Design, synthesis and chemical stability of indolizine derivatives for antidiabetic activity
1
Department of Pharmaceutical Chemistry, Nitte College of Pharmaceutical Sciences, Yelahanka, Bengaluru, Karnataka, India
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2
Department of Pharmaceutical Chemistry, Acharya & BM Reddy College of Pharmacy, Bengaluru, Karnataka, India
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3
Department of Pharmaceutical Chemistry, Alard College of Pharmacy, Pune, India
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Тип публикации: Journal Article
Дата публикации: 2022-07-20
scimago Q3
wos Q4
БС3
SJR: 0.312
CiteScore: 2.1
Impact factor: 1.3
ISSN: 15257770, 15322335
PubMed ID:
35856484
Biochemistry
General Medicine
Genetics
Molecular Medicine
Краткое описание
Prodrugs of metformin were synthesized with the goal of enhancing biological activity of metformin. They were synthesized by combining metformin with 2-substituted indolizine (C7-C12). The synthesized prodrugs were characterized by IR, 1H NMR, 13C NMR, and mass spectroscopy. The chemical hydrolysis of C7-C12 was carried out at pH 1.2, 6.8, and 7.4. All compounds showed encouraging chemical stability at pH 1.2 and 6.8, whereas mild hydrolysis was shown at pH 7.4. Further prodrugs were screened for antidiabetic activity using a streptozotocin-induced model in rat. These derivatives showed substantial results. Among them C8 showed significant activity in the reduction of streptozotocin-induced blood glucose in rats when compared to that of metformin, indicating the effectiveness of prodrug.
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Basavaraj M. et al. Design, synthesis and chemical stability of indolizine derivatives for antidiabetic activity // Nucleosides, Nucleotides and Nucleic Acids. 2022. Vol. 41. No. 11. pp. 1127-1140.
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Basavaraj M., Giles D., Das A. K., Janadri S., Andhale G. S. Design, synthesis and chemical stability of indolizine derivatives for antidiabetic activity // Nucleosides, Nucleotides and Nucleic Acids. 2022. Vol. 41. No. 11. pp. 1127-1140.
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TY - JOUR
DO - 10.1080/15257770.2022.2100418
UR - https://doi.org/10.1080/15257770.2022.2100418
TI - Design, synthesis and chemical stability of indolizine derivatives for antidiabetic activity
T2 - Nucleosides, Nucleotides and Nucleic Acids
AU - Basavaraj, M
AU - Giles, D.
AU - Das, Amit Kumar
AU - Janadri, Suresh
AU - Andhale, Ganesh S
PY - 2022
DA - 2022/07/20
PB - Taylor & Francis
SP - 1127-1140
IS - 11
VL - 41
PMID - 35856484
SN - 1525-7770
SN - 1532-2335
ER -
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@article{2022_Basavaraj,
author = {M Basavaraj and D. Giles and Amit Kumar Das and Suresh Janadri and Ganesh S Andhale},
title = {Design, synthesis and chemical stability of indolizine derivatives for antidiabetic activity},
journal = {Nucleosides, Nucleotides and Nucleic Acids},
year = {2022},
volume = {41},
publisher = {Taylor & Francis},
month = {jul},
url = {https://doi.org/10.1080/15257770.2022.2100418},
number = {11},
pages = {1127--1140},
doi = {10.1080/15257770.2022.2100418}
}
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Basavaraj, M., et al. “Design, synthesis and chemical stability of indolizine derivatives for antidiabetic activity.” Nucleosides, Nucleotides and Nucleic Acids, vol. 41, no. 11, Jul. 2022, pp. 1127-1140. https://doi.org/10.1080/15257770.2022.2100418.