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Bogdanowicz A.,Medical University of Gdansk | Foks H.,Medical University of Gdansk | Gobis K.,Medical University of Gdansk | Augustynowicz-Kopec E.,Institute of Tuberculosis and Pulmonary Diseases
Heteroatom Chemistry | Year: 2012

The synthesis of N′-methyl-4-(pyrrolidin-1-yl)picolinohydrazide and N′-methyl-pyrimidine-2-carbohydrazide derivatives (5a and 5b) was carried out. These compounds were used as starting materials to obtain methyl N′-methylhydrazinecarbodithioates 6a and 6b, which, on reaction with either triethylamine or hydrazine, gave corresponding 1,3,4-oxadiazioles 7a and 7b or 1,2,4-triazoles 9a and 9b with the free NH 2 group at the N-4 position, respectively. Compounds 8a-e, particularly containing cyclic amines at N-4 of the 1,2,4-triazole ring, were also obtained. Synthesized compounds were tested in vitro for their activity against Mycobacterium tuberculosis. The structure-activity relationship analysis for obtained compounds was done. © 2012 Wiley Periodicals, Inc. Source

Antoszczak M.,Adam Mickiewicz University | Maj E.,Polish Academy of Sciences | Napiorkowska A.,Institute of Tuberculosis and Pulmonary Diseases | Stefanska J.,University of Warsaw | And 5 more authors.
Molecules | Year: 2014

A series of 12 novel monosubstituted N-benzyl amides of salinomycin (SAL) was synthesized for the first time and characterized by NMR and FT-IR spectroscopic methods. Molecular structures of three salinomycin derivatives in the solid state were determined using single crystal X-ray method. All compounds obtained were screened for their antiproliferative activity against various human cancer cell lines as well as against the most problematic bacteria strains such as methicillin-resistant Staphylococcus aureus (MRSA) and Staphylococcus epidermidis (MRSE), and Mycobacterium tuberculosis. Novel salinomycin derivatives exhibited potent anticancer activity against drug-resistant cell lines. Additionally, two N-benzyl amides of salinomycin revealed interesting antibacterial activity. The most active were N-benzyl amides of SAL substituted at-ortho position and the least anticancer active derivatives were those substituted at the-para position. © 2014 by the authors; licensee MDPI, Basel, Switzerland. Source

Sobieszczanska-Malek M.,Institute of Cardiology | Komuda K.,Institute of Cardiology | Piotrowska M.,Institute of Cardiology | Korewicki J.,Institute of Cardiology | And 3 more authors.
Annals of Transplantation | Year: 2013

Background: Most of the available data suggest that the risk of malignancy in solid organ recipients is higher than in the general population. In Poland, the prevalence rate for malignancy in the general population is about 1.02%. Material/Methods: At out Outpatient Clinic for patients after heart transplantation we analyzed all 324 patients transplanted from 1987-2011 for the presence of malignancies. The endpoint of the analysis was determined by malignancy diagnosis, patient death, or end of the observation period (December 12, 2011). Results: We detected 31 malignancies in 29 of 324 patients (8.95%). In 2 patients we found 2 types of malignancies. The dominant type of malignancy was pulmonary carcinoma, diagnosed in 11/29 (37.93%) patients. Skin carcinoma was recognized in 7 patients (24.14%). Fourteen (48.3%) patients died (12 men and 2 women): 5 of them in the course of pulmonary carcinoma (35.7%), 3 of skin carcinoma (21.4), 3 in the course of lymphoma, 1 in the course of renal carcinoma, 1 in the course of stomach carcinoma, 1 of colorectal carcinoma, and 1 of prostatic carcinoma. Conclusions: The risk of malignancy development is many times higher for HT patients than in the general population. The high incidence rate for pulmonary carcinoma in the analyzed group of patients was most likely related to smoking before transplantation and continuation of smoking after the procedure in the case of patients who received immunosuppressive therapy. © Ann Transplant, 2013. Source

Gobis K.,Medical University of Gdansk | Foks H.,Medical University of Gdansk | Bojanowski K.,Sunny Biodiscovery, Inc. | Augustynowicz-Kopec E.,Institute of Tuberculosis and Pulmonary Diseases | Napiorkowska A.,Institute of Tuberculosis and Pulmonary Diseases
Bioorganic and Medicinal Chemistry | Year: 2012

A series of novel 3-cyclohexylpropanoic acid derivatives and 3-cyclohexylpropanoic acid-derived nitrogen heterocyclic compounds (1-8) have been synthesized and evaluated for tuberculostatic activity. Compounds 1a, 1c, 1e and 1f bearing benzimidazole or benzimidazole-like systems showed the most potent tuberculostatic activity against Mycobacterium tuberculosis strains with MIC values ranging from 1.5 to 12.5 μg/mL. More importantly 1a (6-chloro-2-(2-cyclohexylethyl)-4-nitro-1H-benzo[d]imidazole) and 1f (2-(2-cyclohexylethyl)-1H-imidazo[4,5-b]phenazine) appeared selective for M. tuberculosis as compared with eukaryotic cells (human fibroblasts), and other antimicrobial strains. These compounds may thus represent a novel, selective class of antitubercular agents. Additionally compound 1a stimulated type I collagen output by fibroblasts, in vitro. © 2011 Elsevier Ltd. All rights reserved. Source

Gobis K.,Medical University of Gdansk | Foks H.,Medical University of Gdansk | Zwolska Z.,Institute of Tuberculosis and Pulmonary Diseases | Augustynowicz-Kope E.,Institute of Tuberculosis and Pulmonary Diseases
Heterocycles | Year: 2010

The novel 1,2,4-triazole derivatives have been synthesized by a few different pathways. Heterocyclic carbohydrazides were used to obtain monoesters of hydrazine acids (16), thiosemicarbazide derivatives (717), and finaly 1,2,4-triazole-5-thiones (1838). Carbohydrazides were also cyclized with methyl carbamodithioates in the presence of DBU giving 1,2,4-triazole-5-thiones (18, 19, 3947). Two of final products (39, 40) were undergone alkylation in alkaline solution to appropriate sulfides (4853). Then methylsulfides (48, 49) were oxidized with peroxyacetic acid to sulfoxides (54, 55). The obtained compounds were tested in vitro towards Mycobacterium tuberculosis. © 2010 The Japan Institute of Heterocyclic Chemistry. Source

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