- Structure-Based Optimization of ML300-Derived, Noncovalent Inhibitors Targeting the Severe Acute Respiratory Syndrome Coronavirus 3CL Protease (SARS-CoV-2 3CLpro)
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Starting from the MLPCN probe compound ML300, a structure-based optimization campaign was initiated against the recent severe acute respiratory syndrome coronavirus (SARS-CoV-2) main protease (3CLpro). X-ray structures of SARS-CoV-1 and SARS-CoV-2 3CLpro enzymes in complex with multiple ML300-based inhibitors, including the original probe ML300, were obtained and proved instrumental in guiding chemistry toward probe compound 41 (CCF0058981). The disclosed inhibitors utilize a noncovalent mode of action and complex in a noncanonical binding mode not observed by peptidic 3CLpro inhibitors. In vitro DMPK profiling highlights key areas where further optimization in the series is required to obtain useful in vivo probes. Antiviral activity was established using a SARS-CoV-2-infected Vero E6 cell viability assay and a plaque formation assay. Compound 41 demonstrates nanomolar activity in these respective assays, comparable in potency to remdesivir. These findings have implications for antiviral development to combat current and future SARS-like zoonotic coronavirus outbreaks.
- Han, Sang Hoon,Goins, Christopher M.,Arya, Tarun,Shin, Woo-Jin,Maw, Joshua,Hooper, Alice,Sonawane, Dhiraj P.,Porter, Matthew R.,Bannister, Breyanne E.,Crouch, Rachel D.,Lindsey, A. Abigail,Lakatos, Gabriella,Martinez, Steven R.,Alvarado, Joseph,Akers, Wendell S.,Wang, Nancy S.,Jung, Jae U.,MacDonald, Jonathan D.,Stauffer, Shaun R.
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- Asymmetric pyrene derivatives comprising amine group including pyridinyl group and organic light-emitting diode including the same
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The present invention relates to pyrene derivatives represented by the following chemical formula A or the following chemical formula B, and an organic light-emitting diode including the same, wherein substituents Py, Ar1 to Ar3, Z and m are the same as d
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Paragraph 0326; 0335-0338; 0498-0502
(2021/04/20)
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- NOVEL HYDRAZONE DERIVATIVE WITH ARYL OR HETEROARYL GROUP SUBSTITUTED AT TERMINAL AMINE GROUP THEREOF AND USE THEREOF
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The present invention relates to novel hydrazone derivatives in which a terminal amine group is substituted with an aryl group or a heteroaryl group, and uses thereof.
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Paragraph 0069; 0097
(2021/11/04)
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- HETEROCYCLIC COMPOUNDS FOR MODULATING NR2F6
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The present disclosure relates to compounds capable of modulating the activity of NR2F6. The compounds of the disclosure may be used in methods for the prevention and/or the treatment of diseases and disorders associated with modulating NR2F6 activity.
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Paragraph 00499-00500
(2021/09/04)
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- Novel hydrazone derivatives comprising aryl or heteroaryl group substituted at terminal amine and use thereof
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The present invention relates to novel hydrazone derivatives with an aryl or heteroaryl group substituted at a terminal amine group thereof and a use thereof.
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Paragraph 0325; 0327; 0328; 0464; 0466; 0467
(2020/08/28)
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- S-triazine compounds as well as preparation method and application thereof
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The invention discloses s-triazine compounds and pharmaceutically acceptable salts thereof; experiments prove that the compounds can be used for treating or preventing diseases related to protein kinase activity, such as leukemia and lymphoma, by inhibiti
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Paragraph 0104; 0107
(2020/05/05)
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- Synthesis method of S-3-(4-aminophenyl) piperidine
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The invention relates to a synthesis method of S-3-(4-aminophenyl) piperidine. The synthetic method of the S-3-(4-aminophenyl) piperidine includes the following steps: taking 3-pyridineboronic acid (I) as a raw material, and preforming Suzuki coupling wit
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- Triazole naphthoquinone connected aromatic (heterocyclic) ring derivative
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The invention belongs to the field of chemical medicine, particularly relates to a micromolecule capable of resisting malignant tumor, acute leukemia and arthritis, multiple sclerosis and immunological rejection and a preparation and application of the mi
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Paragraph 0073; 0074; 0075
(2018/10/01)
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- One-Pot Palladium-Catalyzed Cross-Coupling Treble of Borylation, the Suzuki Reaction and Amination
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A methodology for a sequential palladium-catalyzed cross-coupling procedure consisting of borylation, the Suzuki reaction and amination has been developed for the assembly of molecules with multi-aryl backbones. The linchpin of this development is the meta-terarylphosphine ligand, Cy*Phine, which has been employed as an air- and moisture-stable precatalyst, Pd(Cy*Phine)2Cl2, to improve the efficiency of one-pot borylation–Suzuki reactions. Additionally, the reactivity of the Pd-Cy*Phine system could be tuned to furnish a one-pot, borylation–Suzuki reaction–amination (BSA) cross-coupling treble. The methodology successfully integrated complementary conditions for three distinctly different and modular reactions. Average yields of 74–94% could be achieved for each segment that cumulatively afforded 50–84% yield over the entire three-step sequence in a single pot. (Figure presented.).
- Jong, Howard,Eey, Stanley T.-C.,Lim, Yee Hwee,Pandey, Sangeeta,Iqbal, Nurul Azmah Bte,Yong, Fui Fong,Robins, Edward G.,Johannes, Charles W.
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supporting information
p. 616 - 622
(2017/02/23)
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- Design, synthesis, anticancer activity and docking studies of theophylline containing 1,2,3-triazoles with variant amide derivatives
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A new series of theophylline analogues containing 1,2,3-triazoles with different amide groups (22-41) has been designed and synthesized, and their biological activities have been evaluated as potential anticancer agents. The anticancer activities of the synthesized compounds were studied in four cancer cell lines viz. lung (A549), colon (HT-29), breast (MCF-7) and melanoma (A375). Furthermore, these compounds were screened for computational ADME and Lipinski's analysis followed by molecular docking and binding energy calculations against the various therapeutic targets involved in cell proliferation. The in vitro results demonstrate that compounds 22, 27, 36 and 40 have pivotal anticancer activity. Among these, compounds 22 and 27 have significant cytotoxic activity in all three cell lines; the in silico docking studies also reveal that compounds 22, 27 and 36 have good dock scores, binding affinities and binding energies towards human epidermal growth factor receptor 2. This is the first report to demonstrate theophylline hybrids containing 1,2,3-triazoles as potential anticancer agents.
- Ruddarraju, Radhakrishnam Raju,Murugulla, Adharvana Chari,Kotla, Ravindar,Tirumalasetty, Muni Chandra Babu,Wudayagiri, Rajendra,Donthabakthuni, Shobha,Maroju, Ravichandar
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supporting information
p. 176 - 183
(2017/02/05)
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- Design, synthesis, and evaluation of potent Wnt signaling inhibitors featuring a fused 3-ring system
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The Wnt signaling pathway is a critical developmental pathway which operates through control of cellular functions such as proliferation and differentiation. Aberrant Wnt signaling has been linked to the formation and metastasis of tumors. Porcupine, a member of the membrane-bound O-acyltransferase family of proteins, is an important component of the Wnt pathway. Porcupine catalyzes the palmitoylation of Wnt proteins, a process needed for their secretion and activity. Here we report a novel series of compounds obtained by a scaffold hybridization strategy from a known porcupine inhibitor class. The leading compound 59 demonstrated subnanomolar inhibition of Wnt signaling in a paracrine cellular assay. Compound 59 also showed excellent chemical, plasma and liver microsomal stabilities. Furthermore, compound 59 exhibited good pharmacokinetic profiles with 30% oral bioavailability in rat. Collectively, these results strongly support further optimization of this novel scaffold to develop better Wnt pathway inhibitors.
- Xu, Zhixiang,Li, Jiajun,Wu, Yiyuan,Sun, Zhijian,Luo, Lusong,Hu, Zhilin,He, Sudan,Zheng, Jiyue,Zhang, Hongjian,Zhang, Xiaohu
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p. 154 - 165
(2015/12/04)
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- Diarylthiourea compound with antitumor activity, and preparation method and application thereof
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The invention provides a diarylthiourea compound with antitumor activity, and a preparation method and application thereof. The compound has a structural formula as described in the specification. In the structural formula, R1 and R2 are selected from the group consisting of a halogen group or a group formed by R1 and R2 together; and Ar is a nitrogen heterocyclic ring of pyridine, indazole or quinazoline. The compound provided by the invention has good inhibitory activity to VEGFR-2 kinase, so a signal channel induced by the VEGFR-2 kinase can be blocked through inhibition of the activity of the VEGFR-2 kinase, and proliferation and migration of tumor cells are inhibited; thus, the compound can be applied in preparation of antitumor drugs. Meanwhile, the preparation method for the compound has the following advantages: raw materials are easily available; reaction conditions are mild; the process of reaction is simple to operate; and used reagents are cheap.
