- DNA cleavage, antimicrobial, spectroscopic and fluorescence studies of Co(II), Ni(II) and Cu(II) complexes with SNO donor coumarin Schiff bases
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A series of Co(II), Ni(II) and Cu(II) complexes of the type ML2 have been synthesized with Schiff bases derived from methylthiosemicarbazone and 5-formyl-6-hydroxy coumarin/8-formyl-7-Hydroxy-4-methylcoumarin. The complexes are insoluble in common organic solvents but soluble in DMF and DMSO. The measured molar conductance values in DMF indicate that, the complexes are non-electrolytes in nature. In view of analytical, spectral (IR, UV-vis, ESR, FAB-mass and fluorescence), magnetic and thermal studies, it has been concluded that, all the metal complexes possess octahedral geometry in which ligand is coordinated to metal ion through azomethine nitrogen, thione sulphur and phenolic oxygen atom via deprotonation. The redox behavior of the metal complexes was investigated by using cyclic voltammetry. The Schiff bases and their complexes have been screened for their antibacterial (Escherichia coli, Staphylococcus aureus, Pseudomonas aeruginosa and Salmonella typhi) and antifungal activities (Aspergillus niger, Aspergillus flavus and Cladosporium) by Minimum Inhibitory Concentration method. The DNA cleavage is studied by agarose gel electrophoresis method.
- Patil, Sangamesh A.,Naik, Vinod H.,Kulkarni, Ajaykumar D.,Badami, Prema S.
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Read Online
- Insight on a new indolinone derivative as an orally bioavailable lead compound against renal cell carcinoma
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A series of novel 3-indolinone-thiazolidinones and oxazolidinones 4a-k was synthesized via molecular hybridization approach and sequentially evaluated to explore its cytotoxic activity. The cytotoxicity screening pointed toward the N-cyclohexyl thiazolidinone derivative 4f that revealed promising renal cytotoxicity against CAKI-1 and UO-31 renal cancer cell lines with IC50 values 4.74 and 3.99 μM, respectively, which were comparable to those of sunitinib along with good safety threshold against normal renal cells. Further emphasis on compound 4f renal cytotoxicity was achieved via different enzyme assays and CAKI-1 and UO-31 cell cycle analysis. The results were supported by in silico studies to explore its physicochemical, pharmacokinetic and drug-likeness properties. Finally, compound 4f was subjected to an in vivo pharmacokinetic study through two different routes of administration showing excellent oral bioavailability. This research represents compound 4f as a promising candidate against renal cell carcinoma.
- Fouad, Marwa A.,Zaki, Mayssoune Y.,Lotfy, Raghda A.,Mahmoud, Walaa R.
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- Preparation process of 4-methylthiosemicarbazide
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The invention relates to a preparation process of 4-methylthiosemicarbazide, and belongs to the technical field of pharmaceutical chemicals. The preparation method comprises the following steps: adding hydrazine hydrate into a reaction bottle, dropwise adding carbon disulfide at 20-25 DEG C for 2-3 hours, and keeping the temperature at 20-25 DEG C for 1-2 hours after dropwise adding is finished; controlling the temperature to be 25-30 DEG C, dropwise adding monomethylamine into the reaction bottle for 1-2 hours, introducing nitrogen at the temperature of 70-75 DEG C after dropwise adding is finished, performing refluxing for 1-2 hours, and blowing off hydrogen sulfide gas generated by the reaction; and performing cooling to 0-5 DEG C, performing filtering to obtain an MTSC wet product, carrying out vacuum drying at 55 DEG C for 3 hours, performing heating to 70 DEG C, carrying out vacuum drying for 2-3 hours, and controlling the moisture content to be less than 0.1% to obtain white crystal powder 4-methylthiosemicarbazide. The preparation process is scientific and reasonable in design, wide in raw material source, low in cost, simple in step, green and pollution-free, improves theproduction efficiency, and is beneficial to industrial production.
