Bcl-2 and Bax expression in HeLa cells were also determined.

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Sulfonamide-1,3,5-triazine–thiazoles: discovery of a novel class of antidiabetic agents via inhibition of DPP-4

Abstract: Dipeptidyl peptidase-4 (DPP-4) inhibitors are a novel class of antidiabetic drugs used for treating type 2 diabetes mellitus.

Cited by 45 publications

References 18 publications

Pharmaceutical and medicinal significance of sulfur (SVI)-Containing motifs for drug discovery: A critical review

Pharmaceutical and medicinal significance of sulfur (SVI)-Containing motifs for drug discovery: A critical review

Design and evaluation of novel thrombin-based GLP-1 analogs with peptidic albumin binding domain for the controlled release of GLP-1

Novel 1,3,5‐triazine derivatives exert potent anti‐cervical cancer effects by modulating Bax, Bcl2 and Caspases expression

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