Antihyperglycemic Activity of 2‐Methyl‐3,4,5‐triaryl‐1H‐pyrroles in SLM and STZ Models.

Goel, Atul; Agarwal, Nidhi; Singh, Fateh V.; Sharon, Ashoke; Tiwari, Piyush; Dixit, Manish; Pratap, Ramendra; Srivastava, Arvind K.; Maulik, Prakas R.; Ram, Vishnu Ji

doi:10.1002/chin.200426094

Cited by 19 publications

(22 citation statements)

References 1 publication

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“…21,22 In current scenario, the treatment of type 2 diabetes has been revolutionized with the advent of insulin sensitizers like rosiglitazone and pioglitazone that ameliorate insulin resistance and thereby normalize elevated blood glucose levels but are also associated with hepatotoxicity, weight gain, and edema (Table I). 23,24 The alarming situation emphasized the need to discover new antihyperglycemic agents with reduced or no side effect.…”

Section: Development Perspectives and Current Statusmentioning

confidence: 99%

“…Holmes et al at Affymax reported a series of novel sulfonamides containing a single DFMP group as potent inhibitors of PTP 1B. SAR around the scaffold was also investigated, leading to the identification of compounds with IC 50 or K i values in the low nanomolar range (17)(18)(19)(20)(21) (Table VI). These sulfonamide-based inhibitors exhibit 100 and 30 times higher inhibitory activity than the corresponding tertiary amines and carboxamides, respectively.…”

Section: B Phosphorus-containing Phosphotyrosyl Mimeticsmentioning

confidence: 99%

See 1 more Smart Citation

Protein Tyrosine Phosphatase 1B Inhibitors: A Molecular Level Legitimate Approach for the Management of Diabetes Mellitus

Thareja

Aggarwal

Bhardwaj

et al. 2010

Medicinal Research Reviews

109

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Diabetes mellitus is a systemic disease responsible for morbidity in the western world and is gradually becoming prevalent in developing countries too. The prevalence of diabetes is rapidly increasing in industrialized countries and type 2 diabetes accounts for 90% of the disease. Insulin resistance is a major pathophysiological factor in the development of type 2 diabetes, occurring mainly in muscle, adipose tissues, and liver leading to reduced glucose uptake and utilization and increased glucose production. The prevalence and rising incidence of diabetes emphasized the need to explore new molecular targets and strategies to develop novel antihyperglycemic agents. Protein Tyrosine Phosphatase 1B (PTP 1B) has recently emerged as a promising molecular level legitimate therapeutic target in the effective management of type 2 diabetes. PTP 1B, a cytosolic nonreceptor PTPase, has been implicated as a negative regulator of insulin signal transduction. Therefore, PTP 1B inhibitors would increase insulin sensitivity by blocking the PTP 1B-mediated negative insulin signaling pathway and might be an attractive target for type 2 diabetes mellitus and obesity. With X-ray crystallography and NMR-based fragment screening, the binding interactions of several classes of inhibitors have been elucidated, which could help the design of future PTP 1B inhibitors. The drug discovery research in PTP 1B is a challenging area to work with and many pharmaceutical organizations and academic research laboratories are focusing their research toward the development of potential PTP 1B inhibitors which would prove to be a milestone for the management of diabetes.

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Section: Development Perspectives and Current Statusmentioning

confidence: 99%

Section: B Phosphorus-containing Phosphotyrosyl Mimeticsmentioning

confidence: 99%

Protein Tyrosine Phosphatase 1B Inhibitors: A Molecular Level Legitimate Approach for the Management of Diabetes Mellitus

Thareja

Aggarwal

Bhardwaj

et al. 2010

Medicinal Research Reviews

109

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“…Os pirázois apresentaram atividade hipoglicemiante in vivo, provavelmente através da inibição da atividade do canal ATP-K + das membranas das células β-pancreáticas, o que induz a produção de insulina (Cottineau et al, 2002). Os derivados de 1Hpirróis,2-metil-3,4,5-trifenil-substituídos mostraram inibição da hiperglicemia pós-prandial em ratos normais e diminuíram a taxa de glicose no plasma dos ratos com diabetes induzido por estreptozotocina (Goel et al, 2004). As piridinas e purinas que contêm o grupo 2,4tiazolidinodiona apresentaram atividade hipoglicêmica (Kim et al, 2004).…”

Section: G Negri 132unclassified

Diabetes melito: plantas e princípios ativos naturais hipoglicemiantes

Negri¹

2005

Rev. Bras. Cienc. Farm.

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O diabetes melito é considerada como uma síndrome que é, quanto a etiologia e patogênese, caracterizada por alterar a homeostase do organismo, por distúrbios metabólicos complexos e primários dos carboidratos, que envolvem secundariamente, porém de forma importante, lipídeos e proteínas. Grande número de espécies de plantas tem sido usado experimentalmente para tratar os sintomas do diabetes melito e a distância filogenética entre este grupo de plantas é forte indicação da natureza variada de seus constituintes. Tem sido constatado que muitas substâncias extraídas de plantas reduzem o nível de glicose no sangue. A grande diversidade de classes químicas indica que uma variedade de mecanismos de ação deve estar envolvida na redução do nível de glicose no sangue. Algumas destas substâncias podem ter potencial terapêutico enquanto outras podem produzir hipoglicemia como um efeito colateral devido à sua toxicidade, especialmente hepatotoxidade. Este artigo apresenta uma revisão atualizada e acrescenta mais plantas e princípios ativos hipoglicemiantes à extensa lista existente nos artigos de revisão anteriores.

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“…Other natural and novel compounds that were tested and reported for potential antihyperglycemic properties (for instance, [113,[129][130][131][132][133][134][135][136]), mostly without detailed characterization of cellular targets and molecular interactions, are not discussed in this review.…”

Section: Insulin Receptor Agonists/enhancersmentioning

confidence: 99%

Glucose Transport Regulators

Ben-Yakir¹,

Gruzman²,

Alpert³

et al. 2005

CMCIEMA

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The prevalence of Type 2 diabetes (Non-Insulin-Dependent Diabetes Mellitus) increases at an alarming rate in the world's population, reaching an epidemic proportion. Moreover, impaired glucose tolerance and insulin resistance are being diagnosed nowadays in a growing subpopulation of obese children and adolescents, mostly in Western societies. This adds to the concern that not only the number of NIDDM patients will increase dramatically to over 300 millions within 20 years, but also that overt diabetes and diabetes-related complications will develop earlier in life. The main goal of pharmacological therapy of diabetic patients is to reduce blood glucose levels to the normal range. Indeed, most diabetic patients require oral antihyperglycemic drug therapy; yet, the relatively high rate of failure of these drugs and the chronic nature of the disease, which is associated with progressive dysfunction and exhaustion of pancreatic insulinproducing β-cells, lead in many cases to insulin therapy. Most available antihyperglycemic drugs sensitize β-cells to secrete insulin or overcome peripheral insulin resistance by sensitizing insulin-responsive tissues towards insulin. Nevertheless, genuine insulin mimetic drugs or drugs aimed at directly augmenting the glucose transport system in insulinsensitive tissues are still being sought. This review describes briefly current molecular targets for antihyperglycemic drugs and discusses potential compounds that may act as insulin-mimetics or enhancers. In addition, a novel concept is introduced for the development of carbohydrate derivatives that may augment glucose transport in insulin-sensitive tissues in an insulin-independent manner.

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Antihyperglycemic Activity of 2‐Methyl‐3,4,5‐triaryl‐1H‐pyrroles in SLM and STZ Models.

Cited by 19 publications

References 1 publication

Protein Tyrosine Phosphatase 1B Inhibitors: A Molecular Level Legitimate Approach for the Management of Diabetes Mellitus

Protein Tyrosine Phosphatase 1B Inhibitors: A Molecular Level Legitimate Approach for the Management of Diabetes Mellitus

Diabetes melito: plantas e princípios ativos naturais hipoglicemiantes

Glucose Transport Regulators

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