Synthesis and In-Vitro Antimicrobial Activity of Novel Aminophosphinic Acids Containing Cyclobutane and 1,3-Thiazole

Koparır, Pelin; Karaarslan, Muhsin; Örek, Cahit; Koparır, Metin

doi:10.1080/10426507.2011.604660

Cited by 22 publications

(6 citation statements)

References 13 publications

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“…In 2011, Koparir et al reported aminophosphinic acids 223a-l containing cyclobutane and 1,3-thiazole rings with antibacterial properties (Scheme 42) [145]. Their preparation consisted of a condensation, mediated by hydrochloric acid, of aryl aldehyde derivatives with hypophosphorous acid and 2-amino-thiazoles 222a-c incorporating a substituted cyclobutyl group in position 4.…”

Section: Cyclobutyl-13-thiazolyl Phosphinic Acidsmentioning

confidence: 98%

Synthesis and Biological Applications of Phosphinates and Derivatives

Virieux

Volle

Bakalara

et al. 2014

Topics in Current Chemistry

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This review first outlines general considerations on phosphinic acids and derivatives as bioisosteric groups. The next sections present key aspects of phosphinic acid-based molecules and include a brief description of the biological pathways involved for their activities. The synthetic aspects and the biological activities of such compounds reported in the literature between 2008 and 2013 are also described.

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Section: Cyclobutyl-13-thiazolyl Phosphinic Acidsmentioning

confidence: 98%

Synthesis and Biological Applications of Phosphinates and Derivatives

Virieux

Volle

Bakalara

et al. 2014

Topics in Current Chemistry

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“…Schiff bases 3a--i were prepared following the published procedure 22 aminophosphinic acids 4a--h was performed following Baylis et al 26 Reactions were carried out in boiling ethanol for 24 h, after which mixtures were left overnight to stir at room temperature ( Figure 1). …”

Section: Chemistrymentioning

confidence: 99%

“…20,21 Over the past several years, our laboratories have reported the synthesis of 1-amino-Hphosphinic acids. 22,23 We have reported the synthesis and in vitro antimicrobial activity of novel aminophosphinic acids containing cyclobutane and 1.3-thiazole. Building on previous studies, we have prepared a series of derivatives of new α-aminophosphinic acids ( Figure 1).…”

Section: Introductionmentioning

confidence: 99%

Synthesis and in vitro antioxidant evaluation of new bis(α-aminoalkyl)phosphinic acid derivatives

Sarac

Örek

Çetin

et al. 2016

Phosphorus, Sulfur, and Silicon and the Related Elements

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Diamines were added to arylaldehydes in ethanol, which resulted in corresponding diimines.Novel bis-1-aminophosphinic acid compounds were synthesized through the interaction of diimines and hypophosphorous acid. The new compounds were characterized by elemental analyses, FT-IR and 1 H, 13 C and 31 P NMR techniques. The in vitro antioxidant activity of the newly synthesized compounds were measured and found to exhibit significantly higher antioxidant activity than the standard.

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“…It has always been a challenge to discover and elect highly specific and potent inhibitors for proteases. As phosphinic group (‐PO 2 ‐CH 2 ‐) is mimicking the high energy tetrahedral transition phase of peptide hydrolysis, psuedophosphinic peptides are increasingly studied as inhibitors for proteolytic enzymes …”

Section: Introductionmentioning

confidence: 99%

Investigation of acetylcholinesterase and mammalian DNA topoisomerases, carbonic anhydrase inhibition profiles, and cytotoxic activity of novel bis(α‐aminoalkyl)phosphinic acid derivatives against human breast cancer

Daştan

Koçyiğit

Daştan

et al. 2017

J Biochem & Molecular Tox

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The aim of this study was to evaluate biologically active novel molecules having potentials to be drugs by their antitumor properties and by activities of apoptotic caspase and topoisomerase. Following syntheses of novel eight bis(α-aminoalkyl)phosphinic acid derivatives (4a-h) as a result of array of reactions, compounds were evaluated by cytotoxic effects in vitro on human breast cancer (MCF-7) and normal endothelial (HUVEC) cell lines. All phosphinic acid derivatives were effective for cytotoxicity on both MCF-7 and HUVEC lines, while 4c, 4e, and 4f compounds were found significantly more effective. For the evaluation of antitumor properties of compounds in a highly sensitive method, their effects on inhibiting topoisomerases I and II were investigated. Also, some of the bis(α-aminoalkyl)phosphinic acid derivatives (4a, 4e-h) showed nice inhibitory action against acetylcholinesterase and human carbonic anhydrase isoforms I and II.

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Synthesis and In-Vitro Antimicrobial Activity of Novel Aminophosphinic Acids Containing Cyclobutane and 1,3-Thiazole

Cited by 22 publications

References 13 publications

Synthesis and Biological Applications of Phosphinates and Derivatives

Synthesis and Biological Applications of Phosphinates and Derivatives

Synthesis and in vitro antioxidant evaluation of new bis(α-aminoalkyl)phosphinic acid derivatives

Investigation of acetylcholinesterase and mammalian DNA topoisomerases, carbonic anhydrase inhibition profiles, and cytotoxic activity of novel bis(α‐aminoalkyl)phosphinic acid derivatives against human breast cancer

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