2-Nitrofuran

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Alireza Foroumadi - One of the best experts on this subject based on the ideXlab platform.

  • synthesis and leishmanicidal activity of 1 5 5 nitrofuran 2 yl 1 3 4 thiadiazole 2 yl 4 benzoylepiperazines
    Iranian Journal of Pharmaceutical Research, 2017
    Co-Authors: Alireza Foroumadi, Sussan Kabudanian Ardestani, Hadi Adibi, Samira Shirooie, Arezoo Bozorgomid, Ali Jafari
    Abstract:

    A series of (5-nitrofuran-2-yl)-1, 3, 4-thiadiazole-2-yl derivatives 6a–6e have been synthesized and screened for in vitro anti-leishmanial activity against the promastigote form of L. major. The structure of Schiff bases were confirmed by 1H NMR, IR. Screening results indicate that all of the designed and synthesized final compounds (6a-6e) significantly reduced the viability of promastigotes of L. major in comparison to glucantime (IC50 3× 103 μg/ml). Meta and Para substitutions in benzene ring containing compounds were more potent than other derivative and the most potent compounds were 6d, 6e with IC50 value 94 µM and 77.6 µM, respectively. The experimental data proposes that (5-nitrofuran-2-yl)-1, 3, 4-thiadiazole-2-yl derivatives may be further investigated as a candidate drug for treatment of cutaneous leishmaniasis.

  • synthesis and anti leishmanial activity of 5 5 nitrofuran 2 yl 1 3 4 thiadiazol 2 amines containing n 1 benzyl 1h 1 2 3 triazol 4 yl methyl moieties
    European Journal of Medicinal Chemistry, 2012
    Co-Authors: Azar Tahghighi, Sepideh Razmi, Sussan Kabudanian Ardestani, Abbas Shafiee, Saeed Emami, Farzad Kobarfard, Siavoush Dastmalchi, Mohammad Mahdavi, Parham Foroumadi, Alireza Foroumadi
    Abstract:

    Abstract A novel series of 5-(5-nitrofuran-2-yl)-1,3,4-thiadiazol-2-amines were synthesized by introducing N -[(1-benzyl-1 H -1,2,3-triazol-4-yl)methyl] moiety as a new functionality on the C-2 amine of thiadiazole ring via click chemistry. The title compounds namely, N -[(1-benzyl-1 H -1,2,3-triazol-4-yl)methyl]-5-(5-nitrofuran-2-yl)-1,3,4-thiadiazol-2-amines ( 3a – n ) were characterized by IR, NMR and MS spectra. These compounds were evaluated for their in vitro anti-leishmanial activity against promostigote form of the Leishmania major . Most compounds exhibited good anti-leishmanial activity against the promastigote form of L. major . The most active compound against promostigotes was found to be 4-methylbenzyl analog 3i , which significantly decreases the number of intracellular amastigotes per macrophage, percentage of macrophage infectivity and infectivity index.

  • synthesis and antileishmanial activity of novel 5 5 nitrofuran 2 y1 1 3 4 thiadiazoles with piperazinyl linked benzamidine substituents
    European Journal of Medicinal Chemistry, 2011
    Co-Authors: Azar Tahghighi, Sepideh Razmi, Javid Shahbazi Mojarrad, Sussan Kabudanian Ardestani, Abbas Shafiee, Saeed Emami, Farzane Rezazade Marznaki, Farzad Kobarfard, Siavoush Dastmalchi, Alireza Foroumadi
    Abstract:

    In order to optimize the antileishmanial activity of piperazinyl-linked 5-(5-nitrofuran-2-yl)-1,3,4-thiadiazoles, we synthesized a series of 5-(5-nitrofuran-2-y1)-1,3,4-thiadiazoles with piperazinyl-linked benzamidine substituent as scaffold found in pentamidine related antiprotozoals. The structure of target compounds was confirmed by IR, 1H NMR, 13C NMR and Mass spectral data. All compounds were tested for in vitro activity against the promastigote and amastigote forms of Leishmania major. From the results, we found that the substitution on amidine nitrogen has profound role in the biological activity of these compounds. The 5-nitrofuran-2-yl-1,3,4-thiadiazoles having n-propyl, n-butyl and benzyl side chain on benzamidine (as in compounds 2d, 2e and 2g, respectively) showed very good activity in both forms of promastigote and amastigote. The most active compound was N-propyl-4-(4-(5-(5-nitrofuran-2-yl)-1,3,4-thiadiazol-2-yl)piperazin-1-yl) benzamidine hydrochloride (2d) with IC50 value of 0.08 μM in promastigote model. This compound showed a very low level of toxicity against macrophages (CC50=785 μM), with the highest selectivity index (SI=78.5) among the tested compounds.

  • synthesis and in vitro anti leishmanial activity of 1 5 5 nitrofuran 2 yl 1 3 4 thiadiazol 2 yl and 1 5 5 nitrothiophen 2 yl 1 3 4 thiadiazol 2 yl 4 aroylpiperazines
    Bioorganic & Medicinal Chemistry, 2008
    Co-Authors: Mina Behrouzifardmoghadam, Fatemeh Poorrajab, Sussan Kabudanian Ardestani, Abbas Shafiee, Saeed Emami, Alireza Foroumadi
    Abstract:

    The synthesis and anti-leishmanial activity of nitroheteroaryl-1,3,4-thiadiazole-based compounds including 1-[5-(5-nitrofuran-2-yl)-1,3,4-thiadiazol-2-yl]-4-aroylpiperazines and 1-[5-(5-nitrothiophen-2-yl)-1,3,4-thiadiazol-2-yl]-4-aroylpiperazines were described. Most of the synthesized compounds exhibited potent anti-leishmanial activity against both promastigote and amastigote forms of Leishmania major at non-cytotoxic concentrations. In general, 5-nitrofuran derivatives were more active than the corresponding 5-nitrothiophene analogues.

Sussan Kabudanian Ardestani - One of the best experts on this subject based on the ideXlab platform.

  • synthesis and leishmanicidal activity of 1 5 5 nitrofuran 2 yl 1 3 4 thiadiazole 2 yl 4 benzoylepiperazines
    Iranian Journal of Pharmaceutical Research, 2017
    Co-Authors: Alireza Foroumadi, Sussan Kabudanian Ardestani, Hadi Adibi, Samira Shirooie, Arezoo Bozorgomid, Ali Jafari
    Abstract:

    A series of (5-nitrofuran-2-yl)-1, 3, 4-thiadiazole-2-yl derivatives 6a–6e have been synthesized and screened for in vitro anti-leishmanial activity against the promastigote form of L. major. The structure of Schiff bases were confirmed by 1H NMR, IR. Screening results indicate that all of the designed and synthesized final compounds (6a-6e) significantly reduced the viability of promastigotes of L. major in comparison to glucantime (IC50 3× 103 μg/ml). Meta and Para substitutions in benzene ring containing compounds were more potent than other derivative and the most potent compounds were 6d, 6e with IC50 value 94 µM and 77.6 µM, respectively. The experimental data proposes that (5-nitrofuran-2-yl)-1, 3, 4-thiadiazole-2-yl derivatives may be further investigated as a candidate drug for treatment of cutaneous leishmaniasis.

  • synthesis and anti leishmanial activity of 5 5 nitrofuran 2 yl 1 3 4 thiadiazol 2 amines containing n 1 benzyl 1h 1 2 3 triazol 4 yl methyl moieties
    European Journal of Medicinal Chemistry, 2012
    Co-Authors: Azar Tahghighi, Sepideh Razmi, Sussan Kabudanian Ardestani, Abbas Shafiee, Saeed Emami, Farzad Kobarfard, Siavoush Dastmalchi, Mohammad Mahdavi, Parham Foroumadi, Alireza Foroumadi
    Abstract:

