scholarly journals Synthesis and In Vitro Anti-Toxoplasma gondii Activity of Novel Thiazolidin-4-one Derivatives

Molecules ◽  
2019 ◽  
Vol 24 (17) ◽  
pp. 3029
Author(s):  
Nazar Trotsko ◽  
Adrian Bekier ◽  
Agata Paneth ◽  
Monika Wujec ◽  
Katarzyna Dzitko
Keyword(s):  
Toxoplasma Gondii ◽  
Weight Ratio ◽  
Dimethyl Acetylenedicarboxylate ◽  
Ethyl Bromoacetate ◽  
New Agents ◽  
Inhibition Of Proliferation ◽  
Effective Drugs ◽  
Proliferation In Vitro ◽  
Better Than

Recent findings on the biological activity of thiazolidin-4-ones and taking into account the lack of effective drugs used in the treatment of toxoplasmosis, their numerous side effects, as well as the problem of drug resistance of parasites prompted us to look for new agents. We designed and synthesized a series of new thiazolidin-4-one derivatives through a two-step reaction between 4-substituted thiosemicarbazides with hydroxybenzaldehydes followed by the treatment with ethyl bromoacetate; maleic anhydride and dimethyl acetylenedicarboxylate afforded target compounds. The thiazolidin-4-one derivatives were used to assess the inhibition of Toxoplasma gondii growth in vitro. All active thiazolidine-4-one derivatives (12 compounds) inhibited T. gondii proliferation in vitro much better than used references drugs both sulfadiazine as well as the synergistic effect of sulfadiazine + trimethoprim (weight ratio 5:1). Most active among them derivatives 94 and 95 showed inhibition of proliferation at about 392-fold better than sulfadiazine and 18-fold better than sulfadiazine with trimethoprim. All active compounds (82–88 and 91–95) against T. gondii represent values from 1.75 to 15.86 (CC30/IC50) lower than no cytotoxic value (CC30).

scholarly journals Discovery of Potent and Selective Halogen-Substituted Imidazole-Thiosemicarbazides for Inhibition of Toxoplasma gondii Growth In Vitro via Structure-Based Design

Molecules ◽  
2019 ◽  
Vol 24 (8) ◽  
pp. 1618 ◽  
Author(s):  
Agata Paneth ◽  
Lidia Węglińska ◽  
Adrian Bekier ◽  
Edyta Stefaniszyn ◽  
Monika Wujec ◽  
...  
Keyword(s):  
Toxoplasma Gondii ◽  
Limiting Factor ◽  
In Vitro Proliferation ◽  
Highly Effective ◽  
Rate Limiting ◽  
Better Than

Employing a simple synthetic protocol, a series of highly effective halogen-substituted imidazole-thiosemicarbazides with anti-Toxoplasma gondii effects against the RH tachyzoites, much better than sulfadiazine, were obtained (IC50s 10.30—113.45 µg/mL vs. ~2721.45 µg/mL). The most potent of them, 12, 13, and 15, blocked the in vitro proliferation of T. gondii more potently than trimethoprim (IC50 12.13 µg/mL), as well. The results of lipophilicity studies collectively suggest that logP would be a rate-limiting factor for the anti-Toxoplasma activity of this class of compounds.

scholarly journals In vitro action of antiparasitic drugs, especially artesunate, against Toxoplasma gondii

2012 ◽  
Vol 45 (4) ◽  
pp. 485-490 ◽  
Author(s):  
Thaís Cobellis Gomes ◽  
Heitor Franco de Andrade Júnior ◽  
Susana Angélica Zevallos Lescano ◽  
Vicente Amato-Neto
Keyword(s):  
Toxoplasma Gondii ◽  
Inhibitory Concentration ◽  
Inhibitory Effect ◽  
Congenital Disease ◽  
Nonlinear Regression Analysis ◽  
Antiparasitic Drugs ◽  
Effective Drugs ◽  
Disposable Plastic

INTRODUCTION: Toxoplasmosis is usually a benign infection, except in the event of ocular, central nervous system (CNS), or congenital disease and particularly when the patient is immunocompromised. Treatment consists of drugs that frequently cause adverse effects; thus, newer, more effective drugs are needed. In this study, the possible activity of artesunate, a drug successfully being used for the treatment of malaria, on Toxoplasma gondii growth in cell culture is evaluated and compared with the action of drugs that are already being used against this parasite. METHODS: LLC-MK2 cells were cultivated in RPMI medium, kept in disposable plastic bottles, and incubated at 36ºC with 5% CO2. Tachyzoites of the RH strain were used. The following drugs were tested: artesunate, cotrimoxazole, pentamidine, pyrimethamine, quinine, and trimethoprim. The effects of these drugs on tachyzoites and LLC-MK2 cells were analyzed using nonlinear regression analysis with Prism 3.0 software. RESULTS: Artesunate showed a mean tachyzoite inhibitory concentration (IC50) of 0.075µM and an LLC MK2 toxicity of 2.003µM. Pyrimethamine was effective at an IC50 of 0.482µM and a toxicity of 11.178µM. Trimethoprim alone was effective against the in vitro parasite. Cotrimoxazole also was effective against the parasite but at higher concentrations than those observed for artesunate and pyrimethamine. Pentamidine and quinine had no inhibitory effect over tachyzoites. CONCLUSIONS: Artesunate is proven in vitro to be a useful alternative for the treatment of toxoplasmosis, implying a subsequent in vivo effect and suggesting the mechanism of this drug against the parasite.

