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1.
Hong‐Yu Liang Deng‐Qing Zhang Yun Yue Zhe Shi Sheng‐Yin Zhao 《Archiv der Pharmazie》2010,343(2):114-119
A series of 1,3‐dihydro‐2H‐3‐benzazepin‐2‐ones with a piperazine moiety were designed and synthesized by treating the common intermediate of 1,3‐dihydro‐7,8‐dimethoxy‐3‐[3‐(1‐piperazinyl)propyl]‐2H‐3‐benzazepin‐2‐ones with a variety of N‐aryl‐2‐chloroacetamides and acyl chlorides. Their structures have been characterized by 1H‐NMR, MS, and elemental analysis. The title compounds were evaluated for their bradycardic activity in vitro. Most of the synthesized compounds exhibited some vasorelaxant activity and heart‐rate‐reducing activity with bradycardic potency. 相似文献
2.
《Journal of labelled compounds & radiopharmaceuticals》2017,60(1):49-54
Tetrazoles are a common heterocyclic functionality in many biologically active molecules. [1‐14C]2‐(1H‐Tetrazol‐5‐yl)acetic acid was required as an intermediate in the synthesis of a development candidate as part of a discovery phase program to complete metabolic profiling studies. [1‐14C]2‐(1H‐Tetrazol‐5‐yl)acetic acid was prepared in 4 steps overall and in 3 radiochemical steps from K14CN in an overall 32% radiochemical yield. 相似文献
3.
Design,Synthesis, and Antitumor Activity of (E,Z)‐1‐(dihydrobenzofuran‐5‐yl)‐3‐phenyl‐2‐(1,2,4‐triazol‐1‐yl)‐2‐propen‐1‐ones 下载免费PDF全文
Wan Li Zi‐Hui Yang Ai‐Xi Hu Xiao‐Wei Yan Na Ding Jiao Ye 《Chemical biology & drug design》2015,86(6):1339-1350
A series of (E,Z)‐1‐(dihydrobenzofuran‐5‐yl)‐3‐phenyl‐2‐(1,2,4‐triazol‐1‐yl)‐2‐propen‐1‐ones ( C1 – C35 ) were designed and synthesized, and the structures of compounds (Z)‐ C27 and (Z)‐ C29 were confirmed by single‐crystal X‐ray diffraction. The antitumor activities of these novel compounds against cervical cancer (HeLa), lung cancer (A549), and breast cancer (MCF‐7) cell lines were evaluated in vitro. Majority of the title compounds exhibited strong antitumor activities and were much more promising than the positive control Taxol, which were also accompanied by lower cytotoxicity to normal cells. In particular, compounds (E,Z)‐ C24 exhibited the most consistent potent activities against three neoplastic cells with IC50 values ranging from 3.2 to 7.1 μm . Further researches demonstrated that compounds (E,Z)‐ C24 could induce cell apoptosis and arrest cell cycle at the G2/M and S phases. Meanwhile, the structure–activity relationship between the configurations and cytotoxicity of the compounds was also investigated. 相似文献
4.
Saeed Emami Alireza Foroumadi Nasrin Samadi Mohammad A. Faramarzi Saeed Rajabalian 《Archiv der Pharmazie》2009,342(7):405-411
A series of novel quinolone agents bearing a particular bulky and conformationally constrained bicyclic substituent (2,3‐dihydro‐4‐hydroxyimino‐4H‐1‐benzopyran‐3‐yl‐ moiety) on the piperazine ring of 7‐piperazinyl quinolones (norfloxacin, enoxacin, ciprofloxacin, and levofloxacin) were synthesized and evaluated against a panel of Gram‐positive and Gram‐negative bacteria. Among these derivatives, ciprofloxacin counterpart 9c , highly inhibited the tested Gram‐positive bacteria, superior to that of the reference drugs, and displayed antibacterial activity at non‐cytotoxic concentrations. 相似文献
5.
Jixia Yang Gongzheng Zhang Zhaoyang Wang Zhanxiong Xiao Hongliang Wen 《Journal of labelled compounds & radiopharmaceuticals》2019,62(14):920-924
Parkinson disease (PD) is a neurodegenerative disorder characterized by the accumulation of α‐synuclein into Lewy bodies. 3‐Benzylidine‐indolin‐2‐one represents a class of compounds, which are known to inhibit the accumulation of α‐synuclein. In this paper, we report the synthesis of [13C] and [15N] labelled 1‐benzyl‐(Z)‐3‐(benzylidene)indolin‐2‐one from commercially available [13C2]‐chloroacetic acid and [15N]‐aniline in five steps. The product will be used to study its metabolites in human liver microsomes by liquid chromatography‐tandem mass spectrometry. 相似文献
6.