    Abstract A novel series of 5-(5-nitrofuran-2-yl)-1,3,4-thiadiazol-2-amines were synthesized by introducing N -[(1-benzyl-1 H -1,2,3-triazol-4-yl)methyl] moiety as a new functionality on the C-2 amine of thiadiazole ring via click chemistry. The title compounds namely, N -[(1-benzyl-1 H -1,2,3-triazol-4-yl)methyl]-5-(5-nitrofuran-2-yl)-1,3,4-thiadiazol-2-amines ( 3a – n ) were characterized by IR, NMR and MS spectra. These compounds were evaluated for their in vitro anti-leishmanial activity against promostigote form of the Leishmania major . Most compounds exhibited good anti-leishmanial activity against the promastigote form of L. major . The most active compound against promostigotes was found to be 4-methylbenzyl analog 3i , which significantly decreases the number of intracellular amastigotes per macrophage, percentage of macrophage infectivity and infectivity index.

  • synthesis and antileishmanial activity of novel 5 5 nitrofuran 2 y1 1 3 4 thiadiazoles with piperazinyl linked benzamidine substituents
    European Journal of Medicinal Chemistry, 2011
    Co-Authors: Azar Tahghighi, Sepideh Razmi, Javid Shahbazi Mojarrad, Sussan Kabudanian Ardestani, Abbas Shafiee, Saeed Emami, Farzane Rezazade Marznaki, Farzad Kobarfard, Siavoush Dastmalchi, Alireza Foroumadi
    Abstract:

    In order to optimize the antileishmanial activity of piperazinyl-linked 5-(5-nitrofuran-2-yl)-1,3,4-thiadiazoles, we synthesized a series of 5-(5-nitrofuran-2-y1)-1,3,4-thiadiazoles with piperazinyl-linked benzamidine substituent as scaffold found in pentamidine related antiprotozoals. The structure of target compounds was confirmed by IR, 1H NMR, 13C NMR and Mass spectral data. All compounds were tested for in vitro activity against the promastigote and amastigote forms of Leishmania major. From the results, we found that the substitution on amidine nitrogen has profound role in the biological activity of these compounds. The 5-nitrofuran-2-yl-1,3,4-thiadiazoles having n-propyl, n-butyl and benzyl side chain on benzamidine (as in compounds 2d, 2e and 2g, respectively) showed very good activity in both forms of promastigote and amastigote. The most active compound was N-propyl-4-(4-(5-(5-nitrofuran-2-yl)-1,3,4-thiadiazol-2-yl)piperazin-1-yl) benzamidine hydrochloride (2d) with IC50 value of 0.08 μM in promastigote model. This compound showed a very low level of toxicity against macrophages (CC50=785 μM), with the highest selectivity index (SI=78.5) among the tested compounds.

  • synthesis and in vitro anti leishmanial activity of 1 5 5 nitrofuran 2 yl 1 3 4 thiadiazol 2 yl and 1 5 5 nitrothiophen 2 yl 1 3 4 thiadiazol 2 yl 4 aroylpiperazines
    Bioorganic & Medicinal Chemistry, 2008
    Co-Authors: Mina Behrouzifardmoghadam, Fatemeh Poorrajab, Sussan Kabudanian Ardestani, Abbas Shafiee, Saeed Emami, Alireza Foroumadi
    Abstract:

    The synthesis and anti-leishmanial activity of nitroheteroaryl-1,3,4-thiadiazole-based compounds including 1-[5-(5-nitrofuran-2-yl)-1,3,4-thiadiazol-2-yl]-4-aroylpiperazines and 1-[5-(5-nitrothiophen-2-yl)-1,3,4-thiadiazol-2-yl]-4-aroylpiperazines were described. Most of the synthesized compounds exhibited potent anti-leishmanial activity against both promastigote and amastigote forms of Leishmania major at non-cytotoxic concentrations. In general, 5-nitrofuran derivatives were more active than the corresponding 5-nitrothiophene analogues.

Abbas Shafiee - One of the best experts on this subject based on the ideXlab platform.

  • synthesis and anti leishmanial activity of 5 5 nitrofuran 2 yl 1 3 4 thiadiazol 2 amines containing n 1 benzyl 1h 1 2 3 triazol 4 yl methyl moieties
    European Journal of Medicinal Chemistry, 2012
    Co-Authors: Azar Tahghighi, Sepideh Razmi, Sussan Kabudanian Ardestani, Abbas Shafiee, Saeed Emami, Farzad Kobarfard, Siavoush Dastmalchi, Mohammad Mahdavi, Parham Foroumadi, Alireza Foroumadi
    Abstract:

    Abstract A novel series of 5-(5-nitrofuran-2-yl)-1,3,4-thiadiazol-2-amines were synthesized by introducing N -[(1-benzyl-1 H -1,2,3-triazol-4-yl)methyl] moiety as a new functionality on the C-2 amine of thiadiazole ring via click chemistry. The title compounds namely, N -[(1-benzyl-1 H -1,2,3-triazol-4-yl)methyl]-5-(5-nitrofuran-2-yl)-1,3,4-thiadiazol-2-amines ( 3a – n ) were characterized by IR, NMR and MS spectra. These compounds were evaluated for their in vitro anti-leishmanial activity against promostigote form of the Leishmania major . Most compounds exhibited good anti-leishmanial activity against the promastigote form of L. major . The most active compound against promostigotes was found to be 4-methylbenzyl analog 3i , which significantly decreases the number of intracellular amastigotes per macrophage, percentage of macrophage infectivity and infectivity index.

  • synthesis and antileishmanial activity of novel 5 5 nitrofuran 2 y1 1 3 4 thiadiazoles with piperazinyl linked benzamidine substituents
    European Journal of Medicinal Chemistry, 2011
    Co-Authors: Azar Tahghighi, Sepideh Razmi, Javid Shahbazi Mojarrad, Sussan Kabudanian Ardestani, Abbas Shafiee, Saeed Emami, Farzane Rezazade Marznaki, Farzad Kobarfard, Siavoush Dastmalchi, Alireza Foroumadi
    Abstract:

    In order to optimize the antileishmanial activity of piperazinyl-linked 5-(5-nitrofuran-2-yl)-1,3,4-thiadiazoles, we synthesized a series of 5-(5-nitrofuran-2-y1)-1,3,4-thiadiazoles with piperazinyl-linked benzamidine substituent as scaffold found in pentamidine related antiprotozoals. The structure of target compounds was confirmed by IR, 1H NMR, 13C NMR and Mass spectral data. All compounds were tested for in vitro activity against the promastigote and amastigote forms of Leishmania major. From the results, we found that the substitution on amidine nitrogen has profound role in the biological activity of these compounds. The 5-nitrofuran-2-yl-1,3,4-thiadiazoles having n-propyl, n-butyl and benzyl side chain on benzamidine (as in compounds 2d, 2e and 2g, respectively) showed very good activity in both forms of promastigote and amastigote. The most active compound was N-propyl-4-(4-(5-(5-nitrofuran-2-yl)-1,3,4-thiadiazol-2-yl)piperazin-1-yl) benzamidine hydrochloride (2d) with IC50 value of 0.08 μM in promastigote model. This compound showed a very low level of toxicity against macrophages (CC50=785 μM), with the highest selectivity index (SI=78.5) among the tested compounds.

  • Synthesis and biological activity of 5-nitrofuran-containing (1,3,4-thiadiazol-2-yl)piperazine moieties as a new type of anti-Helicobacter pylori heterocycles
    Serbian Chemical Society, 2011
    Co-Authors: Abbas Shafiee, Farideh Siavoshi, Saeed Emami, Eskandar Alipour, Maryam Omrani, Mohsen Vosooghi, Maryam Nakhjiri, Seyed Esmaeil Sadat-ebrahimi, Azadeh Yahya-meymandi, Mohammad Hassan Moshafi
    Abstract:

    In order to find new and potent drug candidates for the treatment of Helicobacter pylori infections‚ in this study attention was focused on the synthesis and anti-H. pylori activity of a series of 5-(5-nitrofuran-2-yl)-1,3,4-thiadiazoles containing piperazinyl functionality at the C-2 position of the 1,3,4--thiadiazole ring. The synthesis of 1-[5-(5-nitrofuran-2-yl)-1,3,4-thiadiazol-2--yl]piperazine derivatives 3a–h and pyrrolidine derivative 3i was achieved with a versatile and efficient synthetic route via 2-chloro-5-(5-nitrofuran-2-yl)-1,3,4--thiadiazole. The inhibitory activity of the new derivatives 3a–i against twenty clinical H. pylori strains was evaluated by the disc diffusion method and compared with the commercially available standard drug metronidazole. Resulting biological data indicated that most compounds exhibited strong inhibitory activity even at doses lower than 2 μg/disc (average zone of inhibition >20 mm) while metronidazole had little or no growth inhibition at this dose. Compound 3c containing the N-benzoylpiperazin-1-yl moiety showed the most potent inhibitory activity

  • synthesis and in vitro anti leishmanial activity of 1 5 5 nitrofuran 2 yl 1 3 4 thiadiazol 2 yl and 1 5 5 nitrothiophen 2 yl 1 3 4 thiadiazol 2 yl 4 aroylpiperazines
    Bioorganic & Medicinal Chemistry, 2008
    Co-Authors: Mina Behrouzifardmoghadam, Fatemeh Poorrajab, Sussan Kabudanian Ardestani, Abbas Shafiee, Saeed Emami, Alireza Foroumadi
    Abstract:

    The synthesis and anti-leishmanial activity of nitroheteroaryl-1,3,4-thiadiazole-based compounds including 1-[5-(5-nitrofuran-2-yl)-1,3,4-thiadiazol-2-yl]-4-aroylpiperazines and 1-[5-(5-nitrothiophen-2-yl)-1,3,4-thiadiazol-2-yl]-4-aroylpiperazines were described. Most of the synthesized compounds exhibited potent anti-leishmanial activity against both promastigote and amastigote forms of Leishmania major at non-cytotoxic concentrations. In general, 5-nitrofuran derivatives were more active than the corresponding 5-nitrothiophene analogues.

Saeed Emami - One of the best experts on this subject based on the ideXlab platform.

  • synthesis and anti leishmanial activity of 5 5 nitrofuran 2 yl 1 3 4 thiadiazol 2 amines containing n 1 benzyl 1h 1 2 3 triazol 4 yl methyl moieties
    European Journal of Medicinal Chemistry, 2012
    Co-Authors: Azar Tahghighi, Sepideh Razmi, Sussan Kabudanian Ardestani, Abbas Shafiee, Saeed Emami, Farzad Kobarfard, Siavoush Dastmalchi, Mohammad Mahdavi, Parham Foroumadi, Alireza Foroumadi
    Abstract:

    Abstract A novel series of 5-(5-nitrofuran-2-yl)-1,3,4-thiadiazol-2-amines were synthesized by introducing N -[(1-benzyl-1 H -1,2,3-triazol-4-yl)methyl] moiety as a new functionality on the C-2 amine of thiadiazole ring via click chemistry. The title compounds namely, N -[(1-benzyl-1 H -1,2,3-triazol-4-yl)methyl]-5-(5-nitrofuran-2-yl)-1,3,4-thiadiazol-2-amines ( 3a – n ) were characterized by IR, NMR and MS spectra. These compounds were evaluated for their in vitro anti-leishmanial activity against promostigote form of the Leishmania major . Most compounds exhibited good anti-leishmanial activity against the promastigote form of L. major . The most active compound against promostigotes was found to be 4-methylbenzyl analog 3i , which significantly decreases the number of intracellular amastigotes per macrophage, percentage of macrophage infectivity and infectivity index.

  • synthesis and antileishmanial activity of novel 5 5 nitrofuran 2 y1 1 3 4 thiadiazoles with piperazinyl linked benzamidine substituents
    European Journal of Medicinal Chemistry, 2011
    Co-Authors: Azar Tahghighi, Sepideh Razmi, Javid Shahbazi Mojarrad, Sussan Kabudanian Ardestani, Abbas Shafiee, Saeed Emami, Farzane Rezazade Marznaki, Farzad Kobarfard, Siavoush Dastmalchi, Alireza Foroumadi
    Abstract:

    In order to optimize the antileishmanial activity of piperazinyl-linked 5-(5-nitrofuran-2-yl)-1,3,4-thiadiazoles, we synthesized a series of 5-(5-nitrofuran-2-y1)-1,3,4-thiadiazoles with piperazinyl-linked benzamidine substituent as scaffold found in pentamidine related antiprotozoals. The structure of target compounds was confirmed by IR, 1H NMR, 13C NMR and Mass spectral data. All compounds were tested for in vitro activity against the promastigote and amastigote forms of Leishmania major. From the results, we found that the substitution on amidine nitrogen has profound role in the biological activity of these compounds. The 5-nitrofuran-2-yl-1,3,4-thiadiazoles having n-propyl, n-butyl and benzyl side chain on benzamidine (as in compounds 2d, 2e and 2g, respectively) showed very good activity in both forms of promastigote and amastigote. The most active compound was N-propyl-4-(4-(5-(5-nitrofuran-2-yl)-1,3,4-thiadiazol-2-yl)piperazin-1-yl) benzamidine hydrochloride (2d) with IC50 value of 0.08 μM in promastigote model. This compound showed a very low level of toxicity against macrophages (CC50=785 μM), with the highest selectivity index (SI=78.5) among the tested compounds.

  • Synthesis and biological activity of 5-nitrofuran-containing (1,3,4-thiadiazol-2-yl)piperazine moieties as a new type of anti-Helicobacter pylori heterocycles
    Serbian Chemical Society, 2011
    Co-Authors: Abbas Shafiee, Farideh Siavoshi, Saeed Emami, Eskandar Alipour, Maryam Omrani, Mohsen Vosooghi, Maryam Nakhjiri, Seyed Esmaeil Sadat-ebrahimi, Azadeh Yahya-meymandi, Mohammad Hassan Moshafi
    Abstract:

    In order to find new and potent drug candidates for the treatment of Helicobacter pylori infections‚ in this study attention was focused on the synthesis and anti-H. pylori activity of a series of 5-(5-nitrofuran-2-yl)-1,3,4-thiadiazoles containing piperazinyl functionality at the C-2 position of the 1,3,4--thiadiazole ring. The synthesis of 1-[5-(5-nitrofuran-2-yl)-1,3,4-thiadiazol-2--yl]piperazine derivatives 3a–h and pyrrolidine derivative 3i was achieved with a versatile and efficient synthetic route via 2-chloro-5-(5-nitrofuran-2-yl)-1,3,4--thiadiazole. The inhibitory activity of the new derivatives 3a–i against twenty clinical H. pylori strains was evaluated by the disc diffusion method and compared with the commercially available standard drug metronidazole. Resulting biological data indicated that most compounds exhibited strong inhibitory activity even at doses lower than 2 μg/disc (average zone of inhibition >20 mm) while metronidazole had little or no growth inhibition at this dose. Compound 3c containing the N-benzoylpiperazin-1-yl moiety showed the most potent inhibitory activity

  • synthesis and in vitro anti leishmanial activity of 1 5 5 nitrofuran 2 yl 1 3 4 thiadiazol 2 yl and 1 5 5 nitrothiophen 2 yl 1 3 4 thiadiazol 2 yl 4 aroylpiperazines
    Bioorganic & Medicinal Chemistry, 2008
    Co-Authors: Mina Behrouzifardmoghadam, Fatemeh Poorrajab, Sussan Kabudanian Ardestani, Abbas Shafiee, Saeed Emami, Alireza Foroumadi
    Abstract:

    The synthesis and anti-leishmanial activity of nitroheteroaryl-1,3,4-thiadiazole-based compounds including 1-[5-(5-nitrofuran-2-yl)-1,3,4-thiadiazol-2-yl]-4-aroylpiperazines and 1-[5-(5-nitrothiophen-2-yl)-1,3,4-thiadiazol-2-yl]-4-aroylpiperazines were described. Most of the synthesized compounds exhibited potent anti-leishmanial activity against both promastigote and amastigote forms of Leishmania major at non-cytotoxic concentrations. In general, 5-nitrofuran derivatives were more active than the corresponding 5-nitrothiophene analogues.

