- Structure-activity relationship studies of antiplasmodial aminomethylthiazoles
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Structure-activity relationship (SAR) studies around a previously reported antimalarial aminomethylthiazole pyrazole carboxamide 1 are reported. Several analogues were synthesised and profiled for in vitro antiplasmodial activity against the drug-sensitiv
- Cheuka, Peter Mubanga,Cabrera, Diego Gonzalez,Paquet, Tanya,Chibale, Kelly
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Read Online
- Oxime ether compound and application thereof
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The invention discloses an oxime ether compound with a novel structure, the structure is shown as a general formula I, and the definition of each substituent group in the formula is shown in the specification. The compound shown in the general formula I h
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Paragraph 0180-0183
(2021/05/12)
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- N -substituted -2 - amino -4 - saccharin-substituted methylthiazole compound with bactericidal activity Preparation method and application
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N -substituted -2 - amino -4 - saccharin-substituted methylthiazole compounds with bactericidal activity, a preparation method and an application thereof relate to the technical field of organic synthesis and agricultural chemicals. Experiments prove that
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Paragraph 0069-0071
(2021/11/26)
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- Hit-to-Lead Optimization of a Novel Class of Potent, Broad-Spectrum Trypanosomacides
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The parasitic trypanosomes Trypanosoma brucei and T. cruzi are responsible for significant human suffering in the form of human African trypanosomiasis (HAT) and Chagas disease. Drugs currently available to treat these neglected diseases leave much to be
- Russell, Stephanie,Rahmani, Rapha?l,Jones, Amy J.,Newson, Harriet L.,Neilde, Kevin,Cotillo, Ignacio,Rahmani Khajouei, Marzieh,Ferrins, Lori,Qureishi, Sana,Nguyen, Nghi,Martinez-Martinez, Maria S.,Weaver, Donald F.,Kaiser, Marcel,Riley, Jennifer,Thomas, John,De Rycker, Manu,Read, Kevin D.,Flematti, Gavin R.,Ryan, Eileen,Tanghe, Scott,Rodriguez, Ana,Charman, Susan A.,Kessler, Albane,Avery, Vicky M.,Baell, Jonathan B.,Piggott, Matthew J.
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p. 9686 - 9720
(2016/11/19)
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- NOVEL COMPOUND, ORGANIC CATION TRANSPORTER 3 DETECTION AGENT, AND ORGANIC CATION TRANSPORTER 3 ACTIVITY INHIBITOR
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[Problem] The present invention addresses the problem of providing a novel compound. The present invention also addresses the problem of providing an OCT3 detection agent or an OCT3 activity inhibitor, which comprises the novel compound. [Solution] A compound represented by formula (A), a pharmaceutically acceptable salt thereof, or a pharmaceutically acceptable solvate thereof. ????????R1-R2-R3-R4?????(A)
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Paragraph 0753-0755
(2016/08/17)
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- ANTIBACTERIAL SULFONE AND SULFOXIDE SUBSTITUTED HETEROCYCLIC UREA COMPOUNDS
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The present invention provides novel sulfone and sulfoxide substituted heterocyclic urea compounds having useful antibacterial activity. Use of these compounds as pharmaceutical compositions and methods of production are provided.
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Page/Page column 44
(2009/03/07)
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- ANTIBACTERIAL HETEROCYCLIC UREAS
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The present invention provides novel heterocyclic urea compounds having useful antibacterial activity, pharmaceutical compositions comprising one or more of these compounds, methods of making the same, and methods of using the same.
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Page/Page column 36
(2010/11/29)
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- RHO KINASE INHIBITORS
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Substituted amide and urea derivatives useful as inhibitors of Rho kinase are described, which inhibitors can be useful in the treatment of various disorders such as cardiovascular diseases, cancer, neurological diseases, renal diseases, bronchial asthma, erectile dysfunction and glaucoma.
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Page/Page column 153-154
(2008/12/07)
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- AMINE COMPOUNDS
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The present invention provide a compound of the formula:wherein ring A represents an aromatic ring optionally having substituents; B, Y and Ya are the same or different and each represents a bond, etc.; R1 and R2 are the same or different and each represents a hydrogen atom, etc.; R3 represents a hydrogen atom, etc.; R4 and R5 are the same or different and each represents a hydrogen, etc.; R6 represents an indolyl group optionally having substituents; and Z and Za are the same or different and each represents a hydrogen atom, etc.; or a salt thereof or a prodrug thereof, having a somatostatin receptor binding inhibition activity and is useful for preventing and/or treating diseases associated with somatostatin.
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- ANTICANCER COMPOUNDS
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This invention features compounds having formula (I): wherein, R1, R 2,R3, R4, R6, R7, T, X, and Y are as defined herein. This invention also features a method for treating cancer. The method includes administrating to a subject in need thereof a compound of formula (I).
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- In the search for new antiinflammatory drugs: Synthesis and antiinflammatory activity of some thiazolo(3,2-a)pyrimidine derivatives containing a thioether group
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Our strategy for the exploration of new NSAIDs starts on the synthesis of derivatives of 5-oxo-5H-Thiazolo[3,2-a]pyrimidines. The compounds were achieved by the following methods: (a) condensation of 2-amino-4-alkylthiomethylthiazole with ethyl 4-chloro-3-oxobutanoate (PPA method), (b) triphenyl phosphonium salts preparation, (c) Wittig-reaction of the salts with suitable aldehyde. Synthesized compounds were screened for antiinflammatory activity in the carrageenin rat paw oedema assay according to Winter et al. Some of the new synthesize compounds, at the dose used (50 mg/Kg) reduced meaningfully the oedema. The pharmacological effect varies according to the administration time.
- Passarotti,Valenti,Marini
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p. 639 - 643
(2007/10/03)
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