- Synergism of a novel 1,2,4-oxadiazole-containing derivative with oxacillin against methicillin-resistant staphylococcus aureus
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Staphylococcus aureus is an important opportunistic pathogen that causes many infections in humans and animals. The inappropriate use of antibiotics has favored the diffusion of methicillin-resistant S. aureus (MRSA), nullifying the efforts undertaken in
- Buommino, Elisabetta,D’auria, Maria Valeria,De Marino, Simona,Festa, Carmen,Piccolo, Marialuisa,Sciarretta, Martina
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- VASCULAR ADHESION PROTEIN-1 (VAP-1) MODULATORS AND THERAPEUTIC USES THEREOF
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Disclosed herein are small molecule Vascular Adhesion Protein- 1 (VAP-1) modulator compositions, pharmaceutical compositions, the use and preparation thereof.
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Paragraph 0236
(2020/01/24)
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- SSAO INHIBITOR
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The present invention provides an SSAO inhibitor and an application thereof in preparing a drug for treating a disease related to SSAO. In particular, the present invention provides a compound shown in formula (IV) and a pharmaceutically acceptable salt thereof.
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Paragraph 0234-0236; 0277-0279
(2020/04/02)
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- FUNGICIDAL OXADIAZOLES
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Disclosed are compounds of Formula 1, including all geometric and stereoisomers, tautomers, N-oxides, and salts thereof, wherein R1, L and J are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling plant disease caused by a fungal pathogen comprising applying an effective amount of a compound or a composition of the invention.
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Paragraph 0673
(2020/06/07)
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- Synthesis of novel mono and bis nitric oxide donors with high cytocompatibility and release activity
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Four compounds bearing amidoxime functions were synthetized: (1) 2a,b bearing an aromatic amidoxime function, (2) 2c bearing an aliphatic amidoxime function, and (3) 2d bearing aromatic and aliphatic amidoximes functions. The ability of these compounds to
- Sahyoun, Tanya,Gaucher, Caroline,Zhou, Yi,Ouaini, Na?m,Schneider, Rapha?l,Arrault, Axelle
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supporting information
p. 3329 - 3332
(2018/09/27)
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- Small Molecule Inhibition of MicroRNA miR-21 Rescues Chemosensitivity of Renal-Cell Carcinoma to Topotecan
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Chemical probes of microRNA (miRNA) function are potential tools for understanding miRNA biology that also provide new approaches for discovering therapeutics for miRNA-associated diseases. MicroRNA-21 (miR-21) is an oncogenic miRNA that is overexpressed in most cancers and has been strongly associated with driving chemoresistance in cancers such as renal cell carcinoma (RCC). Using a cell-based luciferase reporter assay to screen small molecules, we identified a novel inhibitor of miR-21 function. Following structure-activity relationship studies, an optimized lead compound demonstrated cytotoxicity in several cancer cell lines. In a chemoresistant-RCC cell line, inhibition of miR-21 via small molecule treatment rescued the expression of tumor-suppressor proteins and sensitized cells to topotecan-induced apoptosis. This resulted in a >10-fold improvement in topotecan activity in cell viability and clonogenic assays. Overall, this work reports a novel small molecule inhibitor for perturbing miR-21 function and demonstrates an approach to enhancing the potency of chemotherapeutics specifically for cancers derived from oncomir addiction.
- Naro, Yuta,Ankenbruck, Nicholas,Thomas, Meryl,Tivon, Yaniv,Connelly, Colleen M.,Gardner, Laura,Deiters, Alexander
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p. 5900 - 5909
(2018/08/04)
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- NOVEL OXADIAZOLE DERIVATIVE AND PHARMACEUTICAL CONTAINING SAME
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An amyloid fibril formation inhibitor comprising a compound represented by the following general formulae (I) to (III): wherein Q is -C(=O)-; X is -C(=O)-, -NH-C(=O)-; Y is -(CH2)m-; Z is -(CH2)n-; R1
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Paragraph 0136; 0137
(2018/02/28)
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- ANTI-ENTEROVIRUS 71 THIADIAZOLIDINE DERIVATIVE
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Disclosed is a novel anti-enterovirus 71 (EV71) 1,2,5-thiadiazolidine-1,1-dioxide derivative or a pharmaceutically acceptable salt thereof; and specifically, a compound represented by formula (II) or a pharmaceutically acceptable salt thereof.
