2007-12-7

Usage

InChI:InChI=1/C12H9ClO2/c13-12(14)8-15-11-7-3-5-9-4-1-2-6-10(9)11/h1-7H,8H2

Upstream product

• 2976-75-2 1-Naphthoxyacetic acid 
• 90-15-3 α-naphthol 
• 41643-81-6 ethyl (1-naphthalenyloxy)acetate 

Downstream Products

• 64994-92-9 2-(4-methoxy-phenyl)-5-(naphthalen-1-yloxy-acetyl)-5H-oxazolo[4,5-b]phenoxazine 
• 64994-93-0 2-(2-chloro-phenyl)-5-(naphthalen-1-yloxy-acetyl)-5H-oxazolo[4,5-b]phenoxazine 
• 93947-58-1 N-(2-diethylaminoethyl)-2-(naphthalen-1-yloxy)acetamide 
• 64994-94-1 2-(2-hydroxy-phenyl)-5-(naphthalen-1-yloxy-acetyl)-5H-oxazolo[4,5-b]phenoxazine 
• 78961-69-0 1-Aziridin-1-yl-2-(naphthalen-1-yloxy)-ethanone 
• 88556-13-2 2-[2-(Naphthalen-1-yloxy)-acetylamino]-3-phenyl-propionic acid 
• 61057-68-9 [2-(Naphthalen-1-yloxy)-acetylamino]-acetic acid 
• 1164350-74-6 [2-(naphthalen-1-yloxy)acetylamino]phenylacetic acid 
• 1158842-77-3 C₄₆H₄₀N₂O₆ 
• 58645-78-6 naphtho<1,2-a>-1H-furan-3-one 
• 41643-45-2 N,N-Dibutyl-2-(naphthalen-1-yloxy)-acetamide 

Relevant academic research and scientific papers

Benzoic acid derivative as well as preparation method and medicinal application thereof

The invention discloses a benzoic acid derivative as well as a preparation method and a pharmaceutical application thereof, and belongs to the technical field of medicines. The invention specifically discloses a benzoic acid derivative represented by a co

Synthesis of novel 1,2,5-oxadiazoles and evaluation of action against Acinetobacter baumannii

With multidrug resistant bacteria on the rise, novel antibiotics are becoming highly sought after. In 2008, eleven compounds were identified by high throughput screening as inhibitors of BasE, a key enzyme of the non-ribosomal peptide synthetase pathway found in Acinetobacter baumannii. Herein, we describe the preparation of four structurally similar heterocyclic lead compounds from that study, including one 1,2,5-oxadiazole. A further library of 30 analogues containing the oxadiazole moiety was then generated. All compounds were screened against Acinetobacter baumannii and their minimum inhibitory concentration data is reported, with (E)-3-(2-hydroxyphenyl)-N-(4-methyl-1,2,5-oxadiazol-3-yl)acrylamide 32 found to have an MIC of 0.5 mM. This work provides the foundation for further investigation of 1,2,5-oxadizoles as novel inhibitors of A. baumannii.

Isoflavone amide derivatives, their preparation method and medical use

The invention belongs to the field of medicinal chemistry, and relates to derivatives of isoflavones amides, as well as a preparation method and medical application of derivatives, in particular to the derivatives of the isoflavones amides with the general formula of (I) shown as the specification, the preparation method and the medical application of the derivatives, particularly the application of the derivatives of the isoflavones amides serving as medicaments for preventing or treating hyperlipemia, adiposis or type-II diabetes.

Formononetin derivatives and preparation methods and medical application thereof

The invention relates to the field of pharmaceutical chemistry, and relates to formononetin derivatives and preparation methods and medical application thereof, in particular to formononetin derivatives with the general formula as shown in (I), preparation methods thereof, pharmaceutical compositions containing the compounds and medical application of the derivatives and the pharmaceutical compositions, particularly, application of the derivatives and the pharmaceutical compositions serving as drugs for preventing or treating hyperlipidaemia or obesity or type-II diabetes. Please see the formula in the description.

