- Design, synthesis and biological evaluation of 4,5-dibromo-N-(thiazol-2-yl)-1H-pyrrole-2-carboxamide derivatives as novel DNA gyrase inhibitors
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Development of novel DNA gyrase B inhibitors is an important field of antibacterial drug discovery whose aim is to introduce a more effective representative of this mechanistic class into the clinic. In the present study, two new series of Escherichia coli DNA gyrase inhibitors bearing the 4,5-dibromopyrrolamide moiety have been designed and synthesized. 4,5,6,7-Tetrahydrobenzo[1,2-d]thiazole-2,6-diamine derivatives inhibited E. coli DNA gyrase in the submicromolar to low micromolar range (IC50values between 0.891 and 10.4 μM). Their “ring-opened” analogues, based on the 2-(2-aminothiazol-4-yl)acetic acid scaffold, displayed weaker DNA gyrase inhibition with IC50values between 15.9 and 169 μM. Molecular docking experiments were conducted to study the binding modes of inhibitors.
- Toma?i?, Tihomir,Mirt, Matic,Baran?oková, Michaela,Ila?, Janez,Zidar, Nace,Tammela, P?ivi,Kikelj, Danijel
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Read Online
- NLRP MODULATORS
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In one aspect, compounds of Formula AA, or a pharmaceutically acceptable salt thereof, are featured: or a pharmaceutically acceptable salt thereof, wherein the variables shown in Formula A can be as defined anywhere herein.
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Page/Page column 371; 372
(2020/01/31)
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- NLRP MODULATORS
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In one aspect, compounds of Formula AA, or a pharmaceutically acceptable salt thereof, are featured: or a pharmaceutically acceptable salt thereof, wherein the variables shown in Formula A can be as defined anywhere herein, useful to treat connected to the modulation of NRLP3.
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Page/Page column 346; 362
(2020/01/31)
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- COMPOUNDS AND THEIR METHODS OF USE
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Compounds and compositions comprising compounds that inhibit glutaminase are described herein. Also described herein are methods of using the compounds that inhibit glutaminase in the treatment of cancer.
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Paragraph 0897; 0901; 0902; 0903
(2014/05/25)
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- COMPOUNDS, PHARMACEUTICAL COMPOSITIONS AND USES AS GLUTAMINASE INHIBITORS FOR TREATING CANCERS THEREOF
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Provided are compounds of formula (I), wherein X, Y, Z, W, m, n, o, p, R1, R2 and R6 are defined as in the description. Pharmaceutical compositions and uses as glutaminase inhibitors for treating cancers thereof are also provided.
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Page/Page column 186; 187
(2014/06/11)
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- COMPOUNDS AND THEIR METHODS OF USE
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Provided are compounds of formula (I), which can inhibit glutaminase. Pharmaceutical compositions comprising these compounds and uses as glutaminase inhibitors for treating cancers thereof are also provided.
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Page/Page column 206; 207
(2014/06/11)
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- Synthesis, characterization and antimicrobial studies of a few novel thiazole derivatives
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A series of novel N-[4-(substituted)-1,3-thiazol-2-yl]-2-(substituted) acetamide (9a-m) and methyl 2-(2-(2-(substituted)acetamido)thiazol-4-yl)acetate (9n-o) derivatives have been synthesized and compounds were characterised by spectral and analytical studies. All compounds were screened for their in vitro antibacterial activity against Staphylococcus aureus, Escherichia coli, Pseudomonas aeruginosa and Klebsiella pneumonia by disc diffusion method and for antifungal activity against Penicillium marneffei, Trichophyton mentagrophytes, Aspergillus flavus and Aspergillus fumigatus by serial plate dilution method. Compounds 9b, 9e, 9m and 9o exhibited growth inhibition against all the tested bacterial strains, with MIC values varying from 12.5 to 6.25 μg/ml. Among the compounds tested for antifungal activity, 9a, 9b, 9d, 9j, 9k, 9p and 9n showed wide range of activity against all the tested strains. Most of the newly synthesized compounds were effective against fungal strains rather than bacterial strains. However, some of the compounds like 9a, 9e, 9j, 9k and 9i showed selective sensitivity against some of the bacterial strains whereas they were unable to sustain the growth of other strains.