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Paragraph 0016; 0028-0045
(2020/06/16)
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- A novel 8-nitro quinoline-thiosemicarbazone analogues induces G1/S & G2/M phase cell cycle arrest and apoptosis through ROS mediated mitochondrial pathway
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A series of novel 8-nitro quinoline-based thiosemicarbazone analogues were synthesized and characterized by various spectroscopic and single crystal X-ray analyses. The potent antitumor effects of synthesized compounds towards the cancer cells were evaluated by MTT assay. Amongst, the compound 3a exhibited the highest inhibitory activity and the compounds 3f and 3b were also showed significant activity. The molecular mechanistic studies of cell death have demonstrated that the treated potent compound 3a induced G1/S & G2/M phase cell cycle arrest and induced apoptosis via mitochondrial dysfunction and increased the production of cytotoxic ROS levels. The RT-PCR gene expression analysis revealed that the cell death induced by activation of caspase-3 dependent intrinsic apoptotic signaling pathway. Further, the molecular binding affinity of compounds with estrogen receptor alpha was calculated by molecular docking studies. Thus, novel 8-nitro quinoline-thiosemicarbazone analogues provide a unique tool for breast cancer therapeutic tactics.
- Arasakumar, Thangaraj,Athimoolam, Shunmuganarayanan,Mohan, Palathurai Subramaniam,Saravanan, Arjunan,Shyamsivappan, Selvaraj,Suresh, Thangaraj,Vivek, Raju
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- Synthesis and characterization of a new series of thiadiazole derivatives as potential anticancer agents
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Cancer is one of the most common causes of death in the world. Despite the importance of combating cancer in healthcare systems and research centers, toxicity in normal tissues and the low efficiency of anticancer drugs are major problems in chemotherapy. Nowadays the aim of many medical research projects is to discover new safer and more effective anticancer agents. 1,3,4-Thiadiazole compounds are important fragments in medicinal chemistry because of their wide range of biological activities, including anticancer activities. The aim of this study was to determine the capacity of newly synthesized 1,3,4-thiadiazole compounds as chemotherapeutic agents. The structures of the obtained compounds were elucidated using 1H-NMR, 13C-NMR and mass spectrometry. Although the thiadiazole derivatives did not prove to be significantly cytotoxic to the tumour tissue cultures, compound 4i showed activity against the C6 rat brain cancer cell line (IC50 0.097 mM) at the tested concentrations.
- ?evik, Ulviye Acar,Osmaniye, Derya,Levent, Serkan,Sa?lik, Begüm Nurpelin,?avu?o?lu, Betül Kaya,?zkay, Yusuf,Kaplancikl, Zafer Aslm
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- Novel Schiff bases derived from isothiocyanates: synthesis, characterization, and antioxidant activity
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A series of novel thiosemicarbazones including Schiff bases were synthesized by treatment of various aryl-substituted aldehydes with thiosemicarbazides in ethanol containing one drop of hydrochloric acid at reflux for 3–5 h. For this, thiosemicarbazides were obtained from hydrazine monohydrate and isothiocyanates in cold dry ethanol at 0 °C for 1 h. FT-IR, 1H NMR, 13C NMR, and LC–MS/MS spectroscopic methods and elemental analysis were used to characterize the identification of the synthesized products. The in vitro antioxidant activity of these compounds was tested by the 1,1-diphenyl-2-picryl hydrazyl (DPPH) free radical trapping method. All of the synthesized compounds showed lower antioxidant activity than the ascorbic acid standard and followed the sequence I > VII > X > VI > IV > IX > XI > II > V > III > VIII.
- Yakan, Hasan
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p. 3979 - 3995
(2020/07/03)
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- Anti-cancer, anti-oxidant and molecular docking studies of thiosemicarbazone indole-based derivatives
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Based on the structural elements of bioactive 3-substituted indoles, a new series of indole–thiosemicarbazone hybrid derivatives were designed, synthesized, and well-characterized using different spectral techniques. The intended scaffolds were screened for their in vitro anti-proliferative activities against breast cancer (MCF-7), lung cancer (A-549), and liver cancer (Hep-G2) cell lines, as well as their anti-oxidant properties. Cytotoxicity studies revealed that compound 6n was the most potent, at least threefold more potent than the commercially available reference drug etoposide, against A-549. In addition, morphological analysis by the acridine orange/ethidium bromide double staining test and flow cytometry analysis confirmed induction of apoptosis in the A-549 cells by compound 6n. In order to validate the experimental results, molecular studies were performed to achieve the possible binding interactions of the most potent compound (6n) and colchicine with tubulin as well as ANP with ATPase domain of topoisomerase IIα active sites. Moreover, the radical scavenging potential of the final derivatives was found to be excellent with the range of 0.015–0.630?μM, comparable to the standard ascorbic acid (0.655?μM).
