DESIGN AND SYNTHESIS OF SOME PIPERAZINE HYBRID MOLECULES

WOS: 000428238300008In this work, a new series of piperazine hybrid molecules containing coumarin, isatin, salicyl, furane and 1,2,4-triazol-3-thiol moieties was synthesized in good yields. 2-[4-(4-Nitrophenyl)piperazin-1-yl] acetohydrazide was used as key intermediate to obtain these hybrid molecules. the structures of newly synthesized compounds were identified by H-1 NMR, C-13 NMR and elemental analysis data

Synthesis and Urease Inhibition Study of Some New Quinazolinone Derivatives Bearing Triazole, Thiadiazole, and Piperazine Moiety

WOS: 000450023400011A new series of 2,3-disubstituted quinazolin-4(3H)-one derivatives bearing triazole and thiadiazole nucleus has been synthesized and then screened for their urease inhibition properties. All synthesized compounds showed outstanding urease inhibitory potentials with IC50 values ranging between 0.25 +/- 0.01 and 18.00 +/- 0.64 mu g/mL when compared with standard inhibitors thiourea (IC50 = 15.08 +/- 0.71 mu g/mL) and acetohydroxamic acid (IC50 = 21.05 +/- 0.96 mu g/mL). All new molecules were characterized by H-1 NMR, C-13 NMR, and MS.Scientific and Technological Research Council of Turkey (TUBITAK)Turkiye Bilimsel ve Teknolojik Arastirma Kurumu (TUBITAK) [115Z885]; TUBITAKTurkiye Bilimsel ve Teknolojik Arastirma Kurumu (TUBITAK)This work was supported by the Scientific and Technological Research Council of Turkey (TUBITAK) under the project number of 115Z885. the authors gratefully thank TUBITAK for financial support

Synthesis of Some New Ciprofloxacin Hybrids as Potential Antimicrobial Agents

WOS: 000422654000003A new series of ciprofloxacin hybrid compounds as new type of antimicrobial agents were synthesized and evaluated for antibacterial activity against Gram-positive and Gram-negative bacteria

Synthesis and antimicrobial activity evaluation of new norfloxacine-azole hybrids

WOS: 000451322900006Norfloxacin-azole hybrids 3 and 6a,b were synthesized starting from norfloxacin. The treatment of these compounds with amines as a one-pot three-component reaction produced the corresponding amino derivatives 4a,b, 7a-g and 8a,b in good yields. The conventional and microwave-assisted methods were used with the latter method being more efficient. The structures of the synthesized compounds were characterized by elemental analysis, IR, H-1 NMR, C-13 NMR and MS. All compounds were screened for their antimicrobial activities. Most of them exhibit excellent antibacterial activity but are not active against selected fungi

Novel Azole-Functionalited Flouroquinolone Hybrids: Design, Conventional and Microwave Irradiated Synthesis, Evaluation as Antibacterial and Antioxidant Agents

WOS: 000423790800007Background: The synthesis of new hybrid molecules consisting of several heterocyclic pharmacophores namely fluoroquinolone, 1,2,4-triazole, 1,3,4-oxadiazole and piperazine was carried out by conventional and successfully optimized microwave mediated techniques. Methods: The structures of new compounds were confirmed using spectroscopic techniques. These compounds were screened for their antibacterial activity against E. coli, P. aeruginosa, Y. pseudotuberculosis, S. aureus, E. faecalis, B. cereus and M. smegmatis. Results and Conclusion: Fourteen of these hybrids exhibited excellent antibacterial activities on the test microorganisms when compared with ampicillin with the mic values varying between 0.03-0.25 mu g/mL.Scientific and Technological Research Council of Turkey (TUBITAK)Turkiye Bilimsel ve Teknolojik Arastirma Kurumu (TUBITAK) [113Z181]; Karadeniz Technical University, BAP, TurkeyKaradeniz Teknik University [8623]The support provided by Scientific and Technological Research Council of Turkey (TUBITAK, Project no: 113Z181) and Karadeniz Technical University, BAP, Turkey (Ref. No. 8623) is greatly appreciated

Microwave Assisted Synthesis and Antimicrobial Activity Evaluation of New Heterofunctionalized Norfloxacine Derivatives

WOS: 000389464700011The synthesis of new hybrid compounds containing several heterocyclic groups namely norfloxacine, 1,2,4-triazole, 1,3,4-oxadiazole, piperazine, morpholine, thiomorpholine, 1,3,4-thiadiazole etc. was performed by conventional and successfully optimized microwave assisted techniques. The effect of acid catalyst on one pot tricomponent Mannich reaction was investigated as well. The structures of newly synthesized compounds were eluciated on the basis of spectroscopic techniques. Also, the synthesized compounds were screened for their antimicrobial activities and most of them were found to possess good-moderate antimicrobial activity.Scientific and Technological Research Council of Turkey (TUBITAK)Turkiye Bilimsel ve Teknolojik Arastirma Kurumu (TUBITAK) [111T427, 113Z181]; Karadeniz Technical University, BAP, TurkeyKaradeniz Teknik University [8663]The support provided by Scientific and Technological Research Council of Turkey (TUBITAK, Project no: 111T427 and 113Z181) and Karadeniz Technical University, BAP, Turkey (Ref. no. 8663) and is gratefully acknowledged