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Paragraph 0036-0039; 0050-0053
(2017/02/02)
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- Discovery of biphenyl-aryl ureas as novel VEGFR-2 inhibitors. Part 4: Exploration of diverse hinge-binding fragments
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Abstract VEGFR-2 plays an essential role in angiogenesis and is an important target for cancer therapy. A series of biphenyl-aryl ureas were synthesized and evaluated as novel VEGFR-2 inhibitors. The pyridine, methylamine carbonyl pyridine and pivaloyl amide pyridine were introduced as novel hinge binding fragment. The majority of title compounds displayed potent VEGFR-2 inhibition. In particular, L1, L9, W14 and W15 exhibited significant enzymatic inhibitory activity with IC50 values of 0.36 nM, 0.22 nM, 0.15 nM and 0.14 nM. Compounds L1, L9 and W15 displayed potent antiproliferative activity against A549 and SMMC-7721 cells. SAR study suggested that incorporation of 3-trifluoromethyl and methylamine carbonyl on terminal pyridine could improve VEGFR-2 inhibitory activity. Molecular docking illustrated that urea moiety formed two critical hydrogen bonds with the DFG residues of VEGFR-2. The results indicated that these biphenyl-aryl ureas could serve as promising lead compounds for further optimization.
- Su, Ping,Wang, Jinfeng,Shi, Yaling,Pan, Xiaoyan,Shao, Ruili,Zhang, Jie
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p. 3228 - 3236
(2015/08/03)
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- Nickel-catalyzed monoarylation of ammonia
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Structurally diverse (hetero)aryl chloride, bromide, and tosylate electrophiles were employed in the Ni-catalyzed monoarylation of ammonia, including chemoselective transformations. The employed JosiPhos/[Ni(cod)2] catalyst system enables the use of commercially available stock solutions of ammonia, or the use of ammonia gas in these reactions, thereby demonstrating the versatility and potential scalability of the reported protocol. Proof-of-principle experiments established that air-stable [(JosiPhos)NiCl2] precatalysts can be employed successfully in such transformations. Lighten Up: The substrate scope of the title reaction includes (hetero)aryl chloride, bromide, and tosylate electrophiles. The versatility and potential scalability of the reported method is demonstrated by the use of either commercially available stock solutions of ammonia or ammonia gas.
- Borzenko, Andrey,Rotta-Loria, Nicolas L.,Macqueen, Preston M.,Lavoie, Christopher M.,McDonald, Robert,Stradiotto, Mark
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supporting information
p. 3773 - 3777
(2015/03/18)
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- Facile synthesis of 3-arylpyridine derivatives by palladacycle-catalyzed Stille cross-coupling reaction
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The Stille cross-coupling reaction of a variety of aryl halides (X=Cl, Br, I) with 3-alkylstannylpyridines highly catalyzed by cyclopalladated ferrocenylimine has been developed. This reaction allows formation of arylpyridine derivatives in moderate to excellent yields. Functional groups on aryl halides, such as amino, hydroxyl, keto, and aldehyde are tolerated and the reactions with arylbenzoxale substrates also proceed well.
- Ma, Gaizhi,Leng, Yuting,Wu, Yusheng,Wu, Yangjie
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p. 902 - 909
(2013/07/25)
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- PYRAZINE KINASE INHIBITORS
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Provided are pyrazine compounds for inhibiting of Syk kinase, intermediates used in making such compounds, methods for their preparation, pharmaceutical compositions thereof, methods for inhibition Syk kinase activity, and methods for treating conditions mediated at least in part by Syk kinase activity.
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- NAPHTHALENE DERIVATIVE
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The present invention provides compounds which can regulate VCP activity. The present invention provides the compound of formula (I) (R is as defined in the description) or oxides, esters, prodrugs, pharmaceutically acceptable salts or solvates thereof. The compounds can regulate VCP activity, and thus are useful for treating VCP-mediated diseases such as neurodegenerative diseases.
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- NOVEL CATALYSTS
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The present invention provides novel compounds and ligands that are useful in transition metal catalyzed cross-coupling reactions. For example, the compounds and ligands of the present invention are useful in palladium or gold catalyzed cross-coupling reactions.