Mayda I. Lopez - One of the best experts on this subject based on the ideXlab platform.

  • residue depletion of nitrofuran drugs and their tissue bound metabolites in channel catfish ictalurus punctatus after oral dosing
    Journal of Agricultural and Food Chemistry, 2008
    Co-Authors: Pak-sin Chu, Mayda I. Lopez, Ann Abraham, Kathleen El R Said, Steven M Plakas
    Abstract:

    The depletion of the nitrofuran drugs furazolidone, nitrofurazone, furaltadone, and nitrofurantoin and their tissue-bound metabolites [3-amino-2-oxazolidinone (AOZ), semicarbazide (SC), 3-amino-5-morpholinomethyl-2-oxazolidinone (AMOZ), and 1-aminohydantoin (AH), respectively] were examined in the muscle of channel catfish following oral dosing (1 mg/kg body weight). Parent drugs were measurable in muscle within 2 h. Peak levels were found at 4 h for furazolidone (30.4 ng/g) and at 12 h for nitrofurazone, furaltadone, and nitrofurantoin (104, 35.2, and 9.8 ng/g respectively). Parent drugs were rapidly eliminated from muscle, and tissue concentrations fell below the limit of detection (1 ng/g) at 96 h. Peak levels of tissue-bound AMOZ and AOZ (46.8 and 33.7 ng/g respectively) were measured at 12 h, and of SC and AH (31.1 and 9.1 ng/g, respectively) at 24 h. Tissue-bound metabolites were measurable for up to 56 days postdose. These results support the use of tissue-bound metabolites as target analytes for monitoring nitrofuran drugs in channel catfish.

  • determination and confirmation of nitrofuran residues in honey using lc ms ms
    Journal of Agricultural and Food Chemistry, 2007
    Co-Authors: Mayda I. Lopez, Mark F. Feldlaufer, And Anthony D. Williams, Pak-sin Chu
    Abstract:

    A method was developed for the determination and confirmation of furazolidone, nitrofurazone, furaltadone, and nitrofurantoin as their side-chain residues in honey using liquid chromatography−tandem mass spectrometry (LC-MS/MS). An initial solid-phase extraction cleanup of the honey samples was followed by overnight hydrolysis and derivatization of the nitrofuran side-chain residues with 2-nitrobenzaldehyde. After pH adjustment and liquid−liquid extraction, the extracts were assayed by LC-MS/MS using electrospray ionization in the positive ion mode. The method was validated at concentrations ranging from 0.5 to 2.0 ppb with accuracies of 92−103% and coefficients of variation of ≤10%. The lowest calibration standard used (0.25 ppb) was defined as the limit of quantitation for all four nitrofuran side-chain residues. The extracts and standards were also used for confirmatory purposes. Honey from dosed beehives was assayed to study the stability of the nitrofuran residues and to demonstrate the effectiveness...

  • liquid chromatography tandem mass spectrometry for the determination of protein bound residues in shrimp dosed with nitrofurans
    Journal of Agricultural and Food Chemistry, 2005
    Co-Authors: Mayda I. Lopez
    Abstract:

    An analytical method was developed for the determination of bound residues of the nitrofuran drugs furazolidone, nitrofurazone, furaltadone, and nitrofurantoin with a sensitivity of 1 ppb in shrimp. In this procedure, shrimp tissue is prewashed with solvents followed by overnight acid hydrolysis, during which the side chains of the bound residues are released and simultaneously derivatized with 2-nitrobenzaldehyde. After liquid−liquid extraction cleanup, the derivatives are detected and quantitated using liquid chromatography−mass spectrometry/mass spectrometry (LC-MS/MS) with an atmospheric pressure chemical ionization interface. The method was validated using control shrimp fortified with each side-chain analyte at 1, 2, and 4 ppb. Method accuracies were >80% with coefficients of variation of <20% for all four analytes. Tissues from dosed shrimp were assayed to demonstrate the effectiveness of the method for recovering bound residues of nitrofurans. In shrimp dosed with nitrofurans, nitrofurantoin exhib...