Synthesis and biological evaluation of isoflavone amide derivatives with antihyperlipidemic and preadipocyte antiproliferative activities

A series of isoflavone amides were designed with isoflavone in place of the scaffold of 2-arylbenzoxazole as cholesterol ester transfer protein (CETP) inhibitors. Twelve new compounds were synthesized, and their inhibitory activities of CETP and preadipocyte proliferation were assayed. The hypolipidemic potency of the most effective compound HY-2c was further tested in vivo by hamster. The results indicate that HY-2c exhibited favorable antihyperlipidemic and preadipocyte antiproliferative activities.

Synthesis, biological evaluation, and structure-activity relationships of potent noncovalent and nonpeptidic cruzain inhibitors as anti-Trypanosoma cruzi agents

The development of cruzain inhibitors has been driven by the urgent need to develop novel and more effective drugs for the treatment of Chagas' disease. Herein, we report the lead optimization of a class of noncovalent cruzain inhibitors, starting from an inhibitor previously cocrystallized with the enzyme (Ki = 0.8 μM). With the goal of achieving a better understanding of the structure-activity relationships, we have synthesized and evaluated a series of over 40 analogues, leading to the development of a very promising competitive inhibitor (8r, IC50 = 200 nM, Ki = 82 nM). Investigation of the in vitro trypanocidal activity and preliminary cytotoxicity revealed the potential of the most potent cruzain inhibitors in guiding further medicinal chemistry efforts to develop drug candidates for Chagas' disease.

3-(Arylacetylamino)-N-methylbenzamides: A novel class of selective anti-Helicobacter pylori agents

After chemical modification preceded by the random screening of our chemical library, a novel class of selective anti-Helicobacter pylori agents was generated. Consequently, the 3-(arylacetylamino)-N-methylbenzamides, which were quite easy to prepare, showed potent inhibitory activity against Helicobacter pylori but exhibited no inhibitory activity against other sorts of bacteria and fungi, e.g., Staphylococcus aureus, Bacillus subtilis, Escherichia coli, Pseudomonas aeruginosa, Bacteroides fragilis, and Candida albicans. These compounds showed potent anti-H. pylori activity under acidic conditions, whereas amoxicillin and clarithromycin decreased activity. The 3-(3-arylpropionylamino)-N-methylbenzamides, 3-(aryloxyacetylamino)-N-methylbenzamides, and (3-methylcarbamoylphenyl)carbamic acid 1-arylmethyl esters also exhibited potent anti-H. pylori activity. Finally, we selected 7n (BAS-118) as a candidate compound for further evaluation.

Generation of monospecific nanomolar tyrosine kinase inhibitors via a chemical genetic approach

Selective protein kinase inhibitors are highly sought after as tools for studying cellular signal transduction cascades, yet few have been discovered due to the highly conserved fold of kinase catalytic domains. Through a combination of small molecule syn

Bicyclic N-hydroxyurea inhibitors of 5-lipoxygenase: Pharmacodynamic, pharmacokinetic, and in vitro metabolic studies characterizing N-hydroxy-N-(2,3-dihydro-6-(phenylmethoxy)-3-benzofuranyl)urea

A series of N-hydroxyurea derivatives have been prepared and examined as inhibitors of 5-lipoxygenase. Oral activity was established by examining the inhibition of LTB4 biosynthesis in an ex vivo assay in the mouse. The pharmacodynamic performance in the mouse of selected compounds was assessed using an ex vivo LTB4 assay and an adoptive peritoneal anaphylaxis assay at extended pretreat times. Compounds with an extended duration of action were reexamined as the individual enantiomers in the ex vivo assay, and the (S) enantiomer of N-hydroxy-N-[2,3-dihydro-6-(phenylmethoxy)-3-benzofuranyl]urea, (+)-1a (SB 202235), was selected as the compound with the best overall profile. Higher plasma concentrations and longer plasma half-lives were found for (+)-1a relative to its enantiomer in the mouse, monkey, and dog. In vitro metabolic studies in mouse liver microsomes established enantiospecific glucuronidation as a likely mechanism for the observed differences between the enantiomers of 1a. Enantioselective glucuronidation favoring (-)-1a was also found in human liver microsomes.

SYNTHESIS OF NEW N-ACYL DERIVATIVES OF DL-TRANS-1,2-AMINOCYCLOHEXANOL

New amide derivatives of Dl-trans-1,2-aminocyclohexanol, with a potential action on the cardiovascular system, were obtained.Keywords: N-acyl derivatives of DL-trans-1,2-aminocyclohexanol, elemental analysis, 1H NMR.