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Page/Page column 61-62
(2012/06/01)
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- 2-Pyridyl and 3-pyridylzinc bromides: direct preparation and coupling reaction
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A facile synthetic approach to the direct preparation of 2-pyridyl and 3-pyridylzinc bromides has been demonstrated using Rieke zinc with 2-bromopyridine and 3-bromopyridine, respectively. A variety of different electrophiles have been coupled with the resulting organozinc reagents to give the corresponding cross-coupling products in moderate to good yields.
- Kim, Seung-Hoi,Rieke, Reuben D.
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supporting information; experimental part
p. 3135 - 3146
(2010/06/13)
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- A P,N-Ligand for palladium-catalyzed ammonia arylation: Coupling of deactivated aryl chlorides, chemoselective arylations, and room temperature reactions
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(Figure Presented) Amazing ammonia: A new air-stable P,N-ligand (Mor-DalPhos) is reported that enables the palladium-catalyzed crosscoupling of ammonia to a variety of aryl chloride and aryl tosylate substrates with high chemoselectivity and, for the first time, at room temperature (see scheme; Ad = adamantyl, Ts=para-toluenesulfonyl).
- Lundgren, Rylan J.,Peters, Brendan D.,Alsabeh, Pamela G.,Stradiotto, Mark
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supporting information; experimental part
p. 4071 - 4074
(2010/07/05)
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- Theramutein modulators
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This invention relates to agents that are inhibitors or activators of variant forms of endogenous proteins and novel methods of identifying such variants. Of particular interest are inhibitors and activators of endogenous protein variants, encoded by genes which have mutated, which variants often arise or are at least first identified as having arisen following exposure to a chemical agent which is known to be an inhibitor or activator of the corresponding unmutated endogenous protein.
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Page/Page column 175
(2010/02/17)
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- Efficient diphosphane-based catalyst for the palladium-catalyzed suzuki cross-coupling reaction of 3-pyridylboronic acids
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A highly active catalyst system derived from PdCl2 and 2,2',6,6'- tetramethoxy-4,4'-bis(diphenylphosphanyl)-3,3'-bi- pyridine (P-Phos) has been developed for the Suzuki cross- coupling reaction of pyridylboronic acid with a variety of aryl halides in good to excellent yields, even in the presence of hindered and functional groups. In addition, P-Phos also exhibited high activity in the palladium-catalyzed Suzuki reaction of 2,6-dimethoxypyridylboronic acid in excellent yields with a fast rate. The steric and electronic effects of the P- Phos-palladium complex to this cross-coupling reaction were also discussed.
- Fu, Xing-Li,Wu, Lei-Lei,Fu, Hai-Yan,Chen, Hua,Li, Rui-Xiang
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experimental part
p. 2051 - 2054
(2009/09/06)
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- Air-stable and highly active dendritic phosphine oxide-stabilized palladium nanoparticles: Preparation, characterization and applications in the carbon-carbon bond formation and hydrogenation reactions
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Dendrimer-stabilized palladium nanoparticles were formed in the reduction of palldium bis-(acetylacetonate) [Pd(acac)2] in the presence of phosphine dendrimer ligands using hydrogen in tetrahydrofuran. The resulting Pd nanoparticles were characterized by TEM, 31P NMR and 31P MAS NMR. The results indicated that the dendritic phosphine ligandswere oxidized to phosphine oxides. These dendrimer-stabilized Pd nanoparticles were demonstrated to be efficient catalysts for Suzuki and Stille coupling reactionsand hydrogenations. The dendritic wedges served as a stabilizer for keeping the nanoparticlesfrom aggregating, and asa vehicle for facilitating the separation and/or the recycling of the Pd catalyst. In the case of the Suzuki coupling reaction, these Pd nanoparticles exhibited high catalytic efficiency (TON up to 65,000) and air stability as compared with the commonly used homogeneous catalyst tetrakis(triphenylphosphine)palladium [Pd-(PPh 3)4]. In addition, the results obtained from the bulky dendritic substrate suggest that the Pd nanoparticles might act asres ervoir of catalytically active species, and that the reaction is actually catalyzed by the soluble Pd(0) and/or Pd(II) species leached from the nanoparticle surface.
- Wu, Lei,Li, Zhi-Wei,Zhang, Feng,He, Yan-Mei,Fan, Qing-Hua
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experimental part
p. 846 - 862
(2009/05/07)
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- THERAMUTEIN MODULATORS
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This invention relates to agents that are inhibitors or activators of variant forms of endogenous proteins and novel methods of identifying such variants. Of particular interest are inhibitors and activators of endogenous protein variants, encoded by genes which have mutated, which variants often arise or are at least first identified as having arisen following exposure to a chemical agent which is known to be an inhibitor or activator of the corresponding unmutated endogenous protein.
