volume 41 issue 11 pages 1127-1140

Design, synthesis and chemical stability of indolizine derivatives for antidiabetic activity

M Basavaraj 1
D. Giles 2
Amit Kumar Das 2
Suresh Janadri 1
Ganesh S Andhale 3
1
 
Department of Pharmaceutical Chemistry, Nitte College of Pharmaceutical Sciences, Yelahanka, Bengaluru, Karnataka, India
2
 
Department of Pharmaceutical Chemistry, Acharya & BM Reddy College of Pharmacy, Bengaluru, Karnataka, India
3
 
Department of Pharmaceutical Chemistry, Alard College of Pharmacy, Pune, India
Publication typeJournal Article
Publication date2022-07-20
scimago Q3
wos Q4
SJR0.312
CiteScore2.1
Impact factor1.3
ISSN15257770, 15322335
Biochemistry
General Medicine
Genetics
Molecular Medicine
Abstract
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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GOST Copy
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.
GOST all authors (up to 50) Copy
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.
RIS |
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RIS Copy
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 -
BibTex |
Cite this
BibTex (up to 50 authors) Copy
@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}
}
MLA
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MLA Copy
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.