Pharmacological Treatment of Obesity:  Therapeutic Strategies

Kordik, Cheryl P.; Reitz, Allen B.

doi:10.1021/jm980521l

Cited by 139 publications

(83 citation statements)

References 186 publications

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“…This strong inhibition effects of compounds (14)(15)(16) are in accordance with literature data, concerning fivemembered iminocyclitol derivatives as potent glycosidase inhibitors [38].…”

Section: Inhibition Of A-glucosidase Activity By N-hydroxycinnamoylsupporting

confidence: 91%

“…For this purpose a series of cinnamoyl and hydroxycinnamoyl amides (1)(2)(3)(4)(5)(6)(7)(8)(9)(10)(11)(12)(13)(14)(15)(16) were synthesized in solution phase by EDC/HOBt-mediated couplings as in previously described procedure [33]. Moreover, for the synthesis of C-terminal peptide amides (compounds 15, 16) the standard Fmoc-SPPS was carried out on Rink amide resin.…”

Section: Resultsmentioning

confidence: 99%

“…amides (1)(2)(3)(4)(5)(6)(7)(8)(9)(10)(11)(12)(13)(14) were obtained in moderate to excellent yields by solution phase peptide synthesis, according to the previously described procedure [33]. The chemical structures of all known compounds (1)(2)(3)(4)(5)(6)(7)(8)(9)(10)(11)(12)(13)(14) have been assigned on the basis of their spectral data and compared with published data [33,34].…”

Section: Solution Phase Peptide Synthesis N-hydroxycinnamoylmentioning

confidence: 99%

“…Moreover, the hydroxycinnamic acid amides containing proline (14)(15)(16) were also found to inhibit significantly the enzyme. This strong inhibition effects of compounds (14)(15)(16) are in accordance with literature data, concerning fivemembered iminocyclitol derivatives as potent glycosidase inhibitors [38].…”

Section: Inhibition Of A-glucosidase Activity By N-hydroxycinnamoylmentioning

confidence: 99%

“…The multiple functions of glucosidase inhibitors in the organism comprise the treatment of diabetes mellitus [10][11][12][13] and other diseases such as obesity, HIV infections, and tumors [14][15][16][17][18][19][20][21][22][23], which define these agents as potentially beneficial tools in prevention and treatment of such disorders. At the present, three antiglucosidase drugs, acarbose [24], miglitol [25], and voglibose [26], have been therapeutically used for non-insulin-dependent diabetes (type 2).…”

Section: Introductionmentioning

confidence: 99%

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Structure-Activity Relationships ofN-Cinnamoyl and Hydroxycinnamoyl Amides onα-Glucosidase Inhibition

Chochkova

Petrova

Stoykova

et al. 2017

Journal of Chemistry

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Currently, there is an increasing interest towards -glucosidase inhibition of various diseases including diabetes mellitus type 2, cancer, HIV, and B-and C-type viral hepatitis. Cinnamic acid derivatives have been shown to be potentially valuable as a new group of -glucosidase inhibitors. Therefore, herein, the -glucosidase inhibitory activity of trans-N-cinnamoyl and hydroxycinnamoyl amides was studied in vitro. Results revealed that the tested hydroxycinnamoyl amides (1-16) inhibited a-glucosidase with IC 50 s ranging between 0.76 and 355.1 g/ml. Compounds 1, 2, 5, 6, 9, 14, and 15 showed significant inhibition of yeast -glucosidase, being even more potent ones than the used positive inhibitor acarbose (IC 50 = 2.50 ± 0.21 g/ml).

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“…This strong inhibition effects of compounds (14)(15)(16) are in accordance with literature data, concerning fivemembered iminocyclitol derivatives as potent glycosidase inhibitors [38].…”

Section: Inhibition Of A-glucosidase Activity By N-hydroxycinnamoylsupporting

confidence: 91%

Section: Resultsmentioning

confidence: 99%

Section: Solution Phase Peptide Synthesis N-hydroxycinnamoylmentioning

confidence: 99%

Section: Inhibition Of A-glucosidase Activity By N-hydroxycinnamoylmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

See 3 more Smart Citations

Structure-Activity Relationships ofN-Cinnamoyl and Hydroxycinnamoyl Amides onα-Glucosidase Inhibition

Chochkova

Petrova

Stoykova

et al. 2017

Journal of Chemistry

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National Trends in Antiobesity Medication Use

Stafford¹,

Radley²

2003

Arch Intern Med

100

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Antiobesity Drugs

Tilley¹

2001

Kirk-Othmer Encyclopedia of Chemical Technology

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Obesity is a major medical problem in the United States. In the 1990s, an estimated 55% of the adult U.S. population were above their ideal body weights and as a consequence, were at risk for the development of various chronic ailments including diabetes, cardiovascular disease, and cancer. Both genetic and social factors contribute to the development of obesity. Currently available treatments include diet, exercise, anorectic sympathomimetic agents, and fat absorption inhibitors. Even though most patients are able to lose at least a portion of their excess weight, long‐term weight loss is extremely difficult to achieve, and behavior modification is an absolute requirement for ultimate success. The appetite suppressant drugs with significant sales, phenylpropanolamine, phentermine, and sibutramine, are based on stimulation of the sympathetic nervous system and are indicated only for short‐term treatment of obesity because of their side effect profile and lack of robust efficacy. The first fat absorption inhibitor, the pancreatic lipase inhibitor orlistat, was recently introduced to the U.S. market for use as an adjunct to a reduced‐calorie diet. Although drug treatment is not likely to replace diet and behavior modification for the control of obesity, newer therapeutic agents based on recent discoveries concerning the central nervous system integration of satiety signals and the mechanism of energy utilization in fat and skeletal muscle promise to provide new tools for the management of obesity. Presently, drugs hold only a minute share of the multibillion dollar weight loss market, but promise to capture a larger percentage, as more selective and effective agents become available.

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Pharmacological Treatment of Obesity: Therapeutic Strategies

Cited by 139 publications

References 186 publications

Structure-Activity Relationships ofN-Cinnamoyl and Hydroxycinnamoyl Amides onα-Glucosidase Inhibition

Structure-Activity Relationships ofN-Cinnamoyl and Hydroxycinnamoyl Amides onα-Glucosidase Inhibition

National Trends in Antiobesity Medication Use

Antiobesity Drugs

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