Sulfa Drugs as Inhibitors of Carbonic Anhydrase: New Targets for the Old Drugs

被引：20

作者：

al-Rashida, Mariya ^{[1
]}

Hussain, Sajad ^{[1
]}

Hamayoun, Mehwish ^{[2
]}

Altaf, Aisha ^{[2
]}

Iqbal, Jamshed ^{[2
]}

机构：

[1] Chartered Univ, Forman Christian Coll, Dept Chem, Lahore 54600, Pakistan

[2] COMSATS Inst Informat Technol, Ctr Adv Drug Res, Abbottabad 22060, Pakistan

来源：

BIOMED RESEARCH INTERNATIONAL | 2014年 / 2014卷

关键词：

INCORPORATING 1,3,5-TRIAZINE MOIETIES; ISOZYME-II; SULFONAMIDES; IX; DESIGN; DERIVATIVES; EXPRESSION; TRANSPORT;

D O I：

10.1155/2014/162928

中图分类号：

Q81 [生物工程学（生物技术）]; Q93 [微生物学];

学科分类号：

071005 ; 0836 ; 090102 ; 100705 ;

摘要：

Sulfa drugs are well-known antibacterial agents containing N-substituted sulfonamide group on para position of aniline ring (NH2 RSO2 NHR'). In this study 2,4-dichloro-1,3,5-triazine derivatives of sulfa drugs, sulfamerazine (1b), sulfaquinoxaline (2b), sulfadiazine (3b), sulfadimidine (4b), and sulfachloropyrazine (5b) (1a-5a) were synthesized and characterized. Their carbonic anhydrase inhibition activity was evaluated against bovine cytosolic carbonic anhydrase isozyme II (bCA II). For the sake of comparison the CA inhibition activity of the parent sulfa drugs (1b-5b) was also evaluated. A significant increase in CA inhibition activity of sulfa drugs was observed upon substitution with 2,4-dichloro-1,3,5-triazine moiety. Molecular docking studies were carried out to highlight binding site interactions. ADME properties were calculated to evaluate drug likeness of the compounds.

引用

页数：10

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