Anticancer activities of novel Mannich bases against prostate cancer cells

demirci, serpil/0000-0002-6579-4273WOS: 000489305700012This study was designed to synthesize hybridizing molecules starting from compound of 6-(4-phenyl-piperazin-1-yl)pyridine-3-ylamine by enhancing its biological activity with other heterocycles and to determine anticancer activity of the resulting compounds. To this end, 6-(4-phenylpiperazin-1-yl)pyridin-3-ylamine (4) was used as the leading compound, which is known to exert anticancer activities. The synthesis of the leading compound was carried out using 1-(5-nitropyridin-2-yl)-4-phenylpiperazine (3) which was obtained by a novel method with the reaction of N-phenylpiperazine (2) and 2-chloro-5-nitropyridine. 6-(4-phenylpiperazin-1-yl)pyridin-3-ylamine (4) was converted to compound 5, an active intermediate compound, by substitution of one of the amine hydrogens with ethyl bromoacetate. The resulting ester product (5) followed by the hydrazidation (6) was added arylisocyanate to obtain the active intermediate (8). Then, by a series of substitution through cyclization and condensation reactions, thiazolidinone (9), 1,3,4-oxadiazole (7), and 1,2,4-triazole (10) were synthesized. Novel Mannich bases (11a-11f and 12a-12f) were obtained using oxazole (7) and triazole (10) hetero rings with primer or secondary amine compounds. The characterization of the compounds was completed using FT IR, H-1-NMR, C-13-NMR, HRMS spectroscopic methods and elemental analysis technique. The chemicals, then, were tested for their anticancer activities against prostate cancer cell lines PC3 [ATCC, CRL-1435], LNCaP [ATCC, CRL-1740], and DU145 [ATCC, HTB-81]. The results revealed that the Mannich bases exhibited moderate cytotoxic activity against cancer cells tested.Scientific and Technological Research Council of Turkey (TUBITAK)Turkiye Bilimsel ve Teknolojik Arastirma Kurumu (TUBITAK) [116Z932]The support provided by Scientific and Technological Research Council of Turkey (TUBITAK, Project no: 116Z932) is gratefully acknowledged. We thank to Selami Demirci for his help in paper editing

Mortality analysis of COVID-19 infection in chronic kidney disease, haemodialysis and renal transplant patients compared with patients without kidney disease: A nationwide analysis from Turkey

© The Author(s) 2020.Background. Chronic kidney disease (CKD) and immunosuppression, such as in renal transplantation (RT), stand as one of the established potential risk factors for severe coronavirus disease 2019 (COVID-19). Case morbidity and mortality rates for any type of infection have always been much higher in CKD, haemodialysis (HD) and RT patients than in the general population. A large study comparing COVID-19 outcome in moderate to advanced CKD (Stages 3-5), HD and RT patients with a control group of patients is still lacking. Methods. We conducted a multicentre, retrospective, observational study, involving hospitalized adult patients with COVID-19 from 47 centres in Turkey. Patients with CKD Stages 3-5, chronic HD and RT were compared with patients who had COVID-19 but no kidney disease. Demographics, comorbidities, medications, laboratory tests, COVID-19 treatments and outcome [in-hospital mortality and combined in-hospital outcome mortality or admission to the intensive care unit (ICU)] were compared. Results. A total of 1210 patients were included [median age, 61 (quartile 1-quartile 3 48-71) years, female 551 (45.5%)] composed of four groups: Control (n = 450), HD (n = 390), RT (n = 81) and CKD (n = 289). The ICU admission rate was 266/ 1210 (22.0%). A total of 172/1210 (14.2%) patients died. The ICU admission and in-hospital mortality rates in the CKD group [114/289 (39.4%); 95% confidence interval (CI) 33.9-45.2; and 82/289 (28.4%); 95% CI 23.9-34.5)] were significantly higher than the other groups: HD = 99/390 (25.4%; 95% CI 21.3-29.9; P<0.001) and 63/390 (16.2%; 95% CI 13.0-20.4; P<0.001); RT = 17/81 (21.0%; 95% CI 13.2-30.8; P = 0.002) and 9/81 (11.1%; 95% CI 5.7-19.5; P = 0.001); and control = 36/450 (8.0%; 95% CI 5.8-10.8; P<0.001) and 18/450 (4%; 95% CI 2.5-6.2; P<0.001). Adjusted mortality and adjusted combined outcomes in CKD group and HD groups were significantly higher than the control group [hazard ratio (HR) (95% CI) CKD: 2.88 (1.52- 5.44); P = 0.001; 2.44 (1.35-4.40); P = 0.003; HD: 2.32 (1.21- 4.46); P = 0.011; 2.25 (1.23-4.12); P = 0.008), respectively], but these were not significantly different in the RT from in the control group [HR (95% CI) 1.89 (0.76-4.72); P = 0.169; 1.87 (0.81-4.28); P = 0.138, respectively]. Conclusions. Hospitalized COVID-19 patients with CKDs, including Stages 3-5 CKD, HD and RT, have significantly higher mortality than patients without kidney disease. Stages 3-5 CKD patients have an in-hospital mortality rate as much as HD patients, which may be in part because of similar age and comorbidity burden. We were unable to assess if RT patients were or were not at increased risk for in-hospital mortality because of the relatively small sample size of the RT patients in this study