- Praveen, Aletti S.,Yathirajan, Hemmige S.,Narayana, Badiadka,Sarojini, Balladka K.
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p. 259 - 268
(2014/03/21)
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- Thiazole- and imidazole-containing peptidomimetic inhibitors of protein farnesyltransferase
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Mimetics of the C-terminal CAAX tetrapeptide of Ras protein were designed replacing internal dipeptide AA with 4-amino-2-phenylbenzoic acid and cysteine (C) with 2-amino-4-thiazolyl-, 2-mercapto-4-thiazolyl-, 2-mercapto-4-imidazolyl- and 2-methylmercapto-4-thiazolyl-acetic or propionic acid. The compound in which C is replaced by 2-amino-4-thiazolylacetic acid inhibited FTase activity in the low nanomolar range and showed antiproliferative effect on rat aortic smooth muscle cells interfering with Ras farnesylation. On the basis of these results, 2-aminothiazole can be considered as an alternative to heterocycles, such as pyridine and imidazole, normally used in FTase inhibitors designed as non-thiol CAAX mimetics.
- Bolchi, Cristiano,Pallavicini, Marco,Bernini, Sergio K.,Chiodini, Giuseppe,Corsini, Alberto,Ferri, Nicola,Fumagalli, Laura,Straniero, Valentina,Valoti, Ermanno
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experimental part
p. 5408 - 5412
(2011/10/12)
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- Novel Heterocyclic Compounds
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The present invention relates to novel compounds of the general formula (I), their derivatives, their analogs, their stereoisomers, their pharmaceutically acceptable salts and compositions. The present invention more particularly provides novel heterocyclic compounds of the general formula (I).
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Page/Page column 6
(2010/06/22)
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- NOVEL HETEROCYCLIC COMPOUNDS
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The present invention relates to novel compounds of the general formula (I), their derivatives, their analogs, their stereoisomers, their pharmaceutically acceptable salts and compositions. The present invention more particularly provides novel heterocyclic compounds of the general formula (I).(I).
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Page/Page column 15
(2010/11/25)
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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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- Design and synthesis of heterocyclic hydroxamic acid derivatives as inhibitors of Helicobacter pylori urease
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Helicobacter pylori produces ammonia to help counter the acidic environment in the human stomach. The production of ammonia, essential for the microorganism's survival and virulence, is the product of enzymatic conversion of urea by the H. pylori's urease. Inhibition of urease activity by dipeptide hydroxamic acids has previously been demonstrated using a variety of fluorides, thiols and hydroxamic acids. Studies employing computer-aided drug design techniques have been utilized to suggest a novel series of heterocyclic hydroxamic acid derivatives as potential as urease inhibitors. The heterocyclic compounds 7a,b, 10b, 12b, 16b, and 19b have been designed, synthesized, and preliminarily tested as dipeptide mimics which offer a structure that is more biologically stable than that of the reported dipeptide inhibitors.
- Muri, Estela Maris F.,Mishra, Hetal,Avery, Mitchell A.,Williamson, John S.
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p. 1977 - 1995
(2007/10/03)
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- Reactions of 4-Chloroacetoacetic Esters with Thioureas
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Several heterocyclic acetic acids and esters were synthesized by allowing the appropriate thiourea, ethylenethiourea or trimethylenethiourea to react with 4-chloroacetoacetic esters, followed by acid hydrolysis to the hydrochlorides of the free acids.Both esters and acids of 2-aminothiazole-4-acetic acid, 5,6-dihydroimidazothiazole-3-acetic acid and 6,7-dihydro-5H-thiazolopyrimidine-3-acetic acid were obtained.
- Campaigne, E.,Selby, T. P.
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p. 1255 - 1257
(2007/10/02)
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