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Paragraph 0153-0155
(2017/03/28)
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- 1, 2, 4-oxdiazole compound and its preparation method and application
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The invention discloses a 1,2,4-oxadiazole compound and a preparation method and application thereof. The structural general formula of the compound is shown in a formula I. The preparation method comprises the following steps of: when RB is -CF3, perform
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Paragraph 0066-0069
(2016/10/07)
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- Conjugation of N-acylhydrazone and 1,2,4-oxadiazole leads to the identification of active antimalarial agents
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Malaria, caused by several Plasmodium species, is the major life-threatening parasitic infection worldwide. Due to the parasite resistance to quinoline based drugs, the search for antimalarial agents is necessary. Here, we report the structural design, sy
- dos Santos Filho, José Maurício,de Queiroz e Silva, Diogo Manoel Alves,Macedo, Taís Soares,Teixeira, Helena Mariana Pitangueira,Moreira, Diogo Rodrigo Magalhaes,Challal, Soura,Wolfender, Jean-Luc,Queiroz, Emerson Ferreira,Soares, Milena Botelho Pereira
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p. 5693 - 5701
(2016/11/09)
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- An Efficient Synthesis of 2-Substituted Quinazolin-4(3 H)-ones Catalyzed by Iron(III) Chloride
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A simple and highly efficient synthesis of 2-substituted quinazolin-4(3H)-ones by the iron(III) chloride catalyzed reaction of isatoic anhydride with various amidoxime derivatives was developed. Several aryl and alkyl amidoximes were screened to demonstra
- Mekala, Ramamohan,Akula, Raghunadh,Kamaraju, Raghavendra Rao,Bannoth, Chandrasekhar Kothapalli,Regati, Sridhar,Sarva, Jayaprakash
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supporting information
p. 821 - 826
(2014/04/03)
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- NOVEL AMINOMETHYL-PHENOL DERIVATIVES AS ANTIMALARIAL AGENTS
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The invention relates to novel aminomethyl-phenol derivatives of formula I wherein R1 to R4, X, A and B are as defined for formula I and their use as active ingredients in the preparation of pharmaceutical compositions. The invention
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Page/Page column 54
(2014/05/24)
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- COMPOUNDS HAVING AN ETHR INHIBITING ACTIVITY - USE OF SAID COMPOUNDS AS DRUGS - PHARMACEUTICAL COMPOSITION AND PRODUCT CONTAINING SAID COMPOUNDS
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The present invention relates to compounds of Formula (I), wherein R1 is chosen among the following radicals : (II); (III); (IV), (V), (VI) (VII) and n= 1 or 2 and m=1 or 2 with the proviso that m=2 when R1 is (VIII). The present invention also relates to the use thereof as drugs, more particularly in the treatment of mycobacterial infections and more particularly in the treatment of tuberculosis.
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Page/Page column 10
(2013/05/21)
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- SULFONE DERIVATIVE
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Provided are a compound having an excellent hypoglycemic action, or a pharmaceutically acceptable salt thereof, and a pharmaceutical composition having an excellent therapeutic effect and/or prophylactic effect on type 1 diabetes, type 2 diabetes, and the
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Page/Page column 8-9
(2012/06/01)
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- Ethionamide boosters. 2. Combining bioisosteric replacement and structure-based drug design to solve pharmacokinetic issues in a series of potent 1,2,4-oxadiazole EthR inhibitors
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Mycobacterial transcriptional repressor EthR controls the expression of EthA, the bacterial monooxygenase activating ethionamide, and is thus largely responsible for the low sensitivity of the human pathogen Mycobacterium tuberculosis to this antibiotic.
- Flipo, Marion,Desroses, Matthieu,Lecat-Guillet, Nathalie,Villemagne, Baptiste,Blondiaux, Nicolas,Leroux, Florence,Piveteau, Catherine,Mathys, Vanessa,Flament, Marie-Pierre,Siepmann, Juergen,Villeret, Vincent,Wohlk?nig, Alexandre,Wintjens, René,Soror, Sameh H.,Christophe, Thierry,Jeon, Hee Kyoung,Locht, Camille,Brodin, Priscille,Déprez, Benoit,Baulard, Alain R.,Willand, Nicolas
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experimental part
p. 68 - 83
(2012/03/10)
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- AMIDE DERIVATIVE
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Provided are a compound having an excellent hypoglycemic action, or a pharmaceutically acceptable salt thereof, and a pharmaceutical composition having an excellent therapeutic effect and/or prophylactic effect on type 1 diabetes, type 2 diabetes, and the like, which cause an increase in the blood sugar level due to abnormal sugar metabolism. A compound represented by general formula (I), or a pharmaceutically acceptable salt thereof, is disclosed.