Synthesis,molecular docking,and pharmacological evaluation of N‐(2‐(3,5‐dimethoxyphenyl)benzoxazole‐5‐yl)benzamide derivatives as selective COX‐2 inhibitors and anti‐inflammatory agents 下载免费PDF全文
7.
Braulio Insuasty Alexander Gutiérrez Jairo Quiroga Rodrigo Abonia Manuel Nogueras Justo Cobo Laura Svetaz Marcela Raimondi Susana Zacchino 《Archiv der Pharmazie》2010,343(1):48-53
The present work describes the synthesis and antifungal evaluation of new 5‐arylidene‐(Z)‐2‐dimethylamino‐1,3‐thiazol‐4‐ones 4a – f , obtained by the reaction of aromatic aldehydes 1 and rhodanine 2 followed by treatment with DMF. All compounds were tested against a panel of yeasts, hialohyphomycetes, and dermatophytes using the microbroth dilution method. Compounds 4a and 4c showed antifungal activity, with compound 4a being the most active one. Compound 4a demonstrated to be fungicidal rather than fungistatic and selective activity against Cryptococcus neoformans and dermatophytes. MIC100, MIC80, and MIC50 of 4a were determined against a panel of clinical isolates of C. neoformans showing ranges of MICs between 2 and 16 μg/mL. 相似文献
8.
Discovery of Novel 2‐(piperidin‐4‐yl)‐1H‐benzo[d]imidazole Derivatives as Potential Anti‐Inflammatory Agents 下载免费PDF全文
Xinning Wang Yang Zong Leilei Zhao Junhao Xing Jinpei Zhou Huibin Zhang 《Chemical biology & drug design》2015,86(4):509-516
A novel 2‐(piperidin‐4‐yl)‐1H‐benzo[d]imidazole derivative 5 with good anti‐inflammatory activity was identified from our in‐house library. Based on hit compound 5 , two series of 2‐(piperidin‐4‐yl)‐1H‐benzo[d]imidazole derivative 6a – g and 7a – h were designed and synthesized as novel anti‐inflammatory agents. Most of synthesized compounds exhibited good inhibitory activity on NO and TNF‐α production in LPS‐stimulated RAW 264.7 macrophages, in which the compound 6e showed most potent inhibitory activity on NO (IC50 = 0.86 μm ) and TNF‐α (IC50 = 1.87 μm ) production. Further evaluation revealed that compound 6e displayed more potent in vivo anti‐inflammatory activity than ibuprofen did on xylene‐induced ear oedema in mice. Additionally, Western blot analysis revealed that compound 6e could restore phosphorylation level of IκBα and protein expression of p65 NF‐κB in LPS‐stimulated RAW 264.7 macrophages. 相似文献
9.
Efficient Synthesis of Novel 3‐Aryl‐5‐(4‐chloro‐2‐morpholinothiazol‐5‐yl)‐4,5‐dihydro‐1H‐pyrazoles and Their Antifungal Activity Alone and in Combination with Commercial Antifungal Agents 下载免费PDF全文
Juan Ramírez María Victoria Rodríguez Jairo Quiroga Rodrigo Abonia Maximiliano Sortino Susana A. Zacchino Braulio Insuasty 《Archiv der Pharmazie》2014,347(8):566-575
10.
《Chemical biology & drug design》2018,91(2):526-533
A series of 5‐(4‐(pyridin‐4‐yl)‐1H‐1,2,3‐triazol‐1‐yl)benzonitrile derivatives ( 1a–p ) was designed, synthesized, and identified as xanthine oxidase inhibitors with micromolar level potencies. Among them, the most promising compounds 1j and 1k were obtained with IC50 values of 8.1 and 6.7 μm , respectively. The Lineweaver–Burk plot revealed that compound 1k acted as a mixed‐type xanthine oxidase inhibitor. SAR analysis revealed that a carbon atom occupying the X3 position is not as effective as a nitrogen atom, and an iso‐pentyloxy or a cyclopentyloxy at the 2‐position of benzonitrile moiety will benefit the inhibitory potency. The basis of xanthine oxidase inhibition by 1k was rationalized by molecular modeling studies. 相似文献
11.