- Bakherad, Zohreh,Safavi, Maliheh,Fassihi, Afshin,Sadeghi-Aliabadi, Hojjat,Bakherad, Mohammad,Rastegar, Hossein,Ghasemi, Jahan B.,Sepehri, Saghi,Saghaie, Lotfollah,Mahdavi, Mohammad
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p. 2827 - 2854
(2019/03/13)
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- Inhibitory properties of aromatic thiosemicarbazones on mushroom tyrosinase: Synthesis, kinetic studies, molecular docking and effectiveness in melanogenesis inhibition
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The group of 19 thiosemicarbazones (TSCs) were synthesized and its inhibitory activity toward mushroom tyrosinase and ability to inhibition of melanogenesis in B16 cells were investigated. Moreover, molecular docking of these compounds to the active site of the enzyme was performed. The obtained results allowed to make the structure-activity relationship (SAR) analysis. Kinetic studies revealed that TSCs 1, 2, 11 and 18 have better inhibitory properties than kojic acid, a reference compound, with the best inhibitory constant (Ki) value of 0.38 μM for TSC 2. According to SAR analysis, the smaller and less branched molecules exhibit higher affinity to the enzyme. Melanin production in B16 cells was inhibited by all investigated compounds at micromolar level. Most of compounds studied in this work can be considered as potent inhibitors of tyrosinase and melanogenesis. They may have broad application in food preservatives and cosmetics. Combined results of molecular docking and SAR analysis can be helpful in designing novel tyrosinase inhibitors of desired properties.
- Ha?dys,Goldeman,Jewgiński,Wolińska,Anger,Rossowska,Latajka
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p. 577 - 586
(2018/09/29)
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- Isatin thiazoline hybrids as dual inhibitors of HIV-1 reverse transcriptase
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A series of 3-3-{2-[2-3-methyl-4-phenyl-2,3-dihydro-1,3-thiazol-2-ylidene]hydrazin-1-ylidene-2,3-dihydro-1H-indol-2-one derivatives has been designed and synthesized to study their activity on both HIV-1 (Human Immunodeficiency Virus type 1) RT (Reverse Transcriptase) associated functions. These derivatives are analogs of previously reported series whose biological activity and mode of action have been investigated. In this work we investigated the influence of the introduction of a methyl group in the position 3 of the dihydrothiazole ring and of a chlorine atom in the position 5 of the isatin nucleus. The new synthesized compounds are active towards both DNA polymerase and ribonuclease H in the μM range. The nature of the aromatic group in the position 4 of the thiazole was relevant in determining the biological activity.
- Meleddu, Rita,Distinto, Simona,Bianco, Giulia,Melis, Claudia,Cottiglia, Filippo,Maccioni, Elias,Corona, Angela,Tramontano, Enzo
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p. 130 - 136
(2017/11/30)
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- Three nitrogen heterocycle containing 1, 2, 3 - thiadiazole - 5 - a amidine compounds and synthesis
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The invention discloses an N-trisubstituted-1,2,3-thiadiazole-5-formamidine compound with three aromatic rings of general formula TDCA and a synthesis method of N-trisubstituted-1,2,3-thiadiazole-5-formamidine compound. The target compound of general formula TDCA is obtained by reacting a compound of general formula B and a compound of general formula A, wherein references of X and Y in the general formula A are the same as those in the general formula TDCA.
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Paragraph 0071; 0072; 0073
(2017/08/25)
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- Methyl thiosemicarbazide synthesis process
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The invention discloses a methylthiosemicarbazide synthesis process comprising the following steps: thiourea is dissolved in a solvent; a catalyst is added, and the temperature is increased to 10-200 DEG C under stirring; methyl chloride gas is delivered and a reaction is allowed; when the reaction is finished, nitrogen gas is delivered for purging residual hydrogen chloride gas; hydrazine hydrate is dropped in under a temperature of 30-90 DEG C, and a reaction is carried out; when the reaction is finished, the solvent is distillated; the temperature is reduced to -10 DEG C to 50 DEG C, and a solid material is obtained by filtration; and drying is carried out, such that methylthiosemicarbazide is obtained.
