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1.
Chem Biodivers ; 21(6): e202301942, 2024 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-38393713

RESUMO

This article reports one-pot synthesis of ten novel spirooxindoles using 5-methyl-2-thiohydantoin, isatin derivatives, and malononitrile in good to high yields (65-90 %). The structures of the synthesized compounds were deduced by 1H-NMR, 13C NMR, FT-IR, and Mass spectral data. The antibacterial activity of the compounds was evaluated against two Gram-positive bacteria (Staphylococcus aureus and Bacillus subtilis) and two Gram-negative bacteria (Escherichia coli and Pseudomonas aeruginosa) based on the Kirby-Bauer method. According to the obtained data, the synthesized compounds show more activity against Gram-positive bacteria than Gram-negative bacteria. Also, the antioxidant activity of these compounds was measured using the DPPH radical scavenging test method, which showed good to excellent activity (59.65-94.03 %). Among them, the chlorinated derivatives (4 f-j) exhibited more antioxidant activity (84.85-94.03 %) than the other compounds (4 a-e) (56.65-74.4 %) and even ascorbic acid as a standard antioxidant compound (82.3 %).


Assuntos
Antibacterianos , Antioxidantes , Indóis , Testes de Sensibilidade Microbiana , Compostos de Espiro , Antibacterianos/farmacologia , Antibacterianos/síntese química , Antibacterianos/química , Antioxidantes/farmacologia , Antioxidantes/síntese química , Antioxidantes/química , Compostos de Bifenilo/antagonistas & inibidores , Compostos de Bifenilo/química , Bactérias Gram-Negativas/efeitos dos fármacos , Bactérias Gram-Positivas/efeitos dos fármacos , Indóis/química , Indóis/farmacologia , Indóis/síntese química , Estrutura Molecular , Oxindóis/farmacologia , Oxindóis/química , Oxindóis/síntese química , Picratos/antagonistas & inibidores , Pseudomonas aeruginosa/efeitos dos fármacos , Compostos de Espiro/química , Compostos de Espiro/farmacologia , Compostos de Espiro/síntese química , Espiro-Oxindóis , Staphylococcus aureus/efeitos dos fármacos , Relação Estrutura-Atividade , Isatina/síntese química , Isatina/química , Isatina/farmacologia
2.
J Obstet Gynaecol ; 42(2): 333-337, 2022 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-34151685

RESUMO

The adverse effects of bacterial contamination during in vitro fertilisation and embryo transfer (IVF-ET) have been studied previously. However, data on asymptomatic women with positive bacterial culture and their IVF outcome are lacking. This prospective longitudinal study was conducted on 74 women undergoing IVF-ET, of whom specimens from the endocervix and ET catheter were taken and sent to a laboratory for microbiological assessment. Then, patients were followed up for evaluation of chemical pregnancy (ß-HCG > 25 mIU/mL) and clinical pregnancy (detected foetal heartbeat). The findings revealed that there was no significant difference in terms of biochemical (35.4% vs. 19.2%, p= .116) and clinical pregnancy rate (25.0% vs. 15.4%, p= .257) among ET catheter culture positive and negative women. This finding allows us to conclude that the positive culture in the absence of clinical signs of infection may not increase the risk of implantation failure.Impact StatementWhat is already known on this subject? There is growing evidence indicating that endometritis may decrease the endometrial receptiveness in in vitro fertilisation (IVF) cycles; however, there is a paucity of knowledge regarding IVF outcomes when the bacterial culture of embryo transfer (ET) catheter is positive.What the results of this study add? The present study demonstrates that positive ET catheter culture in asymptomatic women does not increase the risk of IVF failure.What the implications are of these findings for clinical practice and/or further research? Positive-culture, per se, may not be associated with poor IVF outcomes and further studies should be undertaken on this topic in various clinical settings using different protocols.


Assuntos
Transferência Embrionária , Fertilização in vitro , Catéteres , Feminino , Humanos , Estudos Longitudinais , Gravidez , Taxa de Gravidez , Estudos Prospectivos
3.
Chem Biodivers ; 18(9): e2100197, 2021 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-34272925

RESUMO

In this study, the synthesis of new spiropyrazoles, pyrazole and hydantoin heterocycles is reported by three component reactions of parabanic acids, hydrazine derivatives, and phenacyl bromides in the presence of triphenylphosphine as a nucleophile and triethylamine as a base in good to high yields (69-91 %). Evaluation of the synthesized compounds revealed a good to excellent antioxidant activities (37.6-96.2 %) using DPPH inhibitory potency. Among these compounds, hydantoin derivatives displayed higher antioxidant activities (93.7-96.2 %) comparing with spiropyrazoles and pyrazoles. The obtained results showed that Cl and Br substituents on the phenyl ring increased antioxidant activities of the related heterocycles. The antibacterial activities of the synthesized compounds were examined against two Gram-negative (Escherichia coli and Pseudomonas aeruginosa) and two Gram-positive (Staphylococcus aureus and Bacillus subtilis) bacteria. Among the synthesized heterocycles, 2-[1,3-dimethyl-2,5-dioxo-4-(2-oxo-2-phenylethyl)imidazolidin-4-yl]hydrazine-1-carbothioamide exhibited the excellent antibacterial activity against both Gram-positive and Gram-negative bacteria.


Assuntos
Antibacterianos/farmacologia , Antioxidantes/farmacologia , Bactérias Gram-Negativas/efeitos dos fármacos , Bactérias Gram-Positivas/efeitos dos fármacos , Pirazóis/farmacologia , Compostos de Espiro/farmacologia , Antibacterianos/síntese química , Antibacterianos/química , Antioxidantes/síntese química , Antioxidantes/química , Compostos de Bifenilo/antagonistas & inibidores , Testes de Sensibilidade Microbiana , Estrutura Molecular , Picratos/antagonistas & inibidores , Pirazóis/síntese química , Pirazóis/química , Compostos de Espiro/síntese química , Compostos de Espiro/química
4.
J Obstet Gynaecol Res ; 47(1): 296-301, 2021 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-33034145

RESUMO

AIM: This study aimed to evaluate the effect of piroxicam adjuvant therapy on the clinical and biochemical pregnancy rate in patients undergoing in vitro fertilization (IVF) and frozen-thawed embryo transfer (ET) cycles. METHODS: In a randomized, double-blinded, placebo-controlled clinical trial, 178 patients eligible for IVF-ET received either single dose of piroxicam 1-2 h before frozen-thawed ET or a placebo at the same time. Study participants were then followed and compared regarding the primary outcome of the study, which was biochemical (positive ß-human chorionic gonadotrophin test) and clinical pregnancy (detected fetal heart beat in ultrasound) rate. RESULTS: The results of this study indicated that there is no significant association between the piroxicam administration before frozen-thawed ET and the clinical or biochemical pregnancy rate (P = 0.208 and P = 0.699, respectively). CONCLUSION: The findings of the current study suggest that piroxicam administration before ET has no beneficial effects on pregnancy rate among women undergoing IVF and frozen-thawed ET. However, further studies with larger sample sizes and longer follow-ups are recommended.


Assuntos
Transferência Embrionária , Piroxicam , Gonadotropina Coriônica Humana Subunidade beta , Criopreservação , Método Duplo-Cego , Feminino , Fertilização in vitro , Humanos , Gravidez , Taxa de Gravidez
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