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Page/Page column 21
(2012/06/01)
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- Optimization of anti-Trypanosoma cruzi oxadiazoles leads to identification of compounds with efficacy in infected mice
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We recently showed that oxadiazoles have anti-Trypanosoma cruzi activity at micromolar concentrations. These compounds are easy to synthesize and show a number of clear and interpretable structure-activity relationships (SAR), features that make them attr
- Dos Santos Filho, Jose Mauricio,Moreira, Diogo Rodrigo M.,De Simone, Carlos Alberto,Ferreira, Rafaela Salgado,McKerrow, James H.,Meira, Cassio Santana,Guimaraes, Elisalva Teixeira,Soares, Milena Botelho Pereira
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p. 6423 - 6433,11
(2012/12/11)
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- Novel oxadiazole analogues derived from ethacrynic acid: Design, synthesis, and structure - Activity relationships in inhibiting the activity of glutathione S-transferase P1-1 and cancer cell proliferation
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Ethacrynic acid (EA) is a glutathione S-transferase P1-1 (GST P1-1) inhibitor with weak antiproliferative ability in tumor cells. By use of the principle of bioisosterism, a series of novel EA oxadiazole analogues were designed and synthesized. The struct
- Yang, Xinmei,Liu, Guyue,Li, Hongcai,Zhang, Yun,Song, Dandan,Li, Chunmin,Wang, Rui,Liu, Bo,Liang, Wen,Jing, Yongkui,Zhao, Guisen
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experimental part
p. 1015 - 1022
(2010/08/06)
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- Discovery of novel antileishmanial agents in an attempt to synthesize pentamidine - Aplysinopsin hybrid molecule
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In an attempt to synthesize pentamidine-aplysinopsin hybrid molecule 25, a lead molecule 8 (containing Z-configured aplysinopsin moiety) was identified for antileishmanial activity. Optimization of lead 8 provided 24 (containing E-configured aplysinopsin)
- Porwal, Sharad,Chauhan, Shikha S.,Chauhan, Prem M. S.,Shakya, Nishi,Verma, Aditya,Gupta, Suman
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supporting information; experimental part
p. 5793 - 5802
(2010/03/24)
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- NOVEL THIOPHENE DERIVATIVES AS SPHINGOSINE-1-PHOSPHATE-1 RECEPTOR AGONISTS
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The invention relates to novel thiophene derivatives, their preparation and their use as pharmaceutically active compounds. Said compounds particularly act as immunosuppressive agents.
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Page/Page column 12
(2009/01/24)
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- ARYLAMIDINE DERIVATIVE, SALT THEREOF AND ANTIFUNGAL CONTAINING THESE
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An arylamidine derivative represented by the general formula (wherein R 1 represents optionally protected or substituted amidino; and R 2 and R 3 are the same or different and each represents hydrogen or halogeno) or a salt of the derivative. The derivati
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Page/Page column 29
(2008/06/13)
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- NOVEL THIOPHENE DERIVATIVES AS SPHINGOSINE-l-PHOSPHATE-1 RECEPTOR AGONISTS
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The invention relates to novel thiophene derivatives of formula (l),their preparation and their use as pharmaceutically active compounds. Said compounds particulary act as immunosuppressive agents. wherein ring A represents oxadiazole and the other substituents are as defined in the description.
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Page/Page column 39
(2010/11/24)
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- Synthesis and evaluation of substrate-mimicking cytosolic phospholipase A2 inhibitors - Reducing the lipophilicity of the arachidonyl chain isostere
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The high lipophilicity of a series of cytosolic phospholipase A2 inhibitors has been reduced by the modification of a decyloxyphenyl chain designed to mimic the arachidonyl group of the natural substrate. These changes have resulted in an improvement in the whole cell potency of the inhibitors.
- Walters, Iain,Bennion, Colin,Connolly, Stephen,Croshaw, Pamela J.,Hardy, Kim,Hartopp, Paul,Jackson, Clive G.,King, Sarah J.,Lawrence, Louise,Mete, Antonio,Murray, David,Robinson, David H.,Stein, Linda,Wells, Edward,Withnall, W. John
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p. 3645 - 3649
(2007/10/03)
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- Substituted 3-aryl-5-aryl-[1,2,4]-oxadiazoles and analogs as activators of caspases and inducers of apoptosis and the use thereof
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The present invention is directed to substituted 3-aryl-5-aryl-[1,2,4]-oxadiazoles and analogs thereof, represented by the Formula I: wherein Ar1, Ar3, A, B and D are defined herein. The present invention also relates to the discovery that compounds having Formula I are activators of caspases and inducers of apoptosis. Therefore, the activators of caspases and inducers of apoptosis of this invention may be used to induce cell death in a variety of clinical conditions in which uncontrolled growth and spread of abnormal cells occurs.
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- New 1,2,4-oxadiazole derivatives: Synthesis and adrenergic receptors binding studies
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In order to obtain derivatives with simultaneous α- and β-adrenergic blocking activity, compounds having the phenoxypropanolaminic structure of β-adrenergic blockers have been synthesised, as well as 1,2,4-oxadiazole moiety, which could imitate the imidaz
- Brizzi,Brufani,Filocamo,Bruni,Fiaschi
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p. 953 - 966
(2007/10/02)
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