Synthesis and antimicrobial activities of His(2-aryl)Arg and Trp-His(2-aryl) classes of dipeptidomimetics

被引：26

作者：

Mahindra, Amit ^{[1
]}

Sharma, Krishna K. ^{[1
]}

Rathore, Dinesh ^{[1
]}

Khan, Shabana. I. ^{[2
]}

Jacob, Melissa R. ^{[2
]}

Jain, Rahul ^{[1
]}

机构：

[1] Natl Inst Pharmaceut Educ & Res, Dept Med Chem, Sas Nagar 160062, Punjab, India

[2] Univ Mississippi, Sch Pharm, Natl Ctr Nat Prod Res, University, MS 38677 USA

来源：

MEDCHEMCOMM | 2014年 / 5卷 / 05期

关键词：

CRYPTOCOCCAL MENINGITIS; ANTIFUNGAL AGENTS; FUNGAL-INFECTIONS; PEPTIDE-SYNTHESIS; AMPHOTERICIN-B; ECHINOCANDINS; BURDEN; YEASTS; ACIDS;

D O I：

10.1039/c4md00041b

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 communication, we report the design, synthesis and in vitro antimicrobial activity of ultra short peptidomimetics. Besides producing promising antibacterial activities against Staphylococcus aureus and methicillin-resistant S. aureus (MRSA), the dipeptidomimetics exhibited high antifungal activity against C. neoformans with IC50 values in the range of 0.16-19 mu g mL(-1). The most potent analogs exhibited 4-fold higher activity than the currently used drug amphotericin B, with no apparent cytotoxicity in a panel of mammalian cell lines.

引用

页码：671 / 676

页数：6

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