- Directed biosynthesis of 5'-fluoropactamycin in Streptomyces pactum
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A new pactamycin analogue, 5'-fluoropactamycin, was prepared by directed biosynthesis. Supplementation of the fermentation medium of Streptomyces pactum, var. pactum with 3-amino-5-fluorobenzoic acid, an analogue of 3-aminobenzoic acid, an advanced precursor in pactamycin biosynthesis, resulted in co-production of pactamycin and the new pactamycin analogue. A similar feeding experiment with 3-amino-5-methylbenzoic acid did not result in formation of the corresponding methylated pactamycin analogue, but only in inhibition of pactamycin production. Comparison of antimicrobial and cytotoxic activities of pactamycin and 5'-fluoropactamycin showed no significant differences.
- Adams,Rinehart
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- FUSED BICYCLIC COMPOUNDS FOR THE TREATMENT OF PAIN
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Provided herein are compounds that are useful in the treatment of pain in a subject. Also provided herein is a pharmaceutical composition comprising compounds or pharmaceutically acceptable salts thereof, and a pharmaceutically acceptable carrier and methods of treating pain in a subject in need thereof.
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Page/Page column 58; 63-64
(2021/02/12)
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- Fluorine atom substituted benzo heterocycle based conjugated molecule material as well as preparation method and application thereof
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The invention discloses a fluorine atom substituted benzo heterocycle based conjugated molecule material as well as a preparation method and application thereof. The conjugated molecule material is ofan acceptor-donor-acceptor type structure, wherein an a
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Paragraph 0094; 0097; 0098; 0099
(2018/07/30)
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- SERINE/THREONINE PAK1 INHIBITORS
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Compounds having the formula I wherein A, Z, R1a, R1b, R2, R3, R4, R5, R6, R7, R9, R10, Ra, Rb and n are as defined herein are inhibitors of PAK1. Also disclosed are compositions and methods for treating cancer and hyperproliferative disorders.
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Page/Page column 118
(2013/03/26)
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- Potent mGluR5 antagonists: Pyridyl and thiazolyl-ethynyl-3,5-disubstituted- phenyl series
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We report the synthesis of four series of 3,5-disubstituted-phenyl ligands targeting the metabotropic glutamate receptor subtype 5: (2-methylthiazol-4-yl) ethynyl (1a-j,), (6-methylpyridin-2-yl)ethynyl (2a-j), (5-methylpyridin-2-yl) ethynyl (3a-j,), and (pyridin-2-yl)ethynyl (4a-j,). The compounds were evaluated for antagonism of glutamate-mediated mobilization of internal calcium in an mGluR5 in vitro assay. All compounds were found to be full antagonists and exhibited low nanomolar to subnanomolar activity.
- Alagille, David,Dacosta, Herve,Chen, Yelin,Hemstapat, Kamondanai,Rodriguez, Alice,Baldwin, Ronald M.,Conn, Jeffrey P.,Tamagnan, Gilles D.
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supporting information; experimental part
p. 3243 - 3247
(2011/07/07)
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- SUBSTITUTED 1H-BENZIMIDAZOLE-4-CARBOXAMIDES ARE POTENT PARP INHIBITORS
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Compounds of Formula (I) inhibit the PARP enzyme and are useful for treating a disease or a disorder associated with PARP. Also disclosed are pharmaceutical compositions comprising compounds of Formula (I), methods of treatment comprising compounds of For
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Page/Page column 14
(2008/06/13)
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- SUBSTITUTED 1H-BENZIMIDAZOLE-4-CARBOXAMIDES ARE POTENT PARP INHIBITORS
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The present invention relates to 1H-benzimidazole-4-carboxamides of formula (I), their preparation, and their use as inhibitors of the enzyme poly(ADP-ribose)polymerase for the preparation of drugs.
