The synthesis of novel hybrid compounds containing 5-nitrothiazole moiety as potential antiparasitic agents

Yasmin R.H. Saleh; Haythem A. Saadeh; Hargobinder Kaur; Kapil Goyal; Rakesh Sehgal; Mohammad S. Mubarak

doi:10.1007/s00706-015-1511-y

The synthesis of novel hybrid compounds containing 5-nitrothiazole moiety as potential antiparasitic agents

Yasmin R.H. Saleh
, Haythem A. Saadeh
, Hargobinder Kaur
, Kapil Goyal
, Rakesh Sehgal
, Mohammad S. Mubarak

Department of Chemistry

Research output: Contribution to journal › Article › peer-review

8 Citations (Scopus)

Abstract

A number of novel compounds containing 5-nitrothiazole moiety as potential antiparasitic agents have been synthesized through known chemical routes. The structures of the new compounds were confirmed by spectroscopic techniques, ¹H NMR, ¹³C NMR, and mass spectrometry, and by elemental analyses. The prepared compounds were evaluated in vitro for their antigiardial and antitrichomonal activities. All tested compounds exhibited remarkable antigiardial activity with IC₅₀ values ranging from 2.2 to 6.9 μg/cm³ as compared to the reference drug metronidazole (IC₅₀ = 7.3 μg/cm³). In addition, three of the prepared compounds exhibited significant antitrichomonal activity with IC₅₀ values of 4.3, 5.0, and 7.9 μg/cm³, respectively, as compared to the reference drug metronidazole (8.5 μg/cm³). Graphical abstract: [Figure not available: see fulltext.]

Original language	English
Pages (from-to)	2087-2095
Number of pages	9
Journal	Monatshefte fur Chemie
Volume	146
Issue number	12
DOIs	https://doi.org/10.1007/s00706-015-1511-y
Publication status	Published - Dec 1 2015

Keywords

5-Nitrothiazole
Antigiardial activity
Antitrichomonal activity
Chloroquine
Hybrid molecules
Metronidazole

ASJC Scopus subject areas

General Chemistry

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10.1007/s00706-015-1511-y

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title = "The synthesis of novel hybrid compounds containing 5-nitrothiazole moiety as potential antiparasitic agents",

abstract = "A number of novel compounds containing 5-nitrothiazole moiety as potential antiparasitic agents have been synthesized through known chemical routes. The structures of the new compounds were confirmed by spectroscopic techniques, 1H NMR, 13C NMR, and mass spectrometry, and by elemental analyses. The prepared compounds were evaluated in vitro for their antigiardial and antitrichomonal activities. All tested compounds exhibited remarkable antigiardial activity with IC50 values ranging from 2.2 to 6.9 μg/cm3 as compared to the reference drug metronidazole (IC50 = 7.3 μg/cm3). In addition, three of the prepared compounds exhibited significant antitrichomonal activity with IC50 values of 4.3, 5.0, and 7.9 μg/cm3, respectively, as compared to the reference drug metronidazole (8.5 μg/cm3). Graphical abstract: [Figure not available: see fulltext.]",

keywords = "5-Nitrothiazole, Antigiardial activity, Antitrichomonal activity, Chloroquine, Hybrid molecules, Metronidazole",

author = "Saleh, \{Yasmin R.H.\} and Saadeh, \{Haythem A.\} and Hargobinder Kaur and Kapil Goyal and Rakesh Sehgal and Mubarak, \{Mohammad S.\}",

note = "Publisher Copyright: {\textcopyright} 2015 Springer-Verlag Wien.",

year = "2015",

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doi = "10.1007/s00706-015-1511-y",

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T1 - The synthesis of novel hybrid compounds containing 5-nitrothiazole moiety as potential antiparasitic agents

AU - Saleh, Yasmin R.H.

AU - Saadeh, Haythem A.

AU - Kaur, Hargobinder

AU - Goyal, Kapil

AU - Sehgal, Rakesh

AU - Mubarak, Mohammad S.

PY - 2015/12/1

Y1 - 2015/12/1

N2 - A number of novel compounds containing 5-nitrothiazole moiety as potential antiparasitic agents have been synthesized through known chemical routes. The structures of the new compounds were confirmed by spectroscopic techniques, 1H NMR, 13C NMR, and mass spectrometry, and by elemental analyses. The prepared compounds were evaluated in vitro for their antigiardial and antitrichomonal activities. All tested compounds exhibited remarkable antigiardial activity with IC50 values ranging from 2.2 to 6.9 μg/cm3 as compared to the reference drug metronidazole (IC50 = 7.3 μg/cm3). In addition, three of the prepared compounds exhibited significant antitrichomonal activity with IC50 values of 4.3, 5.0, and 7.9 μg/cm3, respectively, as compared to the reference drug metronidazole (8.5 μg/cm3). Graphical abstract: [Figure not available: see fulltext.]

AB - A number of novel compounds containing 5-nitrothiazole moiety as potential antiparasitic agents have been synthesized through known chemical routes. The structures of the new compounds were confirmed by spectroscopic techniques, 1H NMR, 13C NMR, and mass spectrometry, and by elemental analyses. The prepared compounds were evaluated in vitro for their antigiardial and antitrichomonal activities. All tested compounds exhibited remarkable antigiardial activity with IC50 values ranging from 2.2 to 6.9 μg/cm3 as compared to the reference drug metronidazole (IC50 = 7.3 μg/cm3). In addition, three of the prepared compounds exhibited significant antitrichomonal activity with IC50 values of 4.3, 5.0, and 7.9 μg/cm3, respectively, as compared to the reference drug metronidazole (8.5 μg/cm3). Graphical abstract: [Figure not available: see fulltext.]

KW - 5-Nitrothiazole

KW - Antigiardial activity

KW - Antitrichomonal activity

KW - Chloroquine

KW - Hybrid molecules

KW - Metronidazole

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DO - 10.1007/s00706-015-1511-y

M3 - Article

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VL - 146

SP - 2087

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JO - Monatshefte fur Chemie

JF - Monatshefte fur Chemie

IS - 12

ER -

The synthesis of novel hybrid compounds containing 5-nitrothiazole moiety as potential antiparasitic agents

Abstract

Keywords

ASJC Scopus subject areas

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