In Vitro Activities of Position 2 Substitution-Bearing 6-Nitro- and 6-Amino-Benzothiazoles and Their Corresponding Anthranilic Acid Derivatives against<i>Leishmania infantum</i>and<i>Trichomonas vaginalis</i>

Delmas, F.; Giorgio, Carole Di; Robin, Maxime; Azas, Nadine; Gasquet, M.; Detang, Claire; Costa, Muriel; Timon‐David, P.; Galy, Jean

doi:10.1128/aac.46.8.2588-2594.2002

Cited by 51 publications

(31 citation statements)

References 18 publications

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“…The minimum lethal concentration (MLC) was defined as the lowest drug concentration in which no motile organism was observed. The 50% inhibitory concentration (IC 50 ) value was determined as the drug concentration in which 50% T. vaginalis cells were alive and 50% died (Delmas et al, 2002). All experiments were carried out in triplicate.…”

Section: Determination Of Minimum Lethal Concentration (Mlc) and 50% mentioning

confidence: 99%

“…2. This assay was performed according to Wright et al (2010) and Delmas et al (2002) with modifications. Amomum tsao-ko essential oil and geraniol were diluted by geometric dilutions in 96-well plates, ranging from 22.48 mg/ ml to 46.05 mg/ml of A. tsao-ko essential oil, and from 21.43 mg/ml to 43.90 mg/ml of geraniol.…”

Section: Determination Of Minimum Lethal Concentration (Mlc) and 50% mentioning

confidence: 99%

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Anti-Trichomonas vaginalisproperties of the oil ofAmomum tsao-koand its major component, geraniol

Dai

Peng

et al. 2015

Pharmaceutical Biology

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Context: Trichomonosis, caused by the flagellate protozoan Trichomonas vaginalis, is the most common non-viral sexually transmitted disease (STD) and 5-nitroimidazole drugs are used for the treatment. However, a growing number of T. vaginalis isolates are resistant to these drugs, which make it becomes an urgent issue. Objective: The current study was designed to evaluate the anti-T. vaginalis activity of the essential oil from A. tsao-ko used in traditional Chinese medicine and as a spice and its main component, geraniol. Materials and methods:The anti-T. vaginalis activities of A. tsao-ko essential oil and geraniol were evaluated by the minimum lethal concentration (MLC) and 50% inhibitory concentration (IC 50 ) in vitro. The morphological changes of T. vaginalis were observed by transmission electron microscopy (TEM). Additionally, sub-MLC concentration treatment with sub-MLC A. tsao-ko essential oil and geraniol was also performed. Results: This study shows that MLC/IC 50 of A. tsao-ko essential oil was 44.97 mg/ml/22.49 mg/ml for T. vaginalis isolate Tv1, and 89.93 mg/ml/44.97 mg/ml for T. vaginalis isolate Tv2. Those of geraniol were 342.96 mg/ml/171.48 mg/ml, respectively. After A. tsao-ko essential oil or geraniol treatment, obvious similar morphological changes of T. vaginalis were observed by TEM: the nuclear membrane was damaged, nuclei were dissolved, and the chromatin was accumulated; in the cytoplasm, numerous vacuoles appeared, rough endoplasmic reticulum dilated, the number of ribosomes were reduced, organelles disintegrated, the cell membrane was partially damaged, with cytoplasmic leakage, and cell disintegration was observed. The action time did not increase the effect of A. tsao-ko essential oil or geraniol against T. vaginalis, as no significant difference was observed after sub-MLC concentration treatment for 1, 3, and 5 h with A. tsao-ko essential oil and geraniol. Discussion and conclusion: The study describes the first report on the activity and morphological changes of A. tsao-ko essential oil and geraniol against T. vaginalis. The results obtained herein presented new opportunities for antitrichomonal drugs.