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Paragraph 0013; 0014; 0015; 0016; 0017; 0018; 0019; 0020
(2017/08/25)
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- 3-[(E)-(acridin-9′-ylmethylidene)amino]-1-substituted thioureas and their biological activity
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This paper describes the synthesis of a novel series of acridine thiosemicarbazones through a two-step reaction between various isothiocyanates and hydrazine followed by treatment with acridin-9-carbaldehyde. The properties of this series of seven new derivatives are studied using NMR and biochemical techniques, and the DNA-binding properties of the compounds are determined using spectrophotometric studies (UV–vis absorption, fluorescence, and circular/linear dichroism) and viscometry. The binding constants K are estimated as being in the range of 2.2 to 7.8?×?104?M??1 and the percentage of hypochromism was found to be 22.11–49.75% (from UV–vis spectral titration). Electrophoretic experiments prove that the novel compounds demonstrate moderate inhibitory effects against Topo I activity at a concentration of 60?×?10??6?M.
- Be?ka, Michal,Vilková, Mária,Salem, Othman,Ka?párková, Jana,Brabec, Viktor,Ko?urková, Mária
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p. 234 - 241
(2017/03/23)
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- Unexpected formation of 4-alkyl-5-(4-alkylthiosemicarbazido)-4,5-dihydro-1, 2,4-triazine-3(2H)-thiones from 1,3-dialkyl-4,5-bis-(4-alkylthiosemicarbazido) imidazolidin-2-ones in acidic medium
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4-Alkyl-5-(4-alkylthiosemicarbazido)-4,5-dihydro-1,2,4-triazine-3(2H) -thiones are obtained either by heating 1,3-dialkyl-4,5-bis-(4- alkylthiosemicarbazido)imidazolidin-2-ones in acidic medium or the reaction of 1,3-dialkyl-4,5-dihydroxyimidazolidin-2-on
- Gazieva, Galina A.,Poluboyarov, Pavel A.,Kolotyrkina, Natal'ya G.,Lubuzh, Elena D.,Kravchenko, Angelina N.
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- Isatin-β-thiosemicarbazones as potent herpes simplex virus inhibitors
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A series of isatin-β-thiosemicarbazones have been designed and evaluated for antiviral activity against herpes simplex virus type 1 (HSV-1) and type 2 (HSV-2) in a plaque reduction assay. Their cytotoxicity was examined using human rhabdomyosarcoma cells (RD cells). Several derivatives of isatin-β-thiosemicarbazone exhibited significant and selective antiviral activity with low cytotoxicity. It was found that the thiourea group at thiosemicarbazone and the NH functionality at isatin were essential for their antiherpetic activity. The synthesis and structure-activity relationship studies are presented.
- Kang, Iou-Jiun,Wang, Li-Wen,Hsu, Tsu-An,Yueh, Andrew,Lee, Chung-Chi,Lee, Yen-Chun,Lee, Ching-Yin,Chao, Yu-Sheng,Shih, Shin-Ru,Chern, Jyh-Haur
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scheme or table
p. 1948 - 1952
(2011/05/04)
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- Synthesis of new hyodeoxycholic acid thiosemicarbazone derivatives under solvent-free conditions using microwave
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An efficient and simple method for synthesis of new hyodeoxycholic acid thiosemicarbazone derivatives under solvent-free conditions using microwave has been developed. Its main advantages are short reaction times, good conversions and the environmentally friendly nature of the process. The preliminary results indicate that some of these compounds possess inhibitory effects against E. coli.
- Shi, Zhi Chuan,Zhao, Zhi Gang,Liu, Xing Li,Chen, Yu
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experimental part
p. 405 - 408
(2012/01/05)
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- α-Thioureidoalkylation of 4-alkyl- and 4-phenylthiosemicarbazides
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Previously unknown 1,3-dialkyl-4,5-bis[4-alkyl(phenyl)thiosemicarbazido] imidazolidine-2-thiones and 4,5,7-trialkylperhydroimidazo[4,5-e]-1,2,4-triazine- 3,6-dithiones have been synthesized by the α-thio-ureidoalkylation of 4-alkyl(phenyl)thiosemicarbazides using 1,3-dialkyl-4,5-dihydroxyimidazolidine- 2-thiones.