Mahesh Palkar Malleshappa Noolvi Ramappa Sankangoud Veeresh Maddi Andanappa Gadad Laxmi Venkat G. Nargund 《Archiv der Pharmazie》2010,343(6):353-359
Benzothiazole and imidazole compounds are extensively studied heterocyclics due to their wide spectrum of bioactivities. Among them, the imidazo(2,1‐b)‐benzothiazole derivatives are pharmacologically important because of their immunostimulant, anti‐inflammatory, antifungal, antimicrobial, antitumor, and other activities. In the present research work, a novel series of 2,3‐diaryl‐substituted imidazo(2,1‐b)‐benzothiazoles 13a–o have been synthesized by reaction of substituted 2‐aminobenzothiazoles 1–8 and an appropriately substituted α‐bromo‐1‐(4′′‐substituted)‐phenyl‐2‐(4′‐substituted)‐phenyl‐1‐ethanones 9–12 in the presence of anhydrous acetonitrile. They were characterized by physicochemical, elemental, and spectral (IR, 1H‐NMR, and Mass) data. All the synthesized compounds were screened for their in‐vitro antibacterial activity against Gram‐positive, Gram‐negative bacteria. The investigation of antibacterial screening data revealed that most of the compounds tested have demonstrated congruent activity against Staphylococcus aureus, Bacillus subtilis, Escherichia coli, and Pseudomonas aeruginosa as compared with the standard ampicillin. Among the series, compounds 13d , 13h , and 13m exhibited excellent an antibacterial activity profile as compared with the standard. In summary, preliminary results indicate that some of the newly synthesized title compounds exhibited promising antibacterial activities and they warrant more consideration as prospective antimicrobials. 相似文献
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Haydar Yüksek Onur Akyıldırım Mehmet L. Yola Özlem Gürsoy‐Kol Mustafa Çelebier Didem Kart 《Archiv der Pharmazie》2013,346(6):470-480
A series of compounds derived from 4,5‐dihydro‐1H‐1,2,4‐triazol‐5‐one were synthesized and characterized by spectral data. The 12 new compounds were analyzed for their potential in vitro antioxidant activities by three different methods. Compound 4f showed the best activity for the iron binding. In addition, the compounds 4 were titrated potentiometrically with tetrabutylammonium hydroxide in non‐aqueous solvents. The RP‐HPLC capacity factors (k′) of the series were also determined on a C18 column, with methanol/water as the mobile phase. The correlation between log k′ with the percentage of methanol in the mobile phase was used for the determination of the log kw values for these compounds. The antimicrobial activities of these compounds were also screened against bacteria and yeast. 相似文献
14.
Lyudmyla Antypenko Zhanar Sadykova Kostiantyn Shabelnyk Fatuma Meyer Sergiy Kovalenko Vera Meyer Leif‐Alexander Garbe Karl Steffens 《Archiv der Pharmazie》2019,352(10)
Due to their high specificity and efficacy, triazoles have become versatile antifungals to treat fungal infections in human healthcare and to control phytopathogenic fungi in agriculture. However, azole resistance is an emerging problem affecting human health as well as food security. Here we describe the synthesis of 10 novel {2‐(3‐R‐1H‐1,2,4‐triazol‐5‐yl)phenyl}amines. Their structure was ascertained by liquid chromatography–mass spectrometry, 1H and 13C NMR, and elemental analysis data. Applying an in vitro growth assay, these triazoles show moderate to significant antifungal activity against the opportunistic pathogen Aspergillus niger, 12 fungi (Fusarium oxysporum, Fusarium fujikuroi, Colletotrichum higginsianum, Gaeumannomyces graminis, Colletotrichum coccodes, Claviceps purpurea, Alternaria alternata, Mucor indicus, Fusarium graminearum, Verticillium lecanii, Botrytis cinerea, Penicillium digitatum) and three oomycetes (Phytophtora infestans GL‐1, P. infestans 4/91; R+ and 4/91; R?) in the concentration range from 1 to 50 µg/ml (0.003–2.1 μM). Frontier molecular orbital energies were determined to predict their genotoxic potential. Molecular docking calculations taking into account six common fungal enzymes point to 14α‐demethylase (CYP51) and N‐myristoyltransferase as the most probable fungal targets. With respect to effectiveness, structure–activity calculations revealed the strong enhancing impact of adamantyl residues. The shown nonmutagenicity in the Salmonella reverse‐mutagenicity assay and no violations of drug‐likeness parameters suggest the good bioavailability and attractive ecotoxicological profile of the studied triazoles. 相似文献
15.
