Design, synthesis, and docking studies of novel telmisartan-glitazone hybrid analogs for the treatment of metabolic syndrome

Amar G. Chittiboyina; Cassia S. Mizuno; Prashant V. Desai; Akshay Patny; Theodore W. Kurtz; Harrihar A. Pershadsingh; Robert C. Speth; Vardan Karamyan; Mitchell A. Avery

doi:10.1007/s00044-008-9152-x

Design, synthesis, and docking studies of novel telmisartan-glitazone hybrid analogs for the treatment of metabolic syndrome

Amar G. Chittiboyina
, Cassia S. Mizuno
, Prashant V. Desai
, Akshay Patny
, Theodore W. Kurtz
, Harrihar A. Pershadsingh
, Robert C. Speth
, Vardan Karamyan
, Mitchell A. Avery

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

9 Scopus citations

Abstract

A novel hybrid class of telmisartan-rosiglitazone molecules was synthesized in an attempt to discover a dual peroxisome proliferator-activated receptor gamma (PPARγ) agonist/angiotensin II antagonist for treatment for metabolic syndrome. Almost all the synthesized molecules showed moderate PPARγ activity. However, none of the hybrid analogs showed binding affinity toward the AT1 receptor.

Original language	English
Pages (from-to)	589-610
Number of pages	22
Journal	Medicinal Chemistry Research
Volume	18
Issue number	7
DOIs	https://doi.org/10.1007/s00044-008-9152-x
State	Published - Jan 26 2009
Externally published	Yes

ASJC Scopus Subject Areas

General Pharmacology, Toxicology and Pharmaceutics
Organic Chemistry

Keywords

AT antagonist
Glitazones
Hypertension
Metabolic syndrome
PPAR gamma
Telmisartan
Type 2 diabetes
AT1 antagonist

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10.1007/s00044-008-9152-x

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title = "Design, synthesis, and docking studies of novel telmisartan-glitazone hybrid analogs for the treatment of metabolic syndrome",

abstract = "A novel hybrid class of telmisartan-rosiglitazone molecules was synthesized in an attempt to discover a dual peroxisome proliferator-activated receptor gamma (PPARγ) agonist/angiotensin II antagonist for treatment for metabolic syndrome. Almost all the synthesized molecules showed moderate PPARγ activity. However, none of the hybrid analogs showed binding affinity toward the AT1 receptor.",

keywords = "AT antagonist, Glitazones, Hypertension, Metabolic syndrome, PPAR gamma, Telmisartan, Type 2 diabetes, AT1 antagonist",

author = "Chittiboyina, \{Amar G.\} and Mizuno, \{Cassia S.\} and Desai, \{Prashant V.\} and Akshay Patny and Kurtz, \{Theodore W.\} and Pershadsingh, \{Harrihar A.\} and Speth, \{Robert C.\} and Vardan Karamyan and Avery, \{Mitchell A.\}",

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doi = "10.1007/s00044-008-9152-x",

language = "English",

volume = "18",

pages = "589--610",

journal = "Medicinal Chemistry Research",

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T1 - Design, synthesis, and docking studies of novel telmisartan-glitazone hybrid analogs for the treatment of metabolic syndrome

AU - Chittiboyina, Amar G.

AU - Mizuno, Cassia S.

AU - Desai, Prashant V.

AU - Patny, Akshay

AU - Kurtz, Theodore W.

AU - Pershadsingh, Harrihar A.

AU - Speth, Robert C.

AU - Karamyan, Vardan

AU - Avery, Mitchell A.

PY - 2009/1/26

Y1 - 2009/1/26

N2 - A novel hybrid class of telmisartan-rosiglitazone molecules was synthesized in an attempt to discover a dual peroxisome proliferator-activated receptor gamma (PPARγ) agonist/angiotensin II antagonist for treatment for metabolic syndrome. Almost all the synthesized molecules showed moderate PPARγ activity. However, none of the hybrid analogs showed binding affinity toward the AT1 receptor.

AB - A novel hybrid class of telmisartan-rosiglitazone molecules was synthesized in an attempt to discover a dual peroxisome proliferator-activated receptor gamma (PPARγ) agonist/angiotensin II antagonist for treatment for metabolic syndrome. Almost all the synthesized molecules showed moderate PPARγ activity. However, none of the hybrid analogs showed binding affinity toward the AT1 receptor.

KW - AT antagonist

KW - Glitazones

KW - Hypertension

KW - Metabolic syndrome

KW - PPAR gamma

KW - Telmisartan

KW - Type 2 diabetes

KW - AT1 antagonist

UR - https://www.scopus.com/pages/publications/70349243286

UR - https://www.scopus.com/pages/publications/70349243286#tab=citedBy

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M3 - Article

AN - SCOPUS:70349243286

SN - 1054-2523

VL - 18

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JO - Medicinal Chemistry Research

JF - Medicinal Chemistry Research

IS - 7

ER -

Design, synthesis, and docking studies of novel telmisartan-glitazone hybrid analogs for the treatment of metabolic syndrome

Abstract

ASJC Scopus Subject Areas

Keywords

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