- Gazieva,Struchkova,Kolotyrkina
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experimental part
p. 210 - 214
(2011/12/21)
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- Spectroscopic, DNA cleavage and antimicrobial studies of Co(II), Ni(II) and Cu(II) complexes of sulfur donor schiff bases
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A series of Co(II), Ni(II) and Cu(II) complexes of the type ML2 of Schiff bases derived from methylthiosemicarbazide and isatin/chloroisatin have been synthesized. Schiff bases exhibit thiol-thione tautomerism wherein sulfur plays an important role in the coordination. In view of analytical, spectral (IR, NMR, UV-vis, ESR, FAB-Mass) and magnetic studies, it has been concluded that all the metal complexes possess octahedral geometry. The measured molar conductance values in DMF indicate that the complexes are non-electrolytes in nature. The redox behaviors of the metal complexes are investigated by using cyclic voltammetry. The Schiff bases and their metal complexes have been screened for their antibacterial (Escherichia coli, Staphylococcus aureus, Pseudomonas aeruginosa and Salmonella typhi) and antifungal activities (Aspergillus niger, Aspergillus flavus and Cladosporium) by the minimum inhibitory concentration method. The DNA cleavage studies showed the cleavage of DNA by the agarose gel electrophoresis method.
- Patil, Sangamesh A.,Naik, Vinod H.,Kulkarni, Ajaykumar D.,Badami, Prema S.
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experimental part
p. 109 - 121
(2010/11/05)
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- Solvent-free synthesis of indole-based thiosemicarbazones under microwave irradiation
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A rapid, effi cient and environmentally friendly methodology has been developed for the synthesis of indole-3-carboxaldehyde thiosemicarbazones by using aluminum oxide as the solid support under microwave assisted solvent-free conditions. Compared with the conventional heating method, this method gave the target products in good yield.
- Liu, Lingling,Yang, Jie,Zhao, Zhigang,Shi, Peiyu,Liu, Xingli
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experimental part
p. 57 - 60
(2010/05/19)
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- Synthesis and characterization of new thiazolidin-4-one derivatives
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The synthesis of some new functionalized thiazolidin-4-one derivatives has been described. The N-substituted-thiosemicarbazides 3a-3i were obtained though the reaction of alkylamines 2a-2i, carbon disulfide, and hydrazine hydrate. The condensation reaction between 3a-3i and 4-amino-2-methanesulfanylpyrimidine-5- carboxaldehyde 1 afforded the thiosemicarbazones 4a-4i. The corresponding thiazolidin-4-ones 5a-5i were prepared by cyclization of 4a-4i with ethyl bromoacetate. The structures of the final products were confirmed by IR, 1H NMR, 13C NMR, and HRMS.
- Hu, Bao Xiang,Shen, Zhen Lu,Lu, Jun,Hu, Xin Quan,Mo, Wei Min,Sun, Nan,Xu, Dong
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experimental part
p. 523 - 535
(2009/09/25)
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- Thiosemicarbazones active against Clostridium difficile
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A set of closely related furylidene thiosemicarbazones was prepared and screened against various clinically important Gram-positive bacteria. One compound containing an ethylene spacer and a 5-nitrofuryl group was found to have promising activity against Clostridium difficile.
