Naftaleniloksipropanol türevi bazı bileşiklerin çok ilaca dirençli bakterilere karşı in vitro etkinliklerinin incelenmesi

Yıl 2017, Cilt: 21 Sayı: 3, 395 - 402, 01.06.2017

Hayriye Genç , Oğuz Karabay , Mustafa Zengin

https://doi.org/10.16984/saufenbilder.296820

Öz

 Çoklu ilaca dirençli bakterilerin tedavisi bütün
dünya için ciddi bir problem teşkil etmekte ve yeni antibakteriyellere olan
ihtiyaç gün geçtikçe artmaktadır. Bu çalışmada, α-Naftol bileşiğinden oksipropanolamin türevleri sentezlenmiş ve ÇİD (çoklu
ilaca dirençli) bakterilere karşı aktiviteleri değerlendirilmiştir. Gram-pozitif
bakterilerden Staphylococcus aureus
ve Gram-negatif bakterilerden A.
baumannii, P. aeruginosa, E. coli suşları kullanılmıştır. Çalışmada
kullanılan 2a-d bileşiklerinin sentezi için ilk olarak α-naftol ile epiklorohidrin
reaksiyona sokularak 2-((naftelen-1-iloksi)metil)oksiran (1) bileşiği elde
edilmiş ve ardından dört değişik amin türevi ile reaksiyona sokularak 2a-d
türevleri elde edilmiştir. Bu bileşiklerin ÇİD bakterilere karşı in vitro etkinlikleri Kirby-Bauer metodu
ile CLSI standartlarına göre belirlenmiştir. Elde edilen bileşiklerden 2a, 2b
ve 2c her bir bakteri türüne karşı test edilen diğer antibakteriyellerden daha
fazla antibakteriyel etkiye sahipken, 2d bileşiği Gram-negatif bakterilere
karşı ortalama veya altında bir etkinlik göstermiş, Gram-pozitif bakteri olan S. aureus’ a karşı yüksek bir etkinlik
sergilemiştir.

Anahtar Kelimeler

Naftol, Oksipropanolamin, Antibakteriyel, İlaç Direnci, Çoklu ilaç direnci

Examination of in vitro activities of some naphthalenyloxypropanol derivatives against multi-drug resistant bacteria

Öz

Treatment
of multi-drug resistant bacteria is a growing problem for the whole World and
the need for new antibacterial drug is increasing day by day. Herein,
oxipropanolamine derivatives from α-naphthol compound were synthesized and the
activities against MDR (multi-drug resistant) bacteria were evaluated. Strains of S.
aureus which is one of Gram-positive bacteria and A. baumannii, P. aeruginosa, E. coli which are of  Gram-negative bacteria were used.The tested
bacteria are Gram-pozitif stain of S.
aureus and Gram-negatif stains of A.
baumannii, P. aeruginosa, E. coli. For the synthesis of compounds 2a-d
which were used in the study, firstly   2-((naphthalen-1-yloxy)methyl)
oxirane was obtained with the reaction of α-naphthol with epichlorohydrin and then reacted with four
diffrent amine groups to obtain 2a-d derivatives. in vitro activities of these compounds against MDR bacteria were
determined by the Kirby-Bauer method according to CLSI standards. While the
obtained compounds 2a, 2b and 2c have more antibacterial activity than other
tested antibacterials, the compound 2d has shown moderate or blow antibacterial
activity against Gram-negative bacteria, but has a high activity against
gram-positive bacteria S. aureus.

Anahtar Kelimeler

Naphthol, Oxipropanolamine, Antibacterial, Drug Resistance, Multidrug Resistance

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