443998-69-4

Upstream product

• 106-40-1 4-bromo-aniline 
• 89711-08-0 N-(t-butoxycarbonyl)glycinal 

Downstream Products

• 865788-38-1 (2-{N-(4-bromophenyl)-N-[(3-methyl-3H-imidazol-4-yl)methyl]amino}ethyl)carbamic acid tert-butyl ester 
• 910910-76-8 {2-[(4-bromophenyl)-(3H-imidazol-4-ylmethyl)amino]ethyl}carbamic acid tert-butyl ester 
• 926031-06-3 1-methyl-1H-imidazole-4-sulfonic acid {2-[(4-bromophenyl)-(3H-imidazol-4-ylmethyl)amino]ethyl}amide 
• 912482-47-4 N-(4-bromophenyl)-N-(3-methyl-3H-imidazol-4-ylmethyl)-N'-pyridin-2-ylmethylethane-1,2-diamine 
• 865788-41-6 N'-benzyl-N-(4-bromophenyl)-N-[(3-methyl-3H-imidazol-4-yl)methyl]ethane-1,2-diamine 

Relevant academic research and scientific papers

Discovery of a Potent, Selective, and Brain-Penetrant Small Molecule that Activates the Orphan Receptor GPR88 and Reduces Alcohol Intake

The orphan G-protein-coupled receptor GPR88 is highly expressed in the striatum. Studies using GPR88 knockout mice have suggested that the receptor is implicated in alcohol seeking and drinking behaviors. To date, the biological effects of GPR88 activatio

Discovery of N-(2-aminoethyl)-N-benzyloxyphenyl benzamides: New potent Trypanosoma brucei inhibitors

A phenotypic screen of a compound library for antiparasitic activity on Trypanosoma brucei, the causative agent of Human African Trypanosomiasis (HAT), led to the identification of N-(2-aminoethyl)-N-phenyl benzamides as a starting point for hit-to-lead m

Synthesis, pharmacological characterization, and structure - Activity relationship studies of small molecular agonists for the orphan GPR88 receptor

GPR88 is an orphan G-protein-coupled receptor (GPCR) enriched in the striatum. Genetic deletion and gene expression studies have suggested that GPR88 plays an important role in the regulation of striatal functions and is implicated in psychiatric disorder

POLYCYCLIC COMPOUNDS AND METHODS OF MAKING AND USING THE SAME

The present disclosure provides compounds, or pharmaceutically acceptable salts thereof, for inhibiting the growth of a microbe; treating a mammal having a microbial infection, malaria, mucositis, an ophthalmic infection, an otic infection, a cