Insulin and Hypoglycemic Agents

Sleevi, M.

doi:10.1002/0471266949.bmc057

Cited by 4 publications

(2 citation statements)

References 193 publications

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“…The pKa value for thiazolidine-2,4-dione (1) heterocyclic ring is about 6.8 and thus this class of compounds is partially ionized at physiological PH is depicted in Figure 2. ▪ Removal of acidic head function of thiazolidine-2,4-dione (1) heterocyclic ring by N-methylation taken place at 3-position, which lead to loss of oral hypoglycemic activity 80,81 . However, methylation of the imide nitrogen of thiazolidine-2,4-dione (1) heterocyclic ring, which shows good oral hypoglycemic activity only at high level of dose of glitazones.…”

Section: Structure-activity-relationship (Sar) Studies Of Thiazolidinmentioning

confidence: 99%

“…▪ Replacement of central phenoxyalkyl linker (B) by naphthalene ring to give netoglitazone (14) compound of thiazolidine-2,4-diones class, which show more potent activity, as compared to rosiglitazone (4) 44 . Liphophilic Tail ▪ The brief review of oral hypoglycemic activity of thiazolidine-2,4-diones were shown that, incorporation of wide varieties of mostly aromatic and heteroaromatic rings present at liphophilic tail region were produced active agents of thiazolidine-2,4-diones class 80 . ▪ The lipophilic tail is attached to N-CH3 group of phenoxyethyl moiety of phenoxyalkyl linker (B).…”

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confidence: 99%

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Thiazolidine-2,4-Diones: An Update Review of Antidiabetic Agents

Dumbare¹,

Kawale²,

Nade³

et al. 2018

Int. Res. J. Pharm.

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Diabetes mellitus is a serious global health problem and taking its place as one of the main threats to human health in the 21 st century. The National Diabetes Information Clearinghouse & World Health Organization shows above 90% of the diabetic population fall under type 2 diabetes mellitus category. The treatment generally prescribed for type 2 diabetes mellitus has been a combination of diet, exercise and current therapeutic agents Due to their adverse effects and side effects, most of these treatments are considered to be unsatisfactory in terms of preventio n of complications and preservation of quality of life. The current therapeutic agents containing thiazolidine-2,4-diones or glitazones are shown better treatment on type 2 diabetes mellitus via acting on peroxisome proliferator-activated receptor-gamma (PPAR-γ). From these glitazones, troglitazone and rosiglitazone are withdrawn from markets. Pioglitazone and lobeglitazone are used in market. Ciglitazone, englitazone, darglitazone, KRP-297, rivoglitazone and CLX-921 are discontinued in various clinical trials. Mitoglitazone, netoglitazone and balaglitazone are present in various phases of clinical trials. Furthermore, based on various literature surveys, we are studied in details structure activity relationships of various glitazones.

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Section: Structure-activity-relationship (Sar) Studies Of Thiazolidinmentioning

confidence: 99%

mentioning

confidence: 99%

Thiazolidine-2,4-Diones: An Update Review of Antidiabetic Agents

Dumbare¹,

Kawale²,

Nade³

et al. 2018

Int. Res. J. Pharm.

View full text Add to dashboard Cite

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Non-Caloric Sweeteners, Sweetness Modulators, and Sweetener Enhancers

DuBois

Prakash²

2012

Annu. Rev. Food Sci. Technol.

165

148

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For a new sweetness technology to realize strong commercial success, it must be safe, exhibit good taste quality, be sufficiently soluble and stable in food and beverage systems, and be cost effective and patentable. Assessments of the commercial promise of eight synthetic and eight natural non-caloric sweeteners are made relevant to these metrics. High-potency (HP) non-caloric sweeteners, both synthetic and natural, are generally limited in taste quality by (a) low maximal sweetness response, (b) "off" tastes, (c) slow-onset sweet tastes that linger, and (d) sweet tastes that adapt or desensitize the gustatory system. Formulation approaches to address these limitations are discussed. Enhancement of the normal sucrose sensory response by action of a sweetener receptor positive allosteric modulator (PAM) has been achieved with very significant calorie reduction and with retention of the taste quality of sucrose. Research on PAM discovery over the past decade is summarized.

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