Synthesis of novel derivatives of 4-methylbenzimidazole and evaluation of their biological activities

Muhammad Taha; Nor Hadiani Ismail; Waqas Jamil; Hesham Rashwan; Syed Muhammad Kashif; Amyra Amat Sain; Mohd Ilham Adenan; El Hassane Anouar; Muhammad Ali; Fazal Rahim; Khalid M. Khan

doi:10.1016/j.ejmech.2014.07.078

Synthesis of novel derivatives of 4-methylbenzimidazole and evaluation of their biological activities

Muhammad Taha, Nor Hadiani Ismail, Waqas Jamil, Hesham Rashwan, Syed Muhammad Kashif, Amyra Amat Sain, Mohd Ilham Adenan, El Hassane Anouar, Muhammad Ali, Fazal Rahim, Khalid M. Khan

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

72 Scopus citations

Abstract

4-Methylbenzimidazole 1-28 novel derivatives were synthesized and evaluated for their antiglycation and antioxidant activities. Compounds 1-7 and 11 showed excellent activities ranged 140-280 μM, better than standard drug rutin (294.46 ± 1.50 μM). Compound 1-28 were also evaluated for DPPH activities. Compounds 1-8 showed excellent activities, ranging 12-29 μM, better than standard drug n-propylgallate (IC₅₀ = 30.30 ± 0.40 μM). For superoxide anion scavenging activity, compounds 1-7 showed better activity than standard n-propylgallate (IC₅₀ = 106.34 ± 1.6 μM), ranged 82-104 μM. These compounds were found to be nontoxic to THP-1 cells.

Original language	English
Pages (from-to)	731-738
Number of pages	8
Journal	European Journal of Medicinal Chemistry
Volume	84
DOIs	https://doi.org/10.1016/j.ejmech.2014.07.078
State	Published - 12 Sep 2014
Externally published	Yes

Keywords

Antiglycation
Antileishmanial
Antioxidant
Benzimidazole
Stereoisomers

UN SDGs

This output contributes to the following UN Sustainable Development Goals (SDGs)

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10.1016/j.ejmech.2014.07.078

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@article{bc9a05b58f2944058e700e2ddd012ba1,

title = "Synthesis of novel derivatives of 4-methylbenzimidazole and evaluation of their biological activities",

abstract = "4-Methylbenzimidazole 1-28 novel derivatives were synthesized and evaluated for their antiglycation and antioxidant activities. Compounds 1-7 and 11 showed excellent activities ranged 140-280 μM, better than standard drug rutin (294.46 ± 1.50 μM). Compound 1-28 were also evaluated for DPPH activities. Compounds 1-8 showed excellent activities, ranging 12-29 μM, better than standard drug n-propylgallate (IC50 = 30.30 ± 0.40 μM). For superoxide anion scavenging activity, compounds 1-7 showed better activity than standard n-propylgallate (IC50 = 106.34 ± 1.6 μM), ranged 82-104 μM. These compounds were found to be nontoxic to THP-1 cells.",

keywords = "Antiglycation, Antileishmanial, Antioxidant, Benzimidazole, Stereoisomers",

author = "Muhammad Taha and Ismail, \{Nor Hadiani\} and Waqas Jamil and Hesham Rashwan and Kashif, \{Syed Muhammad\} and Sain, \{Amyra Amat\} and Adenan, \{Mohd Ilham\} and Anouar, \{El Hassane\} and Muhammad Ali and Fazal Rahim and Khan, \{Khalid M.\}",

year = "2014",

month = sep,

day = "12",

doi = "10.1016/j.ejmech.2014.07.078",

language = "English",

volume = "84",

pages = "731--738",

journal = "European Journal of Medicinal Chemistry",

issn = "0223-5234",

publisher = "Elsevier Masson s.r.l.",

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TY - JOUR

T1 - Synthesis of novel derivatives of 4-methylbenzimidazole and evaluation of their biological activities

AU - Taha, Muhammad

AU - Ismail, Nor Hadiani

AU - Jamil, Waqas

AU - Rashwan, Hesham

AU - Kashif, Syed Muhammad

AU - Sain, Amyra Amat

AU - Adenan, Mohd Ilham

AU - Anouar, El Hassane

AU - Ali, Muhammad

AU - Rahim, Fazal

AU - Khan, Khalid M.

PY - 2014/9/12

Y1 - 2014/9/12

N2 - 4-Methylbenzimidazole 1-28 novel derivatives were synthesized and evaluated for their antiglycation and antioxidant activities. Compounds 1-7 and 11 showed excellent activities ranged 140-280 μM, better than standard drug rutin (294.46 ± 1.50 μM). Compound 1-28 were also evaluated for DPPH activities. Compounds 1-8 showed excellent activities, ranging 12-29 μM, better than standard drug n-propylgallate (IC50 = 30.30 ± 0.40 μM). For superoxide anion scavenging activity, compounds 1-7 showed better activity than standard n-propylgallate (IC50 = 106.34 ± 1.6 μM), ranged 82-104 μM. These compounds were found to be nontoxic to THP-1 cells.

AB - 4-Methylbenzimidazole 1-28 novel derivatives were synthesized and evaluated for their antiglycation and antioxidant activities. Compounds 1-7 and 11 showed excellent activities ranged 140-280 μM, better than standard drug rutin (294.46 ± 1.50 μM). Compound 1-28 were also evaluated for DPPH activities. Compounds 1-8 showed excellent activities, ranging 12-29 μM, better than standard drug n-propylgallate (IC50 = 30.30 ± 0.40 μM). For superoxide anion scavenging activity, compounds 1-7 showed better activity than standard n-propylgallate (IC50 = 106.34 ± 1.6 μM), ranged 82-104 μM. These compounds were found to be nontoxic to THP-1 cells.

KW - Antiglycation

KW - Antileishmanial

KW - Antioxidant

KW - Benzimidazole

KW - Stereoisomers

UR - http://www.scopus.com/inward/record.url?scp=84905161829&partnerID=8YFLogxK

U2 - 10.1016/j.ejmech.2014.07.078

DO - 10.1016/j.ejmech.2014.07.078

M3 - Article

C2 - 25069019

AN - SCOPUS:84905161829

SN - 0223-5234

VL - 84

SP - 731

EP - 738

JO - European Journal of Medicinal Chemistry

JF - European Journal of Medicinal Chemistry

ER -

Synthesis of novel derivatives of 4-methylbenzimidazole and evaluation of their biological activities

Abstract

Keywords

UN SDGs

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