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Journals / Turkish Journal of Chemistry / 2016 / Cilt: 40 - Sayı: 3

Synthesis, and prediction of molecular properties and antimicrobial activity ofsome acylhydrazones derived fromN-(arylsulfonyl)methionine

Esra TATAR
Hasan Erdinç SELLİTEPE
Şengül Alpay KARAOĞLU
Arif BOZDEVECİ
Christophe PANNECOUQUE
Taibi BEN HADDA
Sevil ŞENKARDES
Sükriye Güniz KÜÇÜKGÜZEL
İlkay KÜÇÜKGÜZEL
Erik DE CLERCQ
Pages
510–534
Publication Date
2022-11-05
DOI
—
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AI Summary & Key Takeaways

AI Insight
⚡ TL;DR(Too Long; Didn't Read)

According to Osiris calculations,the majority of our compounds are supposed to be nonmutagenic and nonirritating.

📌 3 Key Takeaways

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Objective & Hypothesis:A series of 38 new acylhydrazones [3{40], derived from (2S)-4-(methylsulfanyl)-2-[[(4-methylphenyl)sulfonyl]amino]butanoic acid hydrazide [2], were synthesized and evaluated for their anti-HIV and antimicrobial activity withthe further aim to develop acylhydrazones carrying an amino acid side chain.
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Key Findings & Data:Compound23was found active against methicillin-resistantStaphylococcus aureus(MRSA) with a MIC value of 3.9 g/mL.
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Conclusion & Impact:According to Osiris calculations,the majority of our compounds are supposed to be nonmutagenic and nonirritating.
🔬Design:Research Article
📍Scope:Comprehensive Sample
⚙️Variables:Domain Parameters

Abstract

A series of 38 new acylhydrazones [3{40], derived from (2S)-4-(methylsulfanyl)-2-[[(4-methylphenyl)sulfonyl]amino]butanoic acid hydrazide [2], were synthesized and evaluated for their anti-HIV and antimicrobial activity withthe further aim to develop acylhydrazones carrying an amino acid side chain. All tested compounds possess strongeractivity against gram (+) bacteria. Compound23was found active against methicillin-resistantStaphylococcus aureus(MRSA) with a MIC value of 3.9 g/mL. The MIC value of compound30againstEnterococcus faecalis,Listeriamonocytogenes, andBacillus cereuswas 8 g/mL. A computational study for prediction of ADME and drug-likeproperties (solubility, drug-likeness, and drug score) as well as potential toxicity pro les of compounds2{40wasperformed using the Molinspiration online property calculation toolkit and Osiris Property Explorer. As most of ourcompounds meet Lipinski's rule of ve, they promise good solubility and permeability. According to Osiris calculations,the majority of our compounds are supposed to be nonmutagenic and nonirritating.

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Cite This Article

TATAR, E., SELLİTEPE, H. E., KARAOĞLU, Ş. A., BOZDEVECİ, A., PANNECOUQUE, C., HADDA, T. B., ŞENKARDES, S., KÜÇÜKGÜZEL, S. G., KÜÇÜKGÜZEL, İ., CLERCQ, E. D. (2022). Synthesis, and prediction of molecular properties and antimicrobial activity ofsome acylhydrazones derived fromN-(arylsulfonyl)methionine. Turkish Journal of Chemistry, Cilt: 40 - Sayı: 3, 510–534. https://ajindex.com/articles/602008

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References (1)

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