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

被引:69
|
作者
Taha, Muhammad [1 ,2 ]
Ismail, Nor Hadiani [1 ,2 ]
Jamil, Waqas [3 ]
Rashwan, Hesham [4 ]
Kashif, Syed Muhammad [3 ]
Sain, Amyra Amat [5 ]
Adenan, Mohd Ilham [1 ,5 ,6 ]
Anouar, El Hassane [1 ]
Ali, Muhammad [7 ]
Rahim, Fazal [9 ]
Khan, Khalid M. [8 ]
机构
[1] Univ Teknol MARA UiTM, Atta Ur Rahman Inst Nat Prod Discovery, Puncak Alam 42300, Selangor, Malaysia
[2] Univ Teknol MARA, Fac Sci Appl, Shah Alam 40450, Selangor, Malaysia
[3] Univ Sindh Jamshoro, Inst Adv Res Studies Chem Sci, Jamshoro, Pakistan
[4] Univ Teknol MARA, Fac Pharm, Puncak Alam 42300, Selangor, Malaysia
[5] Malaysian Inst Pharmaceut & Nutraceut, Minist Sci Technol & Innovat Bangunan Pentadbiran, Bayan Lepas 11700, Penang, Malaysia
[6] Forest Res Inst Malaysia, Kepong 52109, Selangor, Malaysia
[7] COMSATS Inst Informat Technol, Ctr Adv Drug Res, Abbottabad 22060, KPK, Pakistan
[8] Univ Karachi, Int Ctr Chem & Biol Sci, HEJ Res Inst Chem, Karachi 75270, Pakistan
[9] Hamra Univ, Dept Chem, Mansehra, Pakistan
关键词
Benzimidazole; Antiglycation; Antioxidant; Antileishmanial; Stereoisomers; SCHIFF-BASES; GLYCATION; HYDRAZONE; PRODUCTS;
D O I
10.1016/j.ejmech.2014.07.078
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
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 mu M, better than standard drug rutin (294.46 +/- 1.50 mu M). Compound 1-28 were also evaluated for DPPH activities. Compounds 1-8 showed excellent activities, ranging 12-29 mu M, better than standard drug n-propylgallate (IC50 = 30.30 +/- 0.40 mu M). For superoxide anion scavenging activity, compounds 1-7 showed better activity than standard n-propylgallate (IC50 = 106.34 +/- 1.6 mu M), ranged 82-104 mu M. These compounds were found to be nontoxic to THP-1 cells. (C) 2014 Elsevier Masson SAS. All rights reserved.
引用
收藏
页码:731 / 738
页数:8
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