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1.
Turk Gogus Kalp Damar Cerrahisi Derg ; 31(3): 343-351, 2023 Jul.
Article in English | MEDLINE | ID: mdl-37664771

ABSTRACT

Background: This study aims to compare Cardiac Surgery Score (CASUS) and the Acute Physiology and Chronic Health Evaluation (APACHE II) scoring systems for predicting mortality in patients undergoing isolated coronary artery bypass grafting. Methods: Between January 2019 and March 2019, a total of 204 patients (166 males, 38 females; mean age: 60.5±0.7 years; range, 59.2 to 61.9 years) who underwent isolated coronary artery bypass grafting and were monitored at least for 24 h in the intensive care unit postoperatively were included. Pre-, intra-, and postoperative data were recorded. The CASUS and APACHE II scores were calculated using the most abnormal values for each variable during the first 24 h, postoperatively. Clinical outcomes were seven-day mortality and 30-day mortality, need for reintubation, readmission to the intensive care unit, length of intensive care unit stay and length of hospital stay. Results: The 30-day overall mortality was 4.9% (n=10). The CASUS scores were significantly higher for patients developing mortality within 30 days postoperatively (p=0.030) and for patients needing reintubation (p=0.003). In the receiver operating characteristic curve analysis predicting seven-day mortality and prolonged intensive care unit stay, the area under curve was higher for CASUS scoring compared to APACHE II (0.90 vs. 0.72 and 0.82 vs. 0.76). Conclusion: The CASUS may prove to be a more reliable scoring system than APACHE II for predicting mortality and morbidity in patients undergoing isolated coronary artery bypass grafting.

2.
Chem Biodivers ; 20(8): e202300609, 2023 Aug.
Article in English | MEDLINE | ID: mdl-37423889

ABSTRACT

In this article, we report the synthesis and cytotoxicity evaluation of novel indole-carrying semicarbazide derivatives (IS1-IS15). The target molecules were obtained by the reaction of aryl/alkyl isocyanates with 1H-indole-2-carbohydrazide that was in-house synthesized from 1H-indole-2-carboxylic acid. Following structural characterization by 1 H-NMR, 13 C-NMR, and HR-MS, IS1-IS15 were investigated for their cytotoxic activity against human breast cancer cell lines, MCF-7 and MDA-MB-231. According to the data obtained from the MTT assay, phenyl ring with a lipophilic group at its para-position and alkyl moiety were preferential substituents on the indole-semicarbazide scaffold for antiproliferative activity. The effect of IS12 (N-(4-chloro-3-(trifluoromethyl)phenyl)-2-(1H-indole-2-carbonyl)hydrazine-1-carboxamide), the compound that demonstrated remarkable antiproliferative activity on both cell lines, was also evaluated on the apoptotic pathway. Moreover, the calculation of critical descriptors constituting drug-likeness confirmed the position of the selected compounds in the anticancer drug development process. Finally, molecular docking studies suggested the inhibition of tubulin polymerization as the potential activity mechanism of this class of molecules.


Subject(s)
Antineoplastic Agents , Breast Neoplasms , Humans , Female , Structure-Activity Relationship , Molecular Docking Simulation , Breast Neoplasms/drug therapy , Drug Screening Assays, Antitumor , Cell Proliferation , Antineoplastic Agents/chemistry , Cell Line , Indoles/chemistry , Semicarbazides/pharmacology , Molecular Structure , Cell Line, Tumor
3.
Bioorg Chem ; 102: 104104, 2020 09.
Article in English | MEDLINE | ID: mdl-32736149

ABSTRACT

The development of new antimicrobial compounds is in high demand to overcome the emerging drug resistance against infectious microbial pathogens. In the present study, we carried out the extensive antimicrobial screening of disubstituted urea derivatives. In addition to the classical synthesis of urea compounds by the reaction of amines and isocyanates, we also applied a new route including bromination, oxidation and azidination reactions, respectively, to convert 2-amino-3-methylpyridine to 1,3-disubstituted urea derivatives using various amines. The evaluation of antimicrobial activities against various bacterial strains, Candida albicans as well as Mycobacterium tuberculosis resulted in the discovery of new active molecules. Among them, two compounds, which have the lowest MIC values on Pseudomonas aeruginosa, were further evaluated for their inhibition capacities of biofilm formation. In order to evaluate their potential mechanism of biofilm inhibition, these two compounds were docked into the active site of LasR, which is the transcriptional regulator of bacterial signaling mechanism known as quorum sensing. Finally, the theoretical parameters of the bioactive molecules were calculated to establish their drug-likeness properties.


Subject(s)
Anti-Bacterial Agents/pharmacology , Candida albicans/drug effects , Molecular Docking Simulation , Mycobacterium tuberculosis/drug effects , Urea/pharmacology , Anti-Bacterial Agents/chemical synthesis , Anti-Bacterial Agents/chemistry , Biofilms/drug effects , Dose-Response Relationship, Drug , Microbial Sensitivity Tests , Molecular Structure , Structure-Activity Relationship , Urea/analogs & derivatives , Urea/chemistry
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