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The present invention relates to novel macrocyclic compounds and methods of treating a hepatitis C infection in a subject in need of such therapy with said macrocyclic compounds. The present invention further relates to pharmaceutical compositions comprising the compounds of the present invention, or pharmaceutically acceptable salts, esters, or prodrugs thereof, in combination with a pharmaceutically acceptable carrier or excipient.

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Isoxazole – Wikipedia,
Isoxazole | C3H3NO – PubChem

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The compounds of the invention exhibit antiprotozoal, antimicrobial, and anticancer properties that are useful for the treatment or prevention of infections or cancer in a patient (e.g., a human). For example, the compounds and methods described herein can be used for the treatment or prevention of protozoal infections such as leishmaniasis, malaria, and trypanosoma infections, bacterial infections such as S. aureus and C. albicans, and cancers such as breast, colon, lung, or prostate cancer. The invention further provides methods of synthesizing such compounds as well as kits useful for administering the compounds.

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Isoxazole – Wikipedia,
Isoxazole | C3H3NO – PubChem

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In the search for novel anticancer drugs, the potassium channel KV10.1 has emerged as an interesting cancer target. Here, we report a new group of KV10.1 inhibitors, namely the purpurealidin analogs. These alkaloids are produced by the Verongida sponges and are known for their wide variety of bioactivities. In this study, we describe the synthesis and characterization of 27 purpurealidin analogs. Structurally, bromine substituents at the central phenyl ring and a methoxy group at the distal phenyl ring seem to enhance the activity on KV10.1. The mechanism of action of the most potent analog 5 was investigated. A shift of the activation curve to more negative potentials and an apparent inactivation was observed. Since KV10.1 inhibitors can be interesting anticancer drug lead compounds, the effect of 5 was evaluated on cancerous and non-cancerous cell lines. Compound 5 showed to be cytotoxic and appeared to induce apoptosis in all the evaluated cell lines.

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Isoxazole – Wikipedia,
Isoxazole | C3H3NO – PubChem

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N,C-capped dipeptides belong to a class of noncovalent proteasome inhibitors. Herein we report that the insertion of a beta-amino acid into N,C-capped dipeptides markedly decreases their inhibitory potency against human constitutive proteasome beta5c, while maintaining potent inhibitory activity against human immunoproteasome beta5i, thereby achieving thousands-fold selectivity for beta5i over beta5c. Structure?activity relationship studies revealed that beta5c does not tolerate the beta-amino acid based dipeptidomimetics as does beta5i. In vitro, one such compound was found to inhibit human T cell proliferation. Compounds of this class may have potential as therapeutics for autoimmune and inflammatory diseases with less mechanism-based cytotoxicity than agents that also inhibit the constitutive proteasome.

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Isoxazole – Wikipedia,
Isoxazole | C3H3NO – PubChem

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The construction of two libraries of triazole-containing isothiazolidine 1,1-dioxides is reported utilizing either a one-pot click/aza-Michael or click/OACC esterification protocol. One core dihydroisothiazole 1,1-dioxide scaffold was prepared rapidly on multigram scale via ring-closing metathesis (RCM) and was subjected to a one-pot multicomponent click/aza-Michael protocol with an array of amines and azides for the generation of a 180-member triazole-containing isothiazolidine 1,1-dioxide library. Alternatively, three daughter scaffolds were generated via the aza-Michael of three amino alcohols, followed by a one-pot, multicomponent click/esterification protocol utilizing a ring-opening metathesis polymerization (ROMP)-derived coupling reagent, oligomeric alkyl carbodiimide (OACC) to generate a 41-member library of triazole-containing isothiazole 1,1-dioxides.

