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Ethylene bis-imidazoles are highly potent and selective activators for isozymes VA and VII of carbonic anhydrase, with a potential nootropic effect

A series of ethylene bis-imidazoles was synthesized via a novel microwave-mediated synthesis. Biological testing on eight isozymes of carbonic anhydrase (CA) present in the human brain revealed compounds with nanomolar potency against CA VA and CA VII, also displaying excellent selectivity against other CA isozymes present in this organ. the Partner Organisations 2014.

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Tetrahydropyran – Wikipedia,
Tetrahydropyran – an overview | ScienceDirect Topics

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Inhibitors of human nitric oxide synthase isoforms with the carbamidine moiety as a common structural element

Identification of potent and selective inhibitors of inducible nitric oxide synthase (NOS) is of great interest because of their therapeutic potential for treatment of diseases mediated by excess production of nitric oxide. We present here a comparison of potency and selectivity for amino acid and nonamino acid based compounds as inhibitors of human inducible, human endothelial constitutive and human neuronal constitutive NOS isoforms. In addition, a novel series of substituted amidines has been identified as NOS inhibitors. 2-Methylthioacetamidine and 2-thienylarbamidine were the most potent of the series examined with IC50 values of 3.9 and 2.9 muM for human neuronal constitutive NOS. Cyclopropylcarbamidine and 2-thienylcarbamidine were the most potent inhibitors for human inducible NOS with IC50 values of 5.2 and 6.5 muM, respectively. These substituted amidines represent a new class of NOS inhibitors and provide a foundation for potential therapeutic agents.

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Tetrahydropyran – Wikipedia,
Tetrahydropyran – an overview | ScienceDirect Topics

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Vinylogous tetraazafulvalenes: New deeply coloured compounds derived from simple amidines

A one-step synthesis of vinylogous tetraazafulvalenes by simple cycloacylation of acetamidine 2 with bisimidoyl chlorides of oxalic acid 1 is described. The deeply coloured products 4a-i constitute a new class of stable neutrocyanines as well as compounds with indigoid properties.

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Tetrahydropyran – Wikipedia,
Tetrahydropyran – an overview | ScienceDirect Topics

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Structure-activity relationships of a series of pyrrolo[3,2-d]pyrimidine derivatives and related compounds as neuropeptide Y5 receptor antagonists

Neuropeptide Y (NPY) has been shown to play an important role in the regulation of food intake and energy balance. Pharmacological data suggests that the Y5 receptor subtype contributes to the effects of NPY on appetite, and therefore a Y5 antagonist might be a useful therapeutic agent for the treatment of obesity. In attempts to identify potential Y5 antagonists, a series of pyrrolo[3,2-d]pyrimidine derivatives was prepared and evaluated for their ability to bind to Y5 receptors in vitro. We report here the synthesis and initial structure-activity relationship investigations for this class of compounds. The target compounds were prepared by a variety of synthetic routes designed to modify both the substitution and the heterocyclic core of the pyrrolo[3,2-d]pyrimidine lead 1. In addition to identifying several potent Y5 antagonists for evaluation as potential antiobesity agents, a pharmacophore model for the human Y5 receptor is presented.

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Tetrahydropyran – Wikipedia,
Tetrahydropyran – an overview | ScienceDirect Topics

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Antimalarial activity of 4-amidinoquinoline and 10-amidinobenzonaphthyridine derivatives

