Carbazole-containing sulfonamides and sulfamides: Discovery of cryptochrome modulators as antidiabetic agents

Humphries, Paul S.; Bersot, Ross; Kincaid, John; Mabery, Eric; McCluskie, Kerryn; Park, Timothy; Renner, Travis; Riegler, Erin; Steinfeld, Tod; Turtle, Eric D; Wei, Zhi-Liang; Willis, Erik

doi:10.1016/j.bmcl.2015.12.102

Cited by 60 publications

(30 citation statements)

References 28 publications

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“…Researchers have been investigated various compounds containing sulfonamide moieties. They are tryptamine 1 , chalcones 2 , adamantine 3 , azetidinone 4 , carbazole 5 , catenane 6 , cinnamic acyl 7 , coumarin 8 , cyanopyridines, isoxazoles, pyrazoles, pyrimidines 9 , epipodophyllotoxin 10 , furan containing vinyl sulfonamides 11 , isoquinoline sulfonamide 12 , oxazolidinones 13 , quinolone 14 , thiadiazole 15 , thiazole,pyridone, chromene, hydrazine 16 , thiouracil 17 and triazole 18 . Due to its greater effectiveness and less toxicity it establishes a main class of drugs with numerous types of pharmacological potentials such as antibacterial 19 , antitumor 20 , anti-carbonic anhydrase [21][22][23] , antiretro-viral 24 , anti-malarial 25 , anti-HIV [26].…”

Section: Introductionmentioning

confidence: 99%

Bio-Potent Sulfonamides

Dineshkumar

Thirunarayanan

2019

J. Chil. Chem. Soc.

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Some 4-(substituted phenylsulfonamido)benzoic acids have been synthesized by fly-ash:H 3 PO 3 nano catalyst catalyzed condensation of substituted benzenesulfonyl chlorides and 4-aminobenzoic acid in ultrasound irradiation conditions. The yields of the sulfonamides are more than 90%. The synthesized 4-(substituted phenylsulfonamido) benzoic acid derivatives were characterized by their physical constants, analytical and spectroscopic data. Antimicrobial activities of all sulfonamides were measured by Bauer-Kirby disc diffusion method.

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Section: Introductionmentioning

confidence: 99%

Bio-Potent Sulfonamides

Dineshkumar

Thirunarayanan

2019

J. Chil. Chem. Soc.

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“…Com- stronger cryptochrome modulator with EC 50 ¼ 0.144 mM. The SAR suggested that, the presence of sulfonamides functional group improved lipophilic efficiency of the potent analog [88]. Recently, Deka and co-workers have prepared a new series of thiazolidinediones hybrids and screened for potent peroxisome proliferatoractivated receptor g (PPARg).…”

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

380

174

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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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“…116,119 Consistent with the known role of CRYs in suppressing gluconeogenesis, KL001 administration was shown to improve glucose tolerance in diet-induced obese (DIO) mice. 116,120 Recent investigations have also identified several modulators of CC-components RORa/c and REV-ERBa/b with therapeutic potential in animal models of metabolic disorders. [116][117][118] In this regard, agonists of REV-ERBs (SR9009 and SR9011), 121 and an inverse ROR agonist (SR1555), 122 were found to improve several metabolic parameters in DIO mice.…”

Section: Chronopharmacology: Detoxification Pharmacokinetics and Dymentioning

confidence: 99%

The circadian clock and liver function in health and disease

Mukherji

Bailey

Staels

et al. 2019

Journal of Hepatology

138

116

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Each day, all organisms are subjected to changes in light intensity because of the Earth's rotation around its own axis. To anticipate this geo-physical variability, and to appropriately respond biochemically, most species, including mammals, have evolved an approximate 24-hour endogenous timing mechanism known as the circadian clock (CC). The 'clock' is self-sustained, cell autonomous and present in every cell type. At the core of the clock resides the CC-oscillator, an exquisitely crafted transcriptional-translational feedback system. Remarkably, components of the CC-oscillator not only maintain daily rhythmicity of their own synthesis, but also generate temporal variability in the expression levels of numerous target genes through transcriptional, post-transcriptional and post-translational mechanisms, thus, ensuring proper chronological coordination in the functioning of cells, tissues and organs, including the liver. Indeed, a variety of physiologically critical hepatic functions and cellular processes are CC-controlled. Thus, it is not surprising that modern lifestyle factors (e.g. travel and jet lag, night and rotating shift work), which force 'circadian misalignment', have emerged as major contributors to global health problems including obesity, non-alcoholic fatty liver disease and steatohepatitis. Herein, we provide an overview of the CC-dependent pathways which play critical roles in mediating several hepatic functions under physiological conditions, and whose deregulation is implicated in chronic liver diseases including non-alcoholic steatohepatitis and alcohol-related liver disease.

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Carbazole-containing sulfonamides and sulfamides: Discovery of cryptochrome modulators as antidiabetic agents

Cited by 60 publications

References 28 publications

Bio-Potent Sulfonamides

Bio-Potent Sulfonamides

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

The circadian clock and liver function in health and disease

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