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Isoxazole – Wikipedia,
Isoxazole | C3H3NO – PubChem

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Potent and selective S1P3 receptor (S1P3-R) agonists may represent important proof-of-principle tools used to clarify the receptor biological function and assess the therapeutic potential of the S1P 3-R in cardiovascular, inflammatory and pulmonary diseases. N,N-Dicyclohexyl-5-propylisoxazole-3-carboxamide was identified by a high-throughput screening of MLSMR library as a promising S1P3-R agonist. Rational chemical modifications of the hit allowed the identification of N,N-dicyclohexyl-5-cyclopropylisoxazole-3-carboxamide, a S1P3-R agonist endowed with submicromolar activity and exquisite selectivity over the remaining S1P1,2,4,5-R family members. A combination of ligand competition, site-directed mutagenesis and molecular modeling studies showed that the N,N-dicyclohexyl-5-cyclopropylisoxazole-3-carboxamide is an allosteric agonist and binds to the S1P3-R in a manner that does not disrupt the S1P3-R-S1P binding. The lead molecule herein disclosed constitutes a valuable pharmacological tool to explore the molecular basis of the receptor function, and provides the bases for further rational design of more potent and drug-like S1P3-R allosteric agonists.

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Isoxazole – Wikipedia,
Isoxazole | C3H3NO – PubChem

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A series of 6-aryl-3-pyrrolidinylpyridine analogs was explored as structurally novel negative allosteric modulators of the mGlu5 receptor lacking an alkyne or oxadiazole moiety. Compounds in this series were characterized by tractable SAR, good in vitro potencies and brain penetration in rodents.

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Isoxazole – Wikipedia,
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Design, synthesis, and biological evaluation of peptidomimetic severe acute respiratory syndrome chymotrypsin-like protease (SARS-3CLpro) inhibitors for severe acute respiratory syndrome coronavirus (SARS-CoV) are described. These inhibitors exhibited antiviral activity against SARS-CoV in infected cells in the micromolar range. An X-ray crystal structure of our lead inhibitor (4) bound to SARS-3CLpro provided important drug-design templates for the design of small-molecule inhibitors.

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Isoxazole – Wikipedia,
Isoxazole | C3H3NO – PubChem

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One of the major reasons for studying chemical kinetics is to use measurements of the macroscopic properties of a system, Recommanded Product: 5-Methylisoxazole-3-carboxylic acid, such as the rate of change in the concentration of reactants or products with time.In a article, mentioned the application of 3405-77-4, Name is 5-Methylisoxazole-3-carboxylic acid, molecular formula is C5H5NO3

A variety of methods were used for the preparation of the 5-alkoxymethyl-, 5-alkylthiomethyl,- and 5-dialkylaminomethyl-isoxazoles.A novel method for the separation of the isomeric mixture of 3-(5-)methoxymethyl-5-(3-)methylisoxazoles (obtained by the reaction of 1-methoxypentane-1,3-dione with hydroxylamine), based on the difference in reactivity with n-butyllithium, is described.Methods for the preparation of 5-alkylthiomethylisoxazoles from 5-methylisoxazoles; and 5-alkoxymethylisoxazoles from 5-hydroxymethylisoxazoles are also reported.

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Isoxazole – Wikipedia,
Isoxazole | C3H3NO – PubChem

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Reference of 3405-77-4, Chemistry is the science of change. But why do chemical reactions take place? Why do chemicals react with each other? The answer is in thermodynamics and kinetics.In a document type is Patent, and a compound is mentioned, 3405-77-4, 5-Methylisoxazole-3-carboxylic acid, introducing its new discovery.

Novel phenyl compounds, pharmaceutical compositions containing these compounds, and methods for their pharmaceutical use are disclosed. In certain embodiments, the compounds are agonists and/or ligands of cannabinoid receptors and may be useful, inter alia, for treating and/or preventing pain, gastrointestinal disorders, genitourinary disorders, inflammation, glaucoma, auto-immune diseases, ischemic conditions, immune-related disorders, and neurodegenerative diseases, for providing cardioprotection against ischemic and reperfusion effects, for inducing apoptosis in malignant cells, and as an appetite stimulant.

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Reference:
Isoxazole – Wikipedia,
Isoxazole | C3H3NO – PubChem