- Costello, Cait,Karpanen, Tarja,Lambert, Peter A.,Mistry, Preena,Parker, Katy J.,Rathbone, Daniel L.,Ren, Jiangmeng,Wheeldon, Laura,Worthington, Tony
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p. 1708 - 1711
(2008/09/19)
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- Synthesis and antituberculosis activity of 5-methyl/trifluoromethoxy-1H-indole-2,3-dione 3-thiosemicarbazone derivatives
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New series of 5-methyl/trifluoromethoxy-1H-indole-2,3-dione 3-thiosemicarbazones 3a-t, 1-methyl-5-methyl/trifluoromethoxy-1H-indole-2,3-dione 3-thiosemicarbazones 4a-y and 5-trifluoromethoxy-1-morpholinomethyl-1H-indole-2,3-dione 3-thiosemicarbazones 5a-m were synthesized. The structures of the synthesized compounds were confirmed by spectral data and elemental analysis. The new 5-methyl/trifluoromethoxy-1H-indole-2,3-dione derivatives, along with previously synthesized 5-methyl-1H-indole-2,3-dione 3-thiosemicarbazones 6a-l, were evaluated for in vitro antituberculosis activity against Mycobacterium tuberculosis H37Rv. 5-Methyl-1H-indole-2,3-dione 3-thiosemicarbazones (3b, 3d, 3f, 6c, 6d, and 6f), 5-trifluoromethoxy-1H-indole-2,3-dione 3-thiosemicarbazones (3q-s) and 5-trifluoromethoxy-1-morpholinomethyl-1H-indole-2,3-dione 3-thiosemicarbazones (5e and 5j-l) were found to be the most potent inhibitors of M. tuberculosis growth described in this study.
- Guezel, Oezlen,Karali, Nilguen,Salman, Aydin
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experimental part
p. 8976 - 8987
(2009/04/11)
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- Synthesis and structure-antituberculosis activity relationship of 1H-indole-2,3-dione derivatives
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New series of 5-fluoro-1H-indole-2,3-dione-3-thiosemicarbazones 2a-k and 5-fluoro-1-morpholino/piperidinomethyl-1H-indole-2,3-dione-3-thiosemicarbazones 3a-r were synthesized. The structures of the synthesized compounds were confirmed by spectral data, elemental and single crystal X-ray diffraction analysis. The new 5-fluoro-1H-indole-2,3-dione derivatives, along with previously reported 5-nitro-1H-indole-2,3-dione-3-thiosemicarbazones 2l-v, 1-morpholino/piperidinomethyl-5-nitro-1H-indole-2,3-dione-3-thiosemicarbazones 4a-l, and 5-nitro-1H-indole-2,3-dione-3-[(4-oxo-1,3-thiazolidin-2-ylidene)hydrazones] 5a-s, were evaluated for in vitro antituberculosis activity against Mycobacterium tuberculosis H37Rv. Among the tested compounds, 5-nitro-1H-indole-2,3-dione-3-thiosemicarbazones (2p, 2r, and 2s) and its 1-morpholinomethyl derivatives (4a, 4e, 4g, and 4i) exhibited significant inhibitory activity in the primary screen. The antituberculosis activity of molecules with diverse skeletons was investigated by means of the Electronic-Topological Method (ETM). Ten pharmacophores and ten anti-pharmacophores that have been found by this form the basis of the system capable of predicting the structures of potentially active compounds. The forecasting ability of the system has been tested on structures that differ from those synthesized. The probability of correct identification for active compounds was found as equal to 93% in average. To obtain the algorithmic base for the activity prediction, Artificial Neural Networks were used after the ETM (the so-called combined ETM-ANN method). As the result, only 9 pharmacophores and anti-pharmacophores were chosen as the most important ones for the activity. By this, ANNs classified correctly 94.4%, or 67 compounds from 71.
- Karali, Nilguen,Guersoy, Aysel,Kandemirli, Fatma,Shvets, Nathaly,Kaynak, F. Betuel,Oezbey, Sueheyla,Kovalishyn, Vasyl,Dimoglo, Anatholy
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p. 5888 - 5904
(2008/03/18)
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- Synthesis and antitumor activity of new thiosemicarbazones of 2-acetylimidazo[4,5-b]pyridine
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A number of thiosemicarbazones of 2-acetyl-imidazo[4,5-b]pyridine were prepared in order to investigate their in vitro antineoplastic activities. Three compounds: (i) 2-acetylimidazo[4,5-b]pyridin-4-tert-butyl-3-thiosemicarbazone [(A7), NSC674098], (ii) 2-acetylimidazo[4,5-e]pyridin-4-tert-butyl-3- thiosemicarbazone [(A9), NSC674099], (iii) 2-acetylimidazo[4,5-i] pyridin-4-cyclohexyl-3-thiosemicarbozone [(A11), NSC674101] showed remarkable activity against some of the cell lines tested. The Biological Evaluation Committee of N.C.I, determined that further secondary testing should be carried out (these compounds were tested against prostate cancer).
- Mylonas, Stavros,Mamalis, Athanasios
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p. 1273 - 1281
(2007/10/03)
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- Synthesis, anticancer and antibacterial activity of some novel mononuclear Ru(II) complexes
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In search of potential anticancer drug candidates in ruthenium complexes, a series of mononuclear ruthenium complexes of the type [Ru(phen) 2(nmit)]Cl2 (Ru1), [Ru(bpy)2(nmit)]Cl 2 (Ru2), [Ru(phen)2(icpl)]Cl2 (Ru3), Ru(bpy)2(icpl)]Cl2 (Ru4) (phen51,10-phenanthroline; bpy=2,2′-bipyridine; nmit=N-methyl-isatin-3-thiosemicarbazone, icpl=isatin-3-(4-Cl-phenyl)thiosemicarbazone) and [Ru(phen)2(aze)] Cl2 (Ru5), [Ru(bpy)2(aze)]Cl2 (Ru6) (aze=acetazolamide) and [Ru(phen)2(R-tsc)](ClO4) 2 (R=methyl (Ru7), ethyl (Ru8), cyclohexyl (Ru9), 4-Cl-phenyl (10), 4-Br-phenyl (Ru11), and 4-EtO-phenyl (Ru12), tsc=thiosemicarbazone) were prepared and characterized by elemental analysis, FTIR, 1H-NMR and FAB-MS. Effect of these complexes on the growth of a transplantable murine tumor cell line (Ehrlich Ascites Carcinoma) and their antibacterial activity were studied. In cancer study the effect of hematological profile of the tumor hosts have also been studied. In the cancer study, the complexes Ru1-Ru4, Ru10 and Ru11 have remarkably decreased the tumor volume and viable ascitic cell count as indicated by trypan blue dye exclusion test (p0.05). Treatment with the ruthenium complexes prolonged the lifespan of Ehrlich Ascites Carcinoma (EAC) bearing mice. Tumor inhibition by the ruthenium chelates was followed by improvements in hemoglobin, RBC and WBC values. All the complexes showed antibacterial activity, except Ru5 and Ru6. Thus, the results suggest that these ruthenium complexes have significant antitumor property and antibacterial activity. The results also reflect that the drug does not adversely affect the hematological profiles as compared to that of cisplatin on the host.
- Mazumder, Upal Kanti,Gupta, Malaya,Karki, Subhas Somalingappa,Bhattacharya, Shiladitya,Rathinasamy, Suresh,Thangavel, Sivakumar
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p. 178 - 185
(2007/10/03)
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- Process for the preparation of triazolinones
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The invention relates to a new process and new intermediates for the preparation of triazolinones of the general formula (I) STR1 in which R1 represents in each case optionally substituted alkyl or cycloalkyl and R2 represents amino or in each case optionally substituted alkyl, alkenyl, alkinyl, alkoxy, alkylamino, dialkylamino, cycloalkyl, cycloalkylalkyl or phenyl, and to new intermediates for the preparation of triazolinones, many of which are known and which can be used as intermediates for the preparation of herbicides and insecticides.
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- Process for the production of 2-amino-5-mercapto-1,3,4-thiadiazole
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2-Amino-5-mercapto-1,3,4-thiadiazoles can be produced in very high yields from thiosemicarbazides and carbon disulfide in aqueous phase by working in the presence of the corresponding ammonium salt of bis-2,5-mercapto-1,3,4-thiadiazole at a temperature above 40° C. Preferably the process is carried out in the presence of the mother liquor from a previous reaction.
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- Preparation of lower alkyl thiosemicarbazides
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A process for the production of a lower alkyl-thiosemicarbazide comprising steam distilling an aqueous solution containing hydrazine and an N-lower alkyl-dithiocarbamic acid quaternary ammonium salt thereby to effect pyrolysis while distilling off water, lower alkyl amine and hydrogen sulfide, and cooling the distilland to form crystals of the lower alkylthiosemicarbazide. Advantageously the solution is obtained by reacting carbon disulfide and methylamine in water, followed by addition of hydrazine.
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