Synthesis, and prediction of molecular properties and antimicrobial activity of some acylhydrazones derived from NNN-(arylsulfonyl)methionine

ESRA TATAR; SEVİL ŞENKARDEŞ; HASAN ERDİNÇ SELLİTEPE; ŞÜKRİYE GÜNİZ KÜÇÜKGÜZEL; ŞENGÜL ALPAY KARAOĞLU; ARİF BOZDEVECİ; ERIK DE CLERCQ; CHRISTOPHE PANNECOUQUE; TAİBİ BEN HADDA; İLKAY KÜÇÜKGÜZEL

Makale detayları

Synthesis, and prediction of molecular properties and antimicrobial activity of some acylhydrazones derived from NNN-(arylsulfonyl)methionine

Yazarlar:

ESRA TATAR | SEVİL ŞENKARDEŞ | HASAN ERDİNÇ SELLİTEPE | ŞÜKRİYE GÜNİZ KÜÇÜKGÜZEL | ŞENGÜL ALPAY KARAOĞLU | ARİF BOZDEVECİ | ERIK DE CLERCQ | CHRISTOPHE PANNECOUQUE | TAİBİ BEN HADDA | İLKAY KÜÇÜKGÜZEL

Yayıncı:

TUBITAK

Dergi:

Turkish Journal of Chemistry 2016 Vol.40 Issue 3, pp.510-534

Belge Tipi:

Makale

Yayın Tarihi:

5/2016

Belge Dili:

Türkçe

Document ID (Org No.):

2000726631

Sıklık:

İki Aylık

eISSN:

1303-6130

pISSN:

1300-0527

Özet:

 

A series of 38 new acylhydrazones   [3-40], derived from   (2S)S)S)-4-(methylsulfanyl)-2-[[(4-methylphenyl)sulfonyl] amino]butanoic acid   hydrazide [2], were synthesized and evaluated for their anti-HIV   and antimicrobial activity with the further aim to develop acylhydrazones   carrying an amino acid side chain. All tested compounds possess stronger   activity against gram (+) bacteria. Compound 23 was found active   against methicillin-resistant Staphylococcus aureus (MRSA) with a MIC value of 3.9 μμ\mu g/mL.   The MIC value of compound 30 against Enterococcus faecalis, Listeria monocytogenes, and Bacillus cereus was 8 μμ\mu g/mL. A computational study for prediction of ADME and drug-like properties   (solubility, drug-likeness, and drug score) as well as potential toxicity   profiles of compounds 2-40 was performed using the   Molinspiration online property calculation toolkit and Osiris Property   Explorer. As most of our compounds meet Lipinski's rule of five, they   promise good solubility and permeability. According to Osiris calculations,   the majority of our compounds are supposed to be nonmutagenic and   nonirritating.

Makale detayları

Synthesis, and prediction of molecular properties and antimicrobial activity of some acylhydrazones derived from NNN-(arylsulfonyl)methionine

Yazarlar: ESRA TATAR | SEVİL ŞENKARDEŞ | HASAN ERDİNÇ SELLİTEPE | ŞÜKRİYE GÜNİZ KÜÇÜKGÜZEL | ŞENGÜL ALPAY KARAOĞLU | ARİF BOZDEVECİ | ERIK DE CLERCQ | CHRISTOPHE PANNECOUQUE | TAİBİ BEN HADDA | İLKAY KÜÇÜKGÜZEL

Yayıncı: TUBITAK

Dergi: Turkish Journal of Chemistry 2016 Vol.40 Issue 3, pp.510-534

Belge Tipi: Makale

Yayın Tarihi: 5/2016

Belge Dili: Türkçe

Document ID (Org No.): 2000726631

Sıklık: İki Aylık

eISSN: 1303-6130

pISSN: 1300-0527

Sayı

Yazarlar:

ESRA TATAR | SEVİL ŞENKARDEŞ | HASAN ERDİNÇ SELLİTEPE | ŞÜKRİYE GÜNİZ KÜÇÜKGÜZEL | ŞENGÜL ALPAY KARAOĞLU | ARİF BOZDEVECİ | ERIK DE CLERCQ | CHRISTOPHE PANNECOUQUE | TAİBİ BEN HADDA | İLKAY KÜÇÜKGÜZEL

Yayıncı:

TUBITAK

Dergi:

Turkish Journal of Chemistry 2016 Vol.40 Issue 3, pp.510-534

Belge Tipi:

Makale

Yayın Tarihi:

5/2016

Belge Dili:

Türkçe

Document ID (Org No.):

2000726631

Sıklık:

İki Aylık

eISSN:

1303-6130

pISSN:

1300-0527