313350-41-3

Upstream product

• 27018-76-4 1-benzylindole-3-carboxylic acid 
• 79-37-8 oxalyl dichloride 
• 100-39-0 benzyl bromide 
• 942-24-5 3-methoxycarbonylindole 
• 155134-26-2 1-Benzyl-1H-indole-3-carboxylic acid methyl ester 
• 771-50-6 1H-indole-3-carboxylic acid 
• 487-89-8 Indole-3-carboxaldehyde 
• 10511-51-0 1-Benzylindole-3-carboxaldehyde 

Downstream Products

• 1016011-15-6 N-n-propyl-1-benzylindole-3-carboxamide 
• 1093757-05-1 N-ethyl-1-benzylindole-3-carboxamide 
• 1093757-06-2 N-n-butyl-1-benzylindole-3-carboxamide 
• 860611-46-7 N-methyl-1-benzylindole-3-carboxamide 
• 1003598-16-0 C₂₃H₁₈N₂O 
• 877378-90-0 1-benzyl-N-[2-(6-methoxy-2-naphthyl)-2-oxoethyl]-1H-indole-3-carboxamide 
• 848853-53-2 1-benzyl-N-[(3'-bromo-4'-methoxy-1,1'-biphenyl-4-yl)methyl]-N-methyl-1H-indole-3-carboxamide 

Relevant academic research and scientific papers

Pd(II)-Catalyzed asymmetric oxidative annulation of N-alkoxyheteroaryl amides and 1,3-dienes

The first Pd(II)-catalyzed asymmetric oxidative annulation of N-alkoxyaryl amides and 1,3-dienes is reported, which features particular applicability for quick assembly of different types of chiral heterocycles with high yields and enantioselectivities. A novel chiral pyridine-oxazoline bearing a methoxyl group at the C-5 position and a gem-dimethyl group on the oxazoline moiety was found to be crucial for conversion.

Hydroxamic acids block replication of hepatitis c virus

Intrigued by the role of protein acetylation in hepatitis C virus (HCV) replication, we tested known histone deacetylase (HDAC) inhibitors and a focused library of structurally simple hydroxamic acids for inhibition of a HCV subgenomic replicon. While known HDAC inhibitors with varied inhibitory profiles proved to be either relatively toxic or ineffective, structure-activity relationship (SAR) studies on cinnamic hydroxamic acid and benzo[b]thiophen-2-hydroxamic acid gave rise to compounds 22 and 53, which showed potent and selective anti-HCV activity and therefore are promising starting points for further structural optimization and mechanistic studies.

Construction of indoloquinolinones via Pd(II)-catalyzed tandem CC/CN bond formation: Application to the total synthesis of isocryptolepine

Construction of indoloquinolinone skeleton via Pd-catalyzed tandem CC/CN bond formation has been achieved in moderate to good yields. The method was applied toward the total synthesis of the bioactive natural product isocryptolepine in good overall yields.

Effect of indole-3-acetic acid analogs on the differentiation of HL-60 cells

In continuing search for novel cell differentiation agents, a series of derivatives of indole-3-acetic acid and indole-3-carboxylic acid were prepared and tested against HL-60 cells for their differentiation and antiproliferation activities. Among them, N-ethyl-1-benzylindole-3-carboxamide (14) was the most potent, whereas N-methyl 1-benzylindole-3-acetamide (5) and N-methyl 1-benzylindole-3-carboxamide (13) synergistically potentiated with all-trans-retinoic acid to induce cell differentiation as well as antiproliferation. Our results indicate that these compounds are effective cell differentiation and antiproliferation agents in combination with retinoic acid.

OXAZOLO-NAPHTHYL ACIDS AS PLAMINOGEN ACTIVATOR INHIBTOR TYPE-1 (PAI-1) MODULATORS USEFUL IN THE TREATMENT OF THROMBOSIS AND CARDIOVASCULAR DISEASES

The present invention relates to oxazolo-naphthyl acids of the formula (I) and methods of using them to modulate PAI-1 expression and to treat PAI-1 related disorders.

BIPHENYLOXY-ACIDS

The present invention relates generally to substituted biphenyloxy acids (such as 4'-aryl-amido-biphenyl--4(3)-yloxy-acids and 4’-aryl-amidomethyl-biphenyl-4(3)-yloxy-acids) and methods of using them.

6-(Aryl-amido or aryl-amidomethyl)-naphthalen-2-yloxy-acidic derivatives as inhibitors of plasminogen activator inhibitor type-1 (PAI-1)

This invention provides novel compounds, pharmaceutical compositions and methods of treating thrombotic disorders in mammals, the compounds having the formula: Wherein: Ar is phenyl, naphthyl, furanyl, benzofuranyl, indolyl, pyrazolyl, oxazolyl, fluorenyl, phenylcycloalkane where the cycloalkane can be cyclopropyl, cyclobutyl, cyclopentyl or cyclohexyl and Ar can be optionally substituted by 1 to 3 groups selected from C1-C6 alkyl, C1-C6 alkoxy, hydroxy, phenyl-(CH2)0-6—, phenyl-(CH2)0-6O—, C3-C6 cycloalkyl, —(CH2)—C3-C6 cycloalkyl, halogen, C1-C3 perflouroalkyl and C1-C3 perfluoroalkoxy where phenyl can be substituted with from 1 to 3 groups selected from C1-C6 alkyl, C1-C6 alkoxy, phenyl, halogen, trifluoromethyl or trifluoromethoxy; R1 is hydrogen, C1-C6 alkyl or phenyl-(CH2)1-6— where phenyl can be substituted with C1-C6 alkyl, C1-C6 alkoxy, halo, trifluoromethyl or trifluoromethoxy; R2 and R3 are H, C1-C6 alkyl, phenyl-(CH2)0-3—, halo and C1-C3 perfluoroalkyl where phenyl can be substituted with C1-C6 alkyl, C1-C6 alkoxy, halo, trifluoromethyl or trifluoromethoxy; R4 is —CHR5CO2H or —CH2-tetrazole where R5 is H or benzyl; and n=0 or 1; or a pharmaceutically acceptable salt or ester form thereof.

Indole amide derivatives: Synthesis, structure-activity relationships and molecular modelling studies of a new series of histamine H1-receptor antagonists

A number of indole amide derivatives bearing a basic side chain, in which the indole ring replaces the isoster benzimidazole nucleus typical of some well-known antihistamines, were prepared and tested for their H1- antihistaminic activity. The 1-benzyl-3-indolecarboxamides 32-42 showed antihistaminic (H1) activity (pA2 6-8); the 3-indolylglyoxylylamides 7-16 and the 2-indolecarboxamides 48-56 showed little or no activity. Insertion of the basic side chain of the active 3-indolecarboxamide derivatives into a piperazine ring (compounds 57-59) led to a dramatic loss of activity. All the active compounds proved to be competitive antagonists, since the values of the regression slope were not statistically different from 1. The most active compounds, 32, 33, 38-41, were also tested both in vitro for their anticholinergic activity and in vivo for their ability to antagonize histamine-induced cutaneous vascular permeability in rats. The biological results and the structure-activity relationships of the novel compounds are discussed in the light of molecular modelling studies, taking the molecule of astemizole as a model, and referring to proposed H1-receptor pharmacophore models.