Synthesis, molecular docking and antibacterial evaluation of various quinoline schiff bases: labeling and biodistribution of 99mTc-2-(p-hydroxybenzylidene)-1-(quinolin-4-yl)hydrazine

被引：6

作者：

Al-wabli, Reem I. ^{[1
]}

Khedr, Mohammed A. ^{[2
,3
]}

Kadi, Adnan A. ^{[1
]}

Motaleb, Mohammed A. ^{[4
]}

Al-rashood, Khalid A. ^{[1
]}

Zaghary, Wafaa A. ^{[1
,3
]}

机构：

[1] King Saud Univ, Dept Pharmaceut Chem, Coll Pharm, Riyadh 11451, Saudi Arabia

[2] King Faisal Univ, Dept Pharmaceut Sci, Coll Clin Pharm, Al Hasa, Saudi Arabia

[3] Helwan Univ, Dept Pharmaceut Chem, Coll Pharm, Cairo 11795, Egypt

[4] Atom Energy Author, Labeled Compound Dept, Hot Labs Ctr, Cairo 13759, Egypt

来源：

MEDICINAL CHEMISTRY RESEARCH | 2014年 / 23卷 / 09期

关键词：

Quinoline; Benzylidene; Molecular docking; Antimicrobial activity; Technetium-99m; BIOLOGICAL CHARACTERISTICS; SCINTIGRAPHIC DETECTION; ANTIMICROBIAL PEPTIDES; BACTERIAL-INFECTION; DETECTING SITES; INFLAMMATION; AGENT; DIAGNOSIS; COMPLEX;

D O I：

10.1007/s00044-014-0977-1

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A new series of 2-(substituted benzylidene)-1-(quinoline-4-yl)hydrazine was designed, synthesized, and evaluated for their antimicrobial activity. A molecular docking study was performed against bacterial topoisomerase II (PDB code: 2XCT) using MOE 2012.10 and Leadit 2.1.2 softwares. Compound 4a with the highest antibacterial activity was labeled with one of the most important radioactive isotopes (technetium-99m). (99m) Tc-4a complex showed high labeling yield, stability, and uptake in the inflamed tissue (T/NT = 6.11 +/- A 0.5) compared to the commercially available Tc-99m-ciprofloxacin (T/NT = 3.6 +/- A 0.4).

引用

页码：4011 / 4020

页数：10

共 34 条

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