Chloroquine (CQ) has been used as first line malaria therapeutic drug for decades. Emergence of CQ drug-resistant Plasmodium falciparum malaria throughout endemic areas of the world has limited its clinical value. Mefloquine (MQ) has been used as an effective malaria prophylactic drug due to its being long-acting and having a high potency against blood stage P. falciparum (Pf). However, serious CNS toxicity of MQ has compromised its clinical value as a prophylaxis drug. Therefore, new and inexpensive antimalarial drugs with no cross-resistance to CQ or CNS toxicity are urgently needed to combat this deadly human disease. In this study, a series of new 4-amidinoquinoline (4-AMQ) and 10-amidinobenzonaphthyridine (10-AMB) derivatives were designed, prepared, and assessed to search for new therapeutic agents to replace CQ and MQ. The new derivatives displayed high activity in vitro and in vivo, with no cross-resistance to CQ, and none were toxic in mice up to 160 mpk ¡Á 3. The best compound shows IC50 < 1 ng/mL against D6, W2 and C235 Pf clones, low inhibitory activity in hERG K+ channel blockage testing, negativity in the Ames test, and 5/5 cure @ <15 mpk ¡Á 3 in mice infected with Plasmodium berghei. In addition to these desirable pharmacological profiles, compound 13b, one of the most active compounds, is metabolically stable in both human and mouse liver microsomal preparations and has a plasma t1/2 of 50 h in mice, which made it a good MQ replacement candidate. Do you like my blog? If you like, you can also browse other articles about this kind. Application In Synthesis of 2H-Pyran-3,5(4H,6H)-dione. Thanks for taking the time to read the blog about 61363-56-2

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Tetrahydropyran – Wikipedia,
Tetrahydropyran – an overview | ScienceDirect Topics

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Synthesis and Biological Activity of New HMG-CoA Reductase Inhibitors. 1. Lactones of Pyridine- and Pyrimidine-Substituted 3,5-Dihydroxy-6-heptenoic (-heptanoic) Acids

Lactones of pyridine- and pyrimidine-substituted 3,5-dihydroxy-6-heptenoic (-heptanoic) acids 2-4 have been synthesized.Extensive exploration of structure-activity relationships led to several compounds exceeding the inhibitory activity of mevinolin (1b) on HMG-CoA reductase, both in vitro and in vivo.First clinical trials with 2i (HR 780) are in preparation.

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Tetrahydropyran – Wikipedia,
Tetrahydropyran – an overview | ScienceDirect Topics

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Concise, flexible syntheses of 4-(4-imidazolyl)pyrimidine cyclin-dependent kinase 2 (CDK2) inhibitors

A flexible six-step synthesis of potential cyclin-dependent kinase 2 (CDK2) inhibitors is reported. The synthesis involves the condensation between 3-chloro-4,4-dimethoxy-2-butanone and amidines, which provides acetyl-imidazoles and late stage palladium-catalyzed N-arylation to give the target pyrimidine derivatives.

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Tetrahydropyran – Wikipedia,
Tetrahydropyran – an overview | ScienceDirect Topics

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Amidines of diphenyl sulfones, their derivatives and their use

This disclosure describes novel diphenyl sulfones, diphenyl sulfides, and diphenyl sulfoxides, which possess activity as modulators of the mammalian immune response system.

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Tetrahydropyran – Wikipedia,
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NOVEL PYRIMIDINE DERIVATIVE AND NOVEL PYRIDINE DERIVATIVE

Achiral pyrimidine derivatives and pyridine derivatives of the following formulae or analogs thereof have selective N-type calcium channel antagonistic activity and showed analgesic action when they were taken orally. They are useful as therapeutic agents for pains and various diseases associated with the N-type calcium channels.

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Reference£º
Tetrahydropyran – Wikipedia,
Tetrahydropyran – an overview | ScienceDirect Topics

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SUBSTITUTED BENZENE FUNGICIDES

Disclosed are compounds of Formula 1, including all geometric and stereoisomers, N-oxides, and salts thereof, wherein W is O or S; V is a direct bond or NR3; Q is or CR6aR6b, O, NR7, C=N-O-R7 or C(=O); Y is -C(R5)=N-O-(CR8aR8b)p-X-(CR9aR9b)q-SiR10aR10bR10c; or a phenyl ring subr stituted as defined in the disclosure; or Z; and R1, R2, R3, R4, R5, R6a, R6b, R7, R8a, R8b, R9a, R9b, R10a, R10b, R10c, Z, p and q 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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Reference£º
Tetrahydropyran – Wikipedia,
Tetrahydropyran – an overview | ScienceDirect Topics