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Section: Determination Of Minimum Lethal Concentration (Mlc) and 50% mentioning

confidence: 99%

Section: Determination Of Minimum Lethal Concentration (Mlc) and 50% mentioning

confidence: 99%

Anti-Trichomonas vaginalisproperties of the oil ofAmomum tsao-koand its major component, geraniol

Dai

Peng

et al. 2015

Pharmaceutical Biology

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“…Because of the wide range of activities of the benzothiazole drugs including neuroprotective, anticonvulsive, antiallergenic, antimicrobial and antitumour, Delmas et al [74] investigated the antitrichomonal activities of a variety of benzothiazoles. Generally they exhibited poor trophozoite toxicity, but two compounds had inhibitory concentrations of 1.6 and 2.9 M in comparison with 3.…”

Section: Alternative Chemotherapeutic Agentsmentioning

confidence: 99%

Drug resistance in the sexually transmitted protozoan Trichomonas vaginalis

et al. 2003

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Trichomoniasis is the most common, sexually transmitted infection. It is caused by the flagellated protozoan parasite Trichomonas vaginalis. Symptoms include vaginitis and infections have been associated with preterm delivery, low birth weight and increased infant mortality, as well as predisposing to HIV/AIDS and cervical cancer. Trichomoniasis has the highest prevalence and incidence of any sexually transmitted infection. The 5-nitroimidazole drugs, of which metronidazole is the most prescribed, are the only approved, effective drugs to treat trichomoniasis. Resistance against metronidazole is frequently reported and cross-resistance among the family of 5-nitroimidazole drugs is common, leaving no alternative for treatment, with some cases remaining unresolved. The mechanism of metronidazole resistance in T. vaginalis from treatment failures is not well understood, unlike resistance which is developed in the laboratory under increasing metronidazole pressure. In the latter situation, hydrogenosomal function which is involved in activation of the prodrug, metronidazole, is down-regulated. Reversion to sensitivity is incomplete after removal of drug pressure in the highly resistant parasites while clinically resistant strains, so far analysed, maintain their resistance levels in the absence of drug pressure. Although anaerobic resistance has been regarded as a laboratory induced phenomenon, it clearly has been demonstrated in clinical isolates. Pursuit of both approaches will allow dissection of the underlying mechanisms. Many alternative drugs and treatments have been tested in vivo in cases of refractory trichomoniasis, as well as in vitro with some successes including the broad spectrum anti-parasitic drug nitazoxanide. Drug resistance incidence in T. vaginalis appears to be on the increase and improved surveillance of treatment failures is urged.

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“…Benzothiazole are an important class of bioactive and industrially important organic compounds. From the recent literature, these derivatives are also known to possess anti-tubercular, [3] local anesthetic, [4] antidiabetic, [5] antiulcer, [6] antipsychotic, [7] anti-tumor, [8] anti-oxidant, [9] analgesic, [10] schistosomicidal, [11] antileishmanial, [12] anti-convulsant, [13] anti-parasitic, [14] diuretic, [15] plant growth regulator [16] activities, anthelmintic, [17] Acaricidal. [18] Quinoline or 1-aza-naphthalene is one of the most important N-based heterocyclic aromatic compounds.…”

Section: Introductionmentioning

confidence: 99%

Synthesis and Characterization of Novel N-(Benzo[d]Thiazol-2-yl)-2-(2-(6-Chloroquinolin-4-yl)Hydrazinyl)Acetamide Derivatives Containing Quinoline Linkage as Potent Antibacterial Agents

Bhoi

Borad

Parmar

et al. 2015

ILCPA

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ABSTRACT. As part of ongoing studies in developing new antibacterial agent, a novel series of N-(benzo[d]thiazol-2-yl)-2-(2-(6-chloroquinolin-4-yl)hydrazinyl)acetamide derivatives was synthesized by sequencing reaction of 2-aminobenzothiazole with chloroacetylchloride, hydrazine hydrate and 4,7-dichloroquinoline. The novel heterocycles were characterized by elemental analyses and various spectroscopic techniques. The synthesized compounds were tested in-vitro antibacterial activity against two Gram-positive and two Gram-negative bacteria with standard drugs. Microbiological results showed that the synthesized compounds possessed a broad spectrum of antibacterial activity against the tested microorganisms.

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In Vitro Activities of Position 2 Substitution-Bearing 6-Nitro- and 6-Amino-Benzothiazoles and Their Corresponding Anthranilic Acid Derivatives againstLeishmania infantumandTrichomonas vaginalis

Cited by 51 publications

References 18 publications

Anti-Trichomonas vaginalisproperties of the oil ofAmomum tsao-koand its major component, geraniol

Anti-Trichomonas vaginalisproperties of the oil ofAmomum tsao-koand its major component, geraniol

Drug resistance in the sexually transmitted protozoan Trichomonas vaginalis

Synthesis and Characterization of Novel N-(Benzo[d]Thiazol-2-yl)-2-(2-(6-Chloroquinolin-4-yl)Hydrazinyl)Acetamide Derivatives Containing Quinoline Linkage as Potent Antibacterial Agents

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