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Page/Page column 9
(2008/06/13)
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- Structure-guided design of AMP mimics that inhibit fructose-1,6- bisphosphatase with high affinity and specificity
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AMP binding sites are commonly used by nature for allosteric regulation of enzymes controlling the production and metabolism of carbohydrates and lipids. Since many of these enzymes represent potential drug targets for metabolic diseases, efforts were ini
- Erion, Mark D.,Dang, Qun,Reddy, M. Rami,Kasibhatla, Srinivas Rao,Huang, Jingwei,Lipscomb, William N.,Van Poelje, Paul D.
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p. 15480 - 15490
(2008/09/19)
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- 1H-BENZIMIDAZOLE-4-CARBOXAMIDES SUBSTITUTED WITH PHENYL AT THE 2-POSITION ARE POTENT PARP INHIBITORS
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Compounds having formula (I), inhibit the PARP enzyme and are useful for treating a disease or a disorder associated with PARP. Also disclosed are pharmaceutical compositions comprising compounds having formula (I), methods of treatment comprising compounds having formula (I), and methods of inhibiting the PARP enzyme comprising compounds having formula (I).
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Page/Page column 44
(2010/11/26)
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- 1H-benzimidazole-4-carboxamides substituted with a quaternary carbon at the 2-position are potent PARP inhibitors
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Compounds of Formula (I) inhibit the PARP enzyme and are useful for treating a disease or a disorder associated with PARP. Also disclosed are pharmaceutical compositions comprising compounds of Formula (I), methods of treatment comprising compounds of For
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Page/Page column 25
(2008/06/13)
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- Biologically selective potassium channel openers having 1,1- diethylpropyl group
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To find out selective potassium channel openers (PCOs), we synthesized several 3,5-disubstituted phenylcyanoguanidine derivatives and investigated their structure-activity relationships (SAR). As a result, we discovered selective PCOs having 1,1-diethylpropyl group toward antihypertensive activity.
- Yoshiizumi, Kazuya,Seko, Norihiko,Nishimura, Noriyasu,Ikeda, Shoji,Yoshino, Kohichiro,Kondo, Hirosato,Tanizawa, Kazutaka
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p. 3397 - 3402
(2007/10/03)
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- NMDA antagonists
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The present invention is directed to a new class of 4-sulfanimide-quinoline derivatives and to their use as NMDA antagonists.
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- 2-carbocyclic and 2-heterocyclic quinoline-4-carboxylic acids and salts thereof useful as immunosuppressive agents
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This invention relates to 2-carbocyclic and 2-heterocyclic quinoline-4-carbocyclic acid compounds, and salts thereof, to pharmaceutical compositions comprising such compounds, and to methods of using such compounds for the treatment and/or prevention of o
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- Glycine receptor antagonists and the use thereof
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Methods of treating or preventing neuronal loss associated with stroke, ischemia, CNS trauma, hypoglycemia and surgery, as well as treating neurodegenerative diseases including Alzheimer's disease, amyotrophic lateral sclerosis, Huntington's disease and Down's syndrome, treating or preventing the adverse consequences of the hyperactivity of the excitatory amino acids, as well as treating anxiety, chronic pain, convulsions, inducing anesthesia and treating psychosis are disclosed by administering to an animal in need of such treatment a compound having high affinity for the glycine binding site, lacking PCP side effects and which crosses the blood brain barrier of the animal. Also disclosed are novel 1,4-dihydroquinoxaline-2,3-diones, and pharmaceutical compositions thereof. Also disclosed are highly soluble ammonium salts of 1,4-dihydroquinoxaline-2,3-diones.
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- NMDA ANTAGONISTS
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The present invention is directed to a class of 4,6-disubstituted tryptophan derivatives, 4,6-disubstituted kynurenines, their use as NMDA antagonists and to pharmaceutical compositions containing these compounds.
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- Novel cyanoguanidine derivatives
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Compounds of the formula: STR1 wherein R1 and R2 are independently fluorine, chlorine or bromine atom, and R3 is a C4 -C7 alkyl having at least a branch at the C1 position, exhibit K+ channel opening activity and are useful as hypotensive agents and coronary vasodilators.
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