62246-94-0

Usage

Uses

Due to the limited information available on AKOS 94039, it is not possible to list specific applications or industries where it is used. However, given that AKOS is known for supplying chemicals and biochemicals for scientific, laboratory, or industrial purposes, it can be inferred that AKOS 94039 may be used in similar contexts. To understand the exact applications and industries, it is essential to consult the product's material safety data sheet (MSDS) or contact the manufacturer directly.

InChI:InChI=1/C12H8ClNO/c13-11-3-1-2-10(8-11)12(15)9-4-6-14-7-5-9/h1-8H

Upstream product

• 872-85-5 pyridine-4-carbaldehyde 
• 36229-42-2 (3-chlorophenyl)magnesium bromide 
• 59347-49-8 1-(3-chloro-benzyl)-pyridinium; bromide 
• 100-48-1 pyridine-4-carbonitrile 
• 108-37-2 1-bromo-3-chlorobenzene 

Downstream Products

• 949934-40-1 (3-chlorophenyl)[4-(pyrrolidin-1-ylmethyl)phenyl](pyridin-4-yl)methanol 
• 1585241-54-8 (3Z)-4-(3-chlorophenyl)-N,N-dimethyl-4-(4-pyridyl)but-3-en-1-ammonium trifluoroacetate 
• 1585241-56-0 (3E)-4-(3-chlorophenyl)-N,N-dimethyl-4-(4-pyridyl)but-3-en-1-ammonium trifluoroacetate 

Relevant academic research and scientific papers

Photocatalyst-controlled and visible light-enabled selective oxidation of pyridinium salts

This study proposes two different methods of photocatalytic-controlled and visible light-induced selective oxidation of pyridiniums with air as the terminal oxidant. The key to these transformations is to choose the appropriate light source and photocatal

Chlorpheniramine Analogues Reverse Chloroquine Resistance in Plasmodium falciparum by Inhibiting PfCRT

The emergence and spread of malaria parasites that are resistant to chloroquine (CQ) has been a disaster for world health. The antihistamine chlorpheniramine (CP) partially resensitizes CQ-resistant (CQR) parasites to CQ but possesses little intrinsic antiplasmodial activity. Mutations in the parasite's CQ resistance transporter (PfCRT) confer resistance to CQ by enabling the protein to transport the drug away from its site of action, and it is thought that resistance-reversers such as CP exert their effect by blocking this CQ transport activity. Here, a series of new structural analogues and homologues of CP have been synthesized. We show that these compounds (along with other in vitro CQ resistance-reversers) inhibit the transport of CQ via a resistance-conferring form of PfCRT expressed in Xenopus laevis oocytes. Furthermore, the level of PfCRT-inhibition was found to correlate well with both the restoration of CQ accumulation and the level of CQ resensitization in CQR parasites.

Clotrimazole scaffold as an innovative pharmacophore towards potent antimalarial agents: Design, synthesis, and biological and structure-activity relationship studies

We describe herein the design, synthesis, biological evaluation, and structure-activity relationship (SAR) studies of an innovative class of antimalarial agents based on a polyaromatic pharmacophore structurally related to clotrimazole and easy to synthesize by low-cost synthetic procedures. SAR studies delineated a number of structural features able to modulate the in vitro and in vivo antimalarial activity. A selected set of antimalarials was further biologically investigated and displayed low in vitro toxicity on a panel of human and murine cell lines. In vitro, the novel compounds proved to be selective for free heme, as demonstrated in the β-hematin inhibitory activity assay, and did not show inhibitory activity against 14-α-lanosterol demethylase (a fungal P450 cytochrome). Compounds 2, 4e, and 4n exhibited in vivo activity against P. chabaudi after oral administration and thus represent promising antimalarial agents for further preclinical development.

ANTIMALARIAL AGENTS HAVING POLYAROMATIC STRUCTURE

Antimalarial agents having a novel pharmacophore of formula (I) are herein described. These polycyclic compounds are able to inhibit chloroquine-sensitive and chloroquine-resistant strains ofPlasmodium falciparum (Pf). Furthermore, the synthesis of these compounds involves few steps from commercial products with low cost of production.Λa présente invention concerne des agents antimalariaux comportant un nouveau pharmacophore de formule (I). Ces composés polycycliques sont susceptibles d''inhiber les souches sensibles à la chloroquine et résistantes à la chloroquine de Plasmodium falciparum (Pf). En outre, la synthèse de ces composés est peu onéreuse et implique peu d''étapes à partir des produits commerciaux.