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Page/Page column 208
(2008/12/07)
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- HYDRAZONE DERIVATIVE
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A compound represented by the following formula (I): wherein R1 represents hydrogen, aryl which may have a substituent, a saturated or unsaturated 5- to 7-membered heterocyclic group which may have a substituent, etc.; R2 represents hydrogen, aryl which may have a substituent, a saturated or unsaturated 5- to 7-membered heterocyclic group which may have a substituent, etc.; R3 represents hydrogen, etc.; Ar represents a divalent group derived from aromatic hydrocarbon, etc.; X represents a single bond, linear or branched alkylene having from 1 to 3 carbon atoms which may have a substituent, etc.; and G represents halogen, a saturated or unsaturated 5- or 6-membered cyclic hydrocarbon group which may have a substituent, a saturated or unsaturated 5- to 7-membered heterocyclic group which may have a substituent, etc., a salt thereof or a solvate thereof; and an agent for inhibiting aggregation and/or deposition of an amyloid protein or an amyloid-like protein, which comprises the compound, a salt thereof or a solvate thereof
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Page/Page column 23
(2010/11/08)
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- Palladium-phosphinous acid-catalyzed NaOH-promoted cross-coupling reactions of arylsiloxanes with aryl chlorides and bromides in water
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(Equation presented) A palladium-phosphinous acid-catalyzed and NaOH-promoted coupling method using arylsiloxanes and aryl halides in water has been developed. The POPd1-catalyzed reaction between aryl chlorides or bromides and arylsiloxanes is compatible with various functional groups and affords biaryls in up to 99% yield. This cross-coupling reaction does not require additives such as surfactants or organic cosolvents and proceeds under air, which greatly facilitates operation and catalyst handling.
- Wolf, Christian,Lerebours, Rachel
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p. 1147 - 1150
(2007/10/03)
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- Biarylcarbamoylindolines are novel and selective 5-HT(2C) receptor inverse agonists: Identification of 5-methyl-1-[[2-[(2-methyl-3- pyridyl)oxy]5-pyridyl]carbamoyl]-6-trifluoromethylindoline (SB-243213) as a potential antidepressant/anxiolytic agent
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The evolution, synthesis, and biological activity of a novel series of 5-HT(2C) receptor inverse agonists are reported. Biarylcarbamoylindolines have been identified with excellent 5-HT(2C) affinity and selectivity over 5- HT(2A) receptors. In addition, (pyridyloxypyridyl)carbamoylindolines have been discovered with additional selectivity over the closely related 5-HT(2B) receptor. Compounds from this series are inverse agonists at the human cloned 5-HT(2C) receptor, completely abolishing basal activity in a functional assay. The new series have reduced P450 inhibitory liability compared to a previously described series of 1-(3-pyridylcarbamoyl)indolines (Bromidge et al. J. Med. Chem. 1998, 41, 1598) from which they evolved. Compounds from this series showed excellent oral activity in a rat mCPP hypolocomotion model and in animal models of anxiety. On the basis of their favorable biological profile, 32 (SB-228357) and 40 (SB-243213) have been selected for further evaluation to determine their therapeutic potential for the treatment of CNS disorders such as depression and anxiety.
- Bromidge, Steven M.,Dabbs, Steven,Davies, David T.,Davies, Susannah,Duckworth, D. Malcolm,Forbes, Ian T.,Gaster, Laramie M.,Ham, Peter,Jones, Graham E.,King, Frank D.,Mulholland, Keith R.,Saunders, Damian V.,Wyman, Paul A.,Blaney, Frank E.,Clarke, Stephen E.,Blackburn, Thomas P.,Holland, Vicky,Kennett, Guy A.,Lightowler, Sean,Middlemiss, Derek N.,Trail, Brenda,Riley, Graham J.,Wood, Martyn D.
