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.",

}

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 - https://www.scopus.com/pages/publications/84905161829

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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