Synthesis and Antimicrobial Studies of Coumarin-Substituted Pyrazole Derivatives as Potent Anti-Staphylococcus aureusAgents

被引：43

作者：

Alnufaie, Rawan ^{[1
]}

Raj KC, Hansa ^{[1
]}

Alsup, Nickolas ^{[1
]}

Whitt, Jedidiah ^{[1
]}

Andrew Chambers, Steven ^{[1
]}

Gilmore, David ^{[2
]}

Alam, Mohammad A. ^{[1
]}

机构：

[1] Arkansas State Univ, Coll Sci & Math, Dept Chem & Phys, Jonesboro, AR 72467 USA

[2] Arkansas State Univ, Coll Sci & Math, Dept Biol Sci, Jonesboro, AR 72467 USA

来源：

MOLECULES | 2020年 / 25卷 / 12期

基金：

美国国家卫生研究院;

关键词：

pyrazole; coumarin; antimicrobial; hydrazone; biofilm; Staphylococcus aureus; S; epidermidis; MRSA; ACID;

D O I：

10.3390/molecules25122758

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

In this paper, synthesis and antimicrobial studies of 31 novel coumarin-substituted pyrazole derivatives are reported. Some of these compounds have shown potent activity against methicillin-resistantStaphylococcus aureus(MRSA) with minimum inhibitory concentration (MIC) as low as 3.125 mu g/mL. These molecules are equally potent at inhibiting the development of MRSA biofilm and the destruction of preformed biofilm. These results are very significant as MRSA strains have emerged as one of the most menacing pathogens of humans and this bacterium is bypassing HIV in terms of fatality rate.

引用

页数：16

共 17 条

[1] Pyrazole derived ultra-short antimicrobial peptidomimetics with potent anti-biofilm activity [J].

Ahn, Mija ;

Gunasekaran, Pethaiah ;

Rajasekaran, Ganesan ;

Kim, Eun Young ;

Lee, Soo-Jae ;

Bang, Geul ;

Cho, Kun ;

Hyun, Jae-Kyung ;

Lee, Hyun-Ju ;

Jeon, Young Ho ;

Kim, Nam-Hyung ;

Ryu, Eun Kyoung ;

Shin, Song Yub ;

Bang, Jeong Kyu .

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 2017, 125 :551-564

[2]

Alam MA, 2020, [No title captured], Patent No. [US10596153B2, 10596153]

[3] Synthesis, anti-inflammatory, analgesic, COX1/2-inhibitory activity, and molecular docking studies of hybrid pyrazole analogues [J].

Alam, Md Jahangir ;

Alam, Ozair ;

Khan, Suroor Ahmad ;

Naim, Mohd Javed ;

Islamuddin, Mohammad ;

Deora, Girdhar Singh .

DRUG DESIGN DEVELOPMENT AND THERAPY, 2016, 10 :3529-3543

[4] Synthesis and antimicrobial studies of novel derivatives of 4-(4-formy1-3-phenyl-1H-pyrazol-1-yl)benzoic acid as potent anti-Acinetobacter baumannii agents [J].

Allison, Devin ;

Delancey, Evan ;

Ramey, Hunter ;

Williams, Conrad ;

Alsharif, Zakeyah Ali ;

Al-Khattabi, Hessa ;

Ontko, Allyn ;

Gilmore, David ;

Alam, Mohammad A. .

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2017, 27 (03) :387-392

[5] Advances in Synthesis and Potentially Bioactive of Coumarin Derivatives [J].

Anamika ;

Utreja, Divya ;

Ekta ;

Jain, Nisha ;

Sharma, Shivali .

CURRENT ORGANIC CHEMISTRY, 2018, 22 (26) :2509-2536

[6]

[Anonymous], 2019, New report calls for urgent action to avert antimicrobial resistance crisis

[7] Synthesis and antimicrobial studies of azomethine and N-arylamine derivatives of 4-(4-formyl-3-phenyl-1H-pyrazol-1-yl)benzoic acid as potent anti-methicillin-resistant Staphylococcus aureus agents [J].

Brider, Jamarcus ;

Rowe, Trent ;

Gibler, Danielle Jamie ;

Gottsponer, Adam ;

Delancey, Evan ;

Branscum, Michael Drew ;

Ontko, Allyn ;

Gilmore, David ;

Alam, Mohammad A. .

MEDICINAL CHEMISTRY RESEARCH, 2016, 25 (11) :2691-2697

[8]

CDC, ANT ANT RES AR AMR

[9] Methicillin-resistant Staphylococcus aureus (MRSA): antibiotic-resistance and the biofilm phenotype [J].

Craft, Kelly M. ;

Nguyen, Johny M. ;

Berg, Lawrence J. ;

Townsend, Steven D. .

MEDCHEMCOMM, 2019, 10 (08) :1231-1241

[10] Metabolism and Bioactivation: It's Time to Expect the Unexpected Miniperspective [J].

Driscoll, James P. ;

Sadlowski, Corinne M. ;

Shah, Nina R. ;

Feula, Antonio .

JOURNAL OF MEDICINAL CHEMISTRY, 2020, 63 (12) :6303-6314

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