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p. 1123 - 1134
(2007/10/03)
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- Pyridyl-substituted thioaminyl stable free radicals: Isolation, ESR spectra, and magnetic characterization
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N-[(4-Nitrophenyl)thio]- (1a) and N-[(2,4-dichlorophenyl)thio)]-2,6- diphenyl-4-(3-pyridyl)phenylaminyl (1b), N-[(4-nitrophenyl)thio]- (2a) and N- [(2,4-dichlorophenyl)thio]-4-phenyl-2,6-di(3-pyridyl)-phenylaminyl (2b), and N-[(2,4-dichlorophenyl)thio]-2,6-diphenyl(4-pyridyl)aminyl (3) were generated by PbO2 oxidation of the corresponding precursors. Although 3 was not sufficiently stable to be isolated, both 1 and 2 persisted in solution without decomposition and could be isolated as radical crystals. X-ray crystallographic analysis of 1b revealed that the Ar-N-S-Ar' π-framework is approximately planar and the 2- and 6-phenyl groups are significantly twisted from this plane. The magnetic susceptibility measurements for the isolated radical crystals were carried out using a SQUID magnetometer in the temperature range 1.8-300 K. The susceptibilities of 1a and 2a were explained in terms of a one-dimensional (1D) antiferromagnetic (AFM) regular Heisenberg model with an exchange interaction of 2J/k(B) = -63.4 and -17.8 K, respectively, and that of 1b was interpreted in terms of a 1D AFM alternating Heisenberg model with 2J/k(B) = -12.8 K and α (alternation parameter) = 0.91. On the other hand, that of 2b was explained in terms of a 1D ferromagnetic regular Heisenberg model with 2J/k(B) = 22.4 K.
- Miura, Yozo,Kurokawa, Shinya,Nakatsuji, Masaaki,Ando, Kenjiro,Teki, Yoshio
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p. 8295 - 8303
(2007/10/03)
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- STEROID RECEPTOR MODULATOR COMPOUNDS AND METHODS
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Non-steroidal compounds which are high affinity, high selectivity modulators for steroid receptors are disclosed. Also disclosed are pharmaceutical compositions incorporating such compounds, methods for employing the disclosed compounds and compositions for treating patients requiring steroid receptor agonist or antagonist therapy, intermediates useful in the preparation of the compounds and processes for the preparation of the steroid receptor modulator compounds.
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- STEROID RECEPTOR MODULATOR COMPOUNDS AND METHODS
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Non-steroidal compounds which are high affinity, high selectivity modulators for steroid receptors are disclosed. Also disclosed are pharmaceutical compositions incorporating such compounds, methods for employing the disclosed compounds and compositions for treating patients requiring steroid receptor agonist or antagonist therapy, intermediates useful in the preparation of the compounds and processes for the preparation of the steroid receptor modulator compounds.
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- 6-(1H-imidazol-1-yl)-7-nitro-2,3 (1H,4H)-quinoxalinedione hydrochloride (YM90K) and related compounds: Structure-activity relationships for the AMPA- type non-NMDA receptor
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A novel series of quinoxalinediones possessing imidazolyl and related heteroaromatic substituents was synthesized and evaluated for their activity to inhibit [3H]AMPA binding from rat whole brain. From the structure- activity relationships, it was found that the 1H-imidazol-1-yl moiety could function as a bioisostere for the cyano and nitro groups, and that 6-(1H- imidazol-yl)-7-nitro-2,3(1H,4H)-quinoxalinedione (11) showed the most potent activity for the AMPA receptor. Compound 11 was evaluated for selectivity versus other excitatory amino acid receptors, and its action against AMPA at its receptor in the rat striatum was characterized. These data showed that compound 11 was a selective antagonist for the AMPA receptor with a K(i) value of 0.084 μM, being approximately equipotent with 2,3-dihydro-6-nitro- 7-sulfamoylbenzo(f)quinoxaline (3) (NBQX; K(i) = 0.060 μM). Compound 11 was also found to give protection against sound-induced seizure on DBA/2 mice at the minimum effective dose of 3 mg/kg ip (3; 10 mg/kg ip).
- Ohmori,Sakamoto,Kubota,Shimizu-Sasamata,Okada,Kawasaki,Hidaka,Togami,Furuya,Murase
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p. 467 - 475
(2007/10/02)
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- Pyridyl-substituted-benzofurans
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The present invention provides novel pyridinyl-benzofurans and derivatives thereof which are useful as thromboxane A2 (TXA2) synthetase inhibitors and as such represent potent pharmacological agents.
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- A REGIOSPECIFIC PHOTOREACTION FOR SYNTHESIS OF 3-PHENYLPYRIDINES
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The regiospecific photocoupling of 3-(4-chlorophenyl)-1,1-dimethylurea with pyridine to afford 3-(4-dimethylureidophenyl)pyridine was used to develop a synthetic scheme for the preparation of 3-phenylpyridine.
- Tanaka, Fred S.,Wien, Ronald G.,Hoffer, Barry L.
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p. 951 - 958
(2007/10/02)
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