88138-53-8

Upstream product

• 100-02-7 4-nitro-phenol 
• 4549-32-0 1,8-dibromooctane 

Downstream Products

• 99601-89-5 [8-(4-Nitro-phenoxy)-octyl]-phenyl-amine 
• 94680-04-3 1,8-bis(4-nitrophenoxy)octane 
• 1392196-84-7 methyl 5-((4-(8-azidooctyloxy)phenyl)diazenyl)-2-hydroxybenzoate 
• 1392196-83-6 5-((4-(8-azidooctyloxy)phenyl)diazenyl)-2-hydroxybenzoic acid 
• 1392196-82-5 5-((4-(8-bromooctyloxy)phenyl)diazenyl)-2-hydroxybenzoic acid 
• 1223425-95-3 1-[8-(4-nitrophenoxy)octyl]piperidin-4-one 

Relevant academic research and scientific papers

Synthesis, optimization, in vitro and in vivo study of bicyclic substituted amine as MenA inhibitor

Menaquinone (MK) plays essential role in the electron transport chain (ETC), suggesting MK biosynthesis enzymes as potential targets for drug development. Previously, we demonstrated that Methicillin-resistant Staphylococcus aureus (MRSA) is susceptible t

Synthesis and Antileishmanial Evaluation of Arylimidamide-Azole Hybrids Containing a Phenoxyalkyl Linker

Due to the limitations of existing medications, there is a critical need for new drugs to treat visceral leishmaniasis. Since arylimidamides and antifungal azoles both show oral activity in murine visceral leishmaniasis models, a molecular hybridization approach was employed where arylimidamide and azole groups were separated by phenoxyalkyl linkers in an attempt to capitalize on the favorable antileishmanial properties of both series. Among the target compounds synthesized, a greater antileishmanial potency against intracellular Leishmania donovani was observed as the linker length increased from two to eight carbons and when an imidazole ring was employed as the terminal group compared to a 1,2,4-triazole group. Compound 24c (N-(4-((8-(1H-imidazol-1-yl)octyl)oxy)-2-isopropoxyphenyl) picolinimidamide) displayed activity against L. donovani intracellular amastigotes with an IC50 value of 0.53 μM. When tested in a murine visceral leishmaniasis model, compound 24c at a dose of 75 mg/kg/day p.o. for five consecutive days resulted in a modest 33% decrease in liver parasitemia compared to the control group, indicating that further optimization of these molecules is needed. While potent hybrid compounds bearing an imidazole terminal group were also strong inhibitors of recombinant CYP51 from L. donovani, as assessed by a fluorescence-based assay, additional targets are likely to play an important role in the antileishmanial action of these compounds.

Discovery of Diphenoxy Derivatives with Flexible Linkers as Ligands for β-Amyloid Plaques

The highly rigid and planar scaffolds with π-conjugated systems have been widely considered to be indispensable for β-amyloid (Aβ) binding ligands. In this study, a library of diphenoxy compounds with different types of more flexible linkers as Aβ ligands were synthesized and evaluated. Most of them displayed good affinity (Ki1-42aggregates, and some ligands even showed values of Kiless than 10 nM. Structure-activity relationship analysis revealed that modification on the linkers or substituents tolerated great flexibility, which challenged the long-held belief that rigid and planar structures are exclusively favored for Aβ binding. Three ligands were labeled by iodine-125, and they exhibited good properties in vitro and in vivo, which further supported that this flexible scaffold was potential and promising for the development of Aβ imaging agents.

ANTI-FUNGAL TREATMENT

Provided are compounds, methods, and pharmaceutical compositions useful for treatment of fungal infections, e.g., aspergillosis, candidiasis, cryptococcosis, histoplasmosis, and the like. For example, the pharmaceutical composition may include a pharmaceutically acceptable carrier or excipient, and a compound represented by Ar— C(=NR1)NR2— A---X— Y— Het2 and pharmaceutically acceptable salts thereof. Ar may be an optionally substituted aryl or nitrogen- containing heteroaryl. R1 and R2 may independently be H, optionally substituted C1-C6 aikyi, or optionally substituted C3-C6 cyeloalkyi. A may be a bond or an optionally substituted linking moiety comprising 1, 2, or 3 rings. Each ring in the optionally substituted linking moiety may independently be one of: aryl, cyeloalkyi, heterocycloalkyl, and heteroaryl. X may be O, S, amide, or a bond. Y may be optionally substituted C1-C10 alkyi or optionally substituted C2-C10 alkenyl. Het2 may be an optionally substituted five-membered nitrogen-containing heteroaromatic ring comprising 1, 2, or 3 ring heteroatoms.

ANTI-PARASITIC COMPOUNDS

Provided are compounds, methods, and pharmaceutical compositions useful for treatment of parasites, e.g., Leishmania. For example, the compound may he represented by Ar—C(=NR1)NR2—A—X—Y—Het2, and pharmaceutically acceptable salts thereof. Ar may be an optionally substituted, aryl or nitrogen-containing heteroaryl. R1 and R2 may independently represent H, optionally substituted C1-C6 alkyl, or optionally substituted C3-C6 cycloalkyl. A may be a bond or an optionally substituted linking moiety comprising 1, 2, or 3 rings. Each ring in the optionally substituted linking moiety may independently be one of: aryl, cycloalkyl, heterocycloalkyl, and heteroaryl. X may be O, S, amide, or a bond. Y may be optionally substituted C1-C14 alkyl or optionally substituted C2-C14 alkenyl. Het2 may be an optionally substituted five-membered nitrogen-containing heteroaromatic ring comprising 1, 2, or 3 ring heteroatoms.

Diphenoxyl flexible molecules with high affinity with A[beta] plaque and preparation method and applications thereof

The invention discloses diphenoxyl flexible molecules with high affinity with A[beta] plaque and a preparation method and applications thereof. After the molecules are labeled by radionuclide, the molecules can be used as an A[beta] plaque developing agen

Method and compositions for targeted drug delivery to the lower GI tract

A composition and method for targeted delivery of substances to the lower GI tract comprises a base or scaffold carrier to which a drug or prodrug is fixed or covalently attached. Compound, when taken orally travels through the GI tract of a patient to th

Design, synthesis, and testing of a molecular truck for colonic delivery of 5-aminosalicylic acid

A molecular scaffold bearing eight terminal alkyne groups was synthesized from sucrose. Eight copies of an azide-terminated, azo-linked precursor to 5-aminosalicylic acid were attached to the scaffold via copper(I)-catalyzed azide-alkyne cycloaddition. Th

Hybrid ortho/allosteric ligands for the adenosine A1 receptor

Many G protein-coupled receptors (GPCRs), including the adenosine A 1 receptor (A1AR), have been shown to be allosterically modulated by small molecule ligands. So far, in the absence of structural information, the exact location of

Bifunctional Reactivity of the Nitrophenoxyl Group in Intramolecular Photoreactions

The photochemical behavior of a homologous series of compounds, p-O2NC6H4O(CH2)nNHPh (n = 2-10, 12, and 16) in acetonitrile is reported.The lower (n = 2-6) homologues undergo an apparently nucleophilic type rearrangement to give ω-((p-nitrophenyl)amino)al