Some scientific research about 22013-33-8

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Discovery of novel guanidinophenylpyrazole human acrosin inhibitors by molecular hybridization

Human acrosin is a promising target for male contraceptives. A series of novel guanidinophenylpyrazole derivatives were rationally designed by molecular hybridization of the phenylpyrazole and guanidinobenzoate inhibitors. Most of the target compounds showed potent human acrosin inhibitory activities. In particular, compound F3 was a highly active human acrosin inhibitor (IC50 = 1.26 muM) with good selectivity over trypsin. Molecular docking studies revealed that compound F3 formed hydrophobic and hydrogen bonding interactions with the active site of human acrosin. Compound F3 represents a promising lead compound for the development of novel male contraceptives.

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Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

Brief introduction of 22013-33-8

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Angiotensin converting enzyme inhibitors: N-substituted monocyclic and bicyclic amino acid derivatives

The synthesis of N-(3-mercaptopropionyl)-N-arylglycines (14a-x), -N-arylalanines (15a,b), -N-cycloalkylglycines (16a-k), and -1,2,3,4-tetrahydroisoquinoline-3-carboxylic acids (17a-d), -1,2,3,4-tetrahydroquinoline-2-carboxylic acids (18a-f), and -indoline-2-carboxylic acids (19a-k) is described. In vitro inhibition of angiotensin converting enzyme (ACE) is reported for each compound, and the structure-activity relationship for each series is discussed. The in vivo inhibition of ACE and antihypertensive effects of representative compounds from each series are discussed. The most potent compound, 19d, had an in vitro ACE IC50 of 2.6 x 10-9 M and lowered blood pressure in spontaneous hypertensive rats 85 mm at a dose of 10 mg/kg po.

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Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

Brief introduction of 2,3-Dihydrobenzo[b][1,4]dioxine-5-carboxylic acid

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ISOINDOLINE DERIVATIVES FOR USE IN THE TREATMENT OF A VIRAL INFECTION

Compounds of Formula I are disclosed and methods of treating viral infections with compositions comprising such compounds (Formula I)

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Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

Discovery of 2,3-Dihydrobenzo[b][1,4]dioxin-6-amine

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Dihydrofuro[3,4-b]quinolin-1-one compounds

The invention relates to compound of formula (I): wherein:represents a single or double bond,R0 represents hydrogen or hydroxy or alkoxy,R1 and R2, which are identical or different, each represents hydrogen or halogen or alkyl, alkoxy, hydroxy, polyhaloalkyl, nitro or optionally substituted amino or ?wherein m represents an integer such that 13 represents hydrogen or aryl, heteroaryl, cycloalkyl, optionally substituted alkyl or a group of formula COR7 wherein R7 represents aryl, optionally substituted alkyl, optionally substituted amino or OR10 wherein R10 represents aryl or optionally substituted alkyl,X represents oxygen or sulphur or ?CH2? or ?CH2?CH2?,Ar represents aryl, heteroaryl or arylalkyl,its optical isomers, its hydrates, solvates, and also its addition salts with a pharmaceutically acceptable acid.Medicinal products containing the same are useful in the treatment of cancer.

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Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

More research is needed about 2,3-Dihydrobenzo[b][1,4]dioxine-5-carboxylic acid

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Discovery of novel aminothiadiazole amides as selective EP3 receptor antagonists

This Letter discloses a series of 2-aminothiadiazole amides as selective EP3 receptor antagonists. SAR optimization resulted in compounds with excellent functional activity in vitro. In addition, efforts to optimize DMPK properties in the rat are discussed. These efforts have resulted in the identification of potent, selective EP3 receptor antagonists with excellent DMPK properties suitable for in vivo studies.

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Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

Final Thoughts on Chemistry for (S)-1,4-Benzodioxane-2-carboxylic acid

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Direct synthesis of N-acylalkylenediamines from carboxylic acids under mild conditions

Monoacylated piperazine derivatives were prepared directly from carboxylic acids and piperazine using triphenylphosphine (TPP) and N-bromosuccinimide (NBS) in dichloromethane. Inexpensive and readily available reagents, excellent yields, short reaction times and mild reaction conditions are important features of this method.

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Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

New explortion of 2,3-Dihydrobenzo[b][1,4]dioxin-6-amine

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New analogues of camptothecin, their use as medicaments and the pharmaceutical compositions containing them

A compound of the formula 1wherein the substituents are defined as in the specification which compounds are useful in the treatment of cancer.

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Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

Top Picks: new discover of 2879-20-1

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Reference of 2879-20-1, Catalysts function by providing an alternate reaction mechanism that has a lower activation energy than would be found in the absence of the catalyst. In some cases, the catalyzed mechanism may include additional steps.In a article, 2879-20-1, molcular formula is C10H10O3, introducing its new discovery.

A new protocol for the construction of pyrrolo[4,3,2-de]quinolinones

A facile method has been suggested for constructing pyrrolo[4,3,2-de]quinolinones by addition of acetophenones to 4-nitroisatin followed by reduction of the nitro group and spontaneous cyclisation.

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Reference£º
Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

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Preparation of a camptothecin derivative by intramolecular cyclisation

The present invention relates to a method for the preparation of camptothecin and camptothecin-like compounds and to novel intermediates used in this preparation. In particular, the invention provides a process for the preparation of the camptothecin derivative of formula (I’) known by the chemical name “7-(4-methylpiperazino-methylene)-10,11-ethylenedioxy-20(R,S)-camptothecin”, which comprises cyclising the compound of formula (II’), wherein X is halogen, particularly chloro, bromo, or iodo; and when the compound of formula (I’) is obtained as a mixture of enantiomers optionally resolving the mixture to obtain the desired enantiomer, and/or if desired, converting the resulting compound of formula (I’) or a salt thereof into a physiologically acceptable salt or solvate thereof.

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Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

Discovery of 1-(2,3-Dihydrobenzo[b][1,4]dioxin-6-yl)ethanone

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Hydrochloric acid as an efficient catalyst for intermolecular condensation of alcohols. A simple and highly efficient synthesis of unsymmetrical ethers from benzylic alcohols and alkanols

Benzylic alcohols and diarylmethanols with electron-donating substituents in the aromatic ring reacted with aliphatic alcohols in the presence of a catalytic amount of HCl to give the corresponding alkyl arylmethyl ethers. The reactivity of diarylmethanols in the intermolecular dehydration depended on the nature of substituents in the aromatic rings and structure of aliphatic alcohol.

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Reference£º
Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem