Design, Synthesis and Preliminary Pharmacological Evaluation of New Metformin Derivatives

Mahdi, Monther F.; Arif, Inam Sameh; Jubair, Najwan

doi:10.22159/ijpps.2017v9i1.15250

Cited by 3 publications

References 21 publications

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Entering the Sugar Rush Era: Revisiting the Antihyperglycemic Activities of Biguanides after a Century of Metformin Discovery

Neto

Barssotti

Fiori-Duarte

et al. 2023

CMC

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The development of clinically viable metformin analogs is a challenge largely to be overcome. Despite being an extremely efficient drug for the treatment of type 2 diabetes mellitus, multiple studies were conducted seeking to improve its hypoglycemic activity or to ameliorate aspects such as the low oral absorption and the incidence of gastrointestinal side effects. Furthermore, efforts have been made to attribute new activities, or even to expand the pre-existing ones, that could enhance its effects in the diabetes, such as pancreas-protective, antioxidant, and anti-inflammatory activities. In this manuscript, we describe the analogs of metformin developed in the last three decades, highlighting the lack of computationally based rational approaches to guide their development. We also discuss this is probably a consequence of how unclear the mechanism of action of the parent drug is and highlight the recent advances towards establishment of the main molecular target(s) for metformin. We also explored the binding of metformin, buformin and phenformin to the mitochondrial respiratory chain complex I through molecular docking analyses and reviewed the prospects of applying computational tools to improve the success in the development of such analogs. Therefore, it becomes evident the wide range of molecular targets, as well as the multiple activities displayed by metformin, make this drug a promising prototype for the development of novel entities, particularly for the treatment of type 2 diabetes mellitus.

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Entering the Sugar Rush Era: Revisiting the Antihyperglycemic Activities of Biguanides after a Century of Metformin Discovery

Neto

Barssotti

Fiori-Duarte

et al. 2023

CMC

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The Effect of Concentration Calcium Alginate On Metformine Encapsulated

Cahyaningrum¹,

Herdyastuti²,

Amaria³

et al. 2019

Proceedings of the National Seminar on Chemistry 2019 (SNK-19)

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This research aimed to study the effect of concentration calcium alginate on metformine encapsulation processes and investigated characteristic of metformine encapsulation. The encapsulation of metformine performed using chitosan and calcium alginate polymers with calcium chloride as crosslink agent. The concentrations of calcium alginate were varieties 0.5%; 1.0%; 1.5%; 2.0%; 2.5%; and 3.0% (w/v). The results showed that the highest encapsulation efficiency of metformine on concentration of alginate 2.0% (w/v) and the lowest in the alginate 0% (w/v), respectively by 80.51% and 55.94%. Encapsulation resulted with the highest the spectra FTIR analysis showed that there is vibration in 1497.91 cm-1 that indicated interaction between the carboxyl functional group of alginate and the amine functional group of chitosan

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Assessment of Symptoms, Pregnancy Outcome, and Health-Related Quality of Life among PCOS women Treated with Myo inositol and Metformin

Zainab Abdul Hameed Ibrahim,

Manal Khaled Abdulrida,

Rana Basil Razoqi

2023

AJPS

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PCOS is a complicated endocrine disorder that mostly affects between 5% and 10% of women who are of reproductive age. Obesity, hyperandrogenism, and oligo- or anovulation are frequent clinical PCOS signs. Objective: the study was designed to evaluate the effect of combining Metformin and Myoinositol; the main insulin-sensitizing drugs on improving symptoms and HRQOLQ in PCOS women. Materials and Methods: A study was a prospective, interventional, comparative clinical study conducted on 54 patients (aged 18-40 y) who are divided into three groups: group1 patients allocated to receive Myo-inositol(4g), group2 patients allocated to receive Metformin(1g) and group3 patients allocated to receive Myo-inositol(4g) + Metformin(1g) all for 3 months. Baseline and after 3 months, patients’ information and health related quality of life were documented. Result: Metformin and Myoinositol resulted in symptoms improvement within each study groups as (68.8%, 87.5% and 94.1%) for group 1,2 and 3 respectively, only 4 patients from all groups became pregnant. Also, significant change in HRQOLQ in all study groups after three months of treatment were reported. Conclusion: combining Myoinositol with metformin results in improved PCOS symptoms and pregnancy outcome in addition to improved patient’s quality of life.

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Design, Synthesis and Preliminary Pharmacological Evaluation of New Metformin Derivatives

Cited by 3 publications

References 21 publications

Entering the Sugar Rush Era: Revisiting the Antihyperglycemic Activities of Biguanides after a Century of Metformin Discovery

Entering the Sugar Rush Era: Revisiting the Antihyperglycemic Activities of Biguanides after a Century of Metformin Discovery

The Effect of Concentration Calcium Alginate On Metformine Encapsulated

Assessment of Symptoms, Pregnancy Outcome, and Health-Related Quality of Life among PCOS women Treated with Myo inositol and Metformin

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