1442: CXCL12 Over-Expression and Secretion by Aging Fibroblasts Stimulates Human Prostate Epithelial Proliferation in Vitro

2006 ◽  
Vol 175 (4S) ◽  
pp. 466-466
Author(s):  
Jill A. Macoska ◽  
Lesa Begley ◽  
Christine Monteleon ◽  
James W. MacDonald ◽  
Rajal B. Shah
Keyword(s):  
Human Prostate ◽  
Epithelial Proliferation ◽  
Over Expression ◽  
Proliferation In Vitro

MICROPROPAGATION OF CHICKPEA FROM SHOOT TIP AND NODE SEGMENT

2018 ◽  
Vol 24 (2) ◽  
Author(s):  
J. D. BARSHILE
Keyword(s):  
Shoot Tip ◽  
Root Induction ◽  
Multiple Response ◽  
Ms Medium ◽  
Growth Responses ◽  
Rapid Multiplication ◽  
Micro Propagation ◽  
G 12 ◽  
Better Than

Present investigation was undertaken to standardize technique for in vitro micro-propagation of chickpea( Cicer arietinum ) cultivar Vishwas (Phule G 12). Micropropagation method for chickpea was established and this method enabled much more efficient propagation of plants. The present work was aimed at evolving a protocol for rapid multiplication of chickpea using micropropagation technique. Explants from shoot tip and node segment were cultured on MS medium supplemented with different concentrations of BAP and Kinetin (1.0 to 2.5 mg/l) and their growth responses like shooting were elucidated. The maximum multiple response was observed with 2 mg/l concentration of BAP from both types of explant. The highest number of shoots (12.5 ± 0.3) was achieved on MS medium with 2 mg/l BAP using node segments. The medium supplemented with 2 mg/l of BAP was found better than all other concentrations. Individual shoots were transferred to IBA and IAA (1.0-1.5 mg/l) for root induction. MS medium supplemented with 2 mg/l of IBA proved better for rooting. Rooted plantlets were successfully hardened in greenhouse and established in the pot.

The effect of cyclic AMP on the growth of Toxoplasma gondii in vitro

1990 ◽  
Vol 28 (2) ◽  
pp. 71 ◽  
Author(s):  
W Y Choi ◽  
H W Nam ◽  
J H Youn ◽  
D J Kim ◽  
W K Kim ◽  
...  
Keyword(s):  
Toxoplasma Gondii ◽  
Cyclic Amp

Age-Related Changes in the Effects of Serum from Lean and Obese Pigs on Myogenic Cell Proliferation in Vitro

1982 ◽  
Vol 54 (4) ◽  
pp. 763-768 ◽  
Author(s):  
Ronald E. Allen ◽  
Gail Robinson ◽  
Matthew J. Parsons ◽  
Robert A. Merkel ◽  
William T. Magee
Keyword(s):  
Cell Proliferation ◽  
Myogenic Cell ◽  
Age Related ◽  
Proliferation In Vitro ◽  
Age Related Changes

Synthesis and Antifungal Activity of Coumarins Derivatives Against Sporothrix spp.

2018 ◽  
Vol 18 (2) ◽  
pp. 164-171 ◽  
Author(s):  
Luana da S.M. Forezi ◽  
Luana Pereira Borba-Santos ◽  
Mariana F.C. Cardoso ◽  
Vitor F. Ferreira ◽  
Sonia Rozental ◽  
...  
Keyword(s):  
Antifungal Activity ◽  
Antifungal Agents ◽  
Sporothrix Schenckii ◽  
Public Health Problem ◽  
Domestic Animals ◽  
Coumarin Derivatives ◽  
Sporothrix Brasiliensis ◽  
Synthetic Routes ◽  
Effective Drugs

Sporotrichosis is a serious public health problem in Brazil that affects human patients and domestic animals, mainly cats. Thus, the search for new antifungal agents is required also due to the emergence and to the lack of effective drugs available in the therapeutic arsenal. The aim of this study was to evaluate the in vitro antifungal profile of two synthetic series of coumarin derivatives against Sporothrix schenckii and Sporothrix brasiliensis. The three-components synthetic routes used for the preparation of coumarin derivatives have proved to be quite efficient and compounds 16 and 17 have been prepared in good yields. The inhibitory activity of nineteen synthetic coumarins derivatives 16a-i and 17a-j were evaluated against Sporothrix spp. yeasts and the most potent compounds were 16b and 17i. However, according to concentrations able to inhibit (minimum inhibitory concentrations) and kill (minimum fungicidal concentrations) the cells, 17i was more effective than 16b against Sporothrix spp. Thus, 17i exhibited good antifungal activity against S. brasiliensis and S. schenckii, suggesting that it is an important scaffold for the development of novel antifungal agents.

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