Synthesis and evaluation of novel triazoles and mannich bases functionalized 1,4-dihydropyridine as angiotensin converting enzyme (ACE) inhibitors

Ravindra M. Kumbhare; Umesh B. Kosurkar; Pankaj K. Bagul; Abhinav Kanwal; K. Appalanaidu; Tulshiram L. Dadmal; Sanjay Kumar Banerjee

doi:10.1016/j.bmc.2014.09.027

Synthesis and evaluation of novel triazoles and mannich bases functionalized 1,4-dihydropyridine as angiotensin converting enzyme (ACE) inhibitors

Ravindra M. Kumbhare, Umesh B. Kosurkar, Pankaj K. Bagul, Abhinav Kanwal, K. Appalanaidu, Tulshiram L. Dadmal, Sanjay Kumar Banerjee

Department of Pharmacology, Manipal College of Pharmaceutical Sciences, Manipal

Research output: Contribution to journal › Article › peer-review

15 Citations (Scopus)

Abstract

A series of novel diethyl 2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylate embedded triazole and mannich bases were synthesized, and evaluated for their angiotensin converting enzyme (ACE) inhibitory activity. Screening of above synthesized compounds for ACE inhibition showed that triazoles functionalized compounds have better ACE inhibitory activity compared to that of mannich bases analogues. Among all triazoles we found 6h, 6i and 6j to have good ACE inhibition activity with IC₅₀ values 0.713 μM, 0.409 μM and 0.653 μM, respectively. Among mannich bases series compounds, only 7c resulted as most active ACE inhibitor with IC₅₀ value of 0.928 μM.

Original language	English
Pages (from-to)	5824-5830
Number of pages	7
Journal	Bioorganic and Medicinal Chemistry
Volume	22
Issue number	21
DOIs	https://doi.org/10.1016/j.bmc.2014.09.027
Publication status	Published - 01-11-2014

All Science Journal Classification (ASJC) codes

Biochemistry
Molecular Medicine
Molecular Biology
Pharmaceutical Science
Drug Discovery
Clinical Biochemistry
Organic Chemistry

Access to Document

10.1016/j.bmc.2014.09.027

Cite this

@article{383b39c7c8aa4cecaa3cbf941d6ccf5a,

title = "Synthesis and evaluation of novel triazoles and mannich bases functionalized 1,4-dihydropyridine as angiotensin converting enzyme (ACE) inhibitors",

abstract = "A series of novel diethyl 2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylate embedded triazole and mannich bases were synthesized, and evaluated for their angiotensin converting enzyme (ACE) inhibitory activity. Screening of above synthesized compounds for ACE inhibition showed that triazoles functionalized compounds have better ACE inhibitory activity compared to that of mannich bases analogues. Among all triazoles we found 6h, 6i and 6j to have good ACE inhibition activity with IC50 values 0.713 μM, 0.409 μM and 0.653 μM, respectively. Among mannich bases series compounds, only 7c resulted as most active ACE inhibitor with IC50 value of 0.928 μM.",

author = "Kumbhare, {Ravindra M.} and Kosurkar, {Umesh B.} and Bagul, {Pankaj K.} and Abhinav Kanwal and K. Appalanaidu and Dadmal, {Tulshiram L.} and Banerjee, {Sanjay Kumar}",

year = "2014",

month = nov,

day = "1",

doi = "10.1016/j.bmc.2014.09.027",

language = "English",

volume = "22",

pages = "5824--5830",

journal = "Bioorganic and Medicinal Chemistry",

issn = "0968-0896",

publisher = "Elsevier Ireland Ltd",

number = "21",

}

TY - JOUR

T1 - Synthesis and evaluation of novel triazoles and mannich bases functionalized 1,4-dihydropyridine as angiotensin converting enzyme (ACE) inhibitors

AU - Kumbhare, Ravindra M.

AU - Kosurkar, Umesh B.

AU - Bagul, Pankaj K.

AU - Kanwal, Abhinav

AU - Appalanaidu, K.

AU - Dadmal, Tulshiram L.

AU - Banerjee, Sanjay Kumar

PY - 2014/11/1

Y1 - 2014/11/1

N2 - A series of novel diethyl 2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylate embedded triazole and mannich bases were synthesized, and evaluated for their angiotensin converting enzyme (ACE) inhibitory activity. Screening of above synthesized compounds for ACE inhibition showed that triazoles functionalized compounds have better ACE inhibitory activity compared to that of mannich bases analogues. Among all triazoles we found 6h, 6i and 6j to have good ACE inhibition activity with IC50 values 0.713 μM, 0.409 μM and 0.653 μM, respectively. Among mannich bases series compounds, only 7c resulted as most active ACE inhibitor with IC50 value of 0.928 μM.

AB - A series of novel diethyl 2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylate embedded triazole and mannich bases were synthesized, and evaluated for their angiotensin converting enzyme (ACE) inhibitory activity. Screening of above synthesized compounds for ACE inhibition showed that triazoles functionalized compounds have better ACE inhibitory activity compared to that of mannich bases analogues. Among all triazoles we found 6h, 6i and 6j to have good ACE inhibition activity with IC50 values 0.713 μM, 0.409 μM and 0.653 μM, respectively. Among mannich bases series compounds, only 7c resulted as most active ACE inhibitor with IC50 value of 0.928 μM.

UR - http://www.scopus.com/inward/record.url?scp=84908419203&partnerID=8YFLogxK

UR - http://www.scopus.com/inward/citedby.url?scp=84908419203&partnerID=8YFLogxK

U2 - 10.1016/j.bmc.2014.09.027

DO - 10.1016/j.bmc.2014.09.027

M3 - Article

C2 - 25300819

AN - SCOPUS:84908419203

SN - 0968-0896

VL - 22

SP - 5824

EP - 5830

JO - Bioorganic and Medicinal Chemistry

JF - Bioorganic and Medicinal Chemistry

IS - 21

ER -

Synthesis and evaluation of novel triazoles and mannich bases functionalized 1,4-dihydropyridine as angiotensin converting enzyme (ACE) inhibitors

Abstract

All Science Journal Classification (ASJC) codes

Access to Document

Other files and links

Fingerprint

Cite this