A series of N‐substituted‐1H‐benzimidazole‐5(6)‐sulfonamides and 3‐(5,6‐dichloro‐1H‐benzimidazol‐2‐yl)‐N‐substituted benzensulfonamides were synthesized and evaluated for antibacterial activity against Staphylococcus aureus and methicillin‐resistant S. aureus (MRSA). Certain compounds inhibit bacterial growth with low MIC (μg/mL) values. The most active compounds 30 , 31 , and 32 have the lowest MIC values with 0.39 to 0.19 μg/mL. Among the compounds having sulfonamido moities, 16 , 23 , and 24 exhibited the strongest antibacterial activity with 1.56 μg/mL MIC values. 相似文献
16.
《Journal of labelled compounds & radiopharmaceuticals》2005,48(8):621-627
N‐[1‐(4‐chlorophenyl)‐1H‐pyrrol‐2‐yl‐13C4‐methyleneamino]guanidinium acetate has been synthesized by a four‐step procedure. This involved reduction of the Weinreb amide N,N′‐dimethyl‐N,N′‐dimethyloxybutane‐1,4‐diamide‐1,2,3,4‐13C4 by Dibal‐H to give the corresponding unstable dialdehyde which is reacted in situ with 4‐chloroaniline to form 1‐(4‐chlorophenyl)‐1H‐pyrrole‐13C4. This pyrrole analogue underwent a Vilsmeyer acylation with POCl3/DMF followed by final reaction with aminoguanidine bicarbonate to produce the desired labelled compound with 99% atom 13C. By using DMF [α‐14C] a radio‐labelled analogue was synthesized with a specific activity of 60 mCi/mmol. Copyright © 2005 John Wiley & Sons, Ltd. 相似文献
17.
Mohammed Iqbal A. Khazi Ningaraddi S. Belavagi Kwang R. Kim Young‐Dae Gong Imtiyaz Ahmed M. Khazi 《Chemical biology & drug design》2013,82(2):147-155
A novel series of 5‐(2‐alkyl/aryl‐6‐arylimidazo[2,1‐b][1,3,4]thiadiazol‐5‐yl)methylene‐1,3‐thiazolidinediones were synthesized as possible PPARγ agonists. The structures of these target molecules were established by spectral and analytical data. All the newly synthesized compounds were screened for their in vivo hypoglycaemic and hypolipidemic activity in male Wistar rats. Further, compounds with good activity were screened for PPARγ agonist activity. Among the screened compounds, 5‐{[2‐Cyclohexyl‐6‐(4‐methoxyphenyl)imidazo[2,1‐b] [1,3,4]thiadiazol‐5‐yl]methylene}‐1,3‐thiazolidine‐2,4‐dione (3i) exhibits promising hypoglycaemic and hypolipidemic activity via potential PPARγ agonist activity. 相似文献
18.
Kamel Metwally Ashraf Khalil Harris Pratsinis Dimitris Kletsas 《Archiv der Pharmazie》2010,343(8):465-472
As part of our ongoing research effort to develop new antimitotic agents based on the recently reported pyrimido[4,5‐c]quinoline‐1(2H)‐one ring skeleton, we were interested in identifying structural elements that contribute to the cytotoxicity of this class of compounds. The effect of several quinoline‐ring substituents was examined and the new compounds were evaluated in vitro for cytotoxicity against three human cancer cell lines namely, lung fibrosarcoma HT‐1080, colon adenocarcinoma HT‐29, and breast carcinoma MDA‐MB‐231. Most of the compounds showed cytotoxic activity in the low micromolar and sub‐micromolar range. Structure‐activity relationship information revealed that a combination of electronic and steric factors may be involved. Flow cytometric cell cycle analysis performed on HT‐1080 cells revealed that the most cytotoxic compounds 48 , 50 , 54 , 59 , and 63 inhibit the S‐phase and arrest the cells in the G2/M phase of the cell cycle suggesting an antimitotic action of these compounds. 相似文献
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In this study on the development of new anticonvulsants, fourteen ethyl 2,2‐dimethyl‐1‐(2‐substitutedhydrazinecarboxamido) cyclopropanecarboxylate derivatives were synthesized and tested for anticonvulsant activity using the maximal electroshock, subcutaneous pentylenetetrazole screens, which are the most widely employed seizure models for early identification of candidate anticonvulsants. Their neurotoxicity was determined applying the rotorod test. Two compounds 6f and 6k showed promising anticonvulsant activities in both models employed for anticonvulsant evaluation. The most active compound 6k showed the maximal electroshock‐induced seizures with ED50 value of 9.2 mg/kg and TD50 value of 387.5 mg/kg after intraperitoneally injection to mice, which provided compound 6k with a protective index (TD50/ED50) of 42.1 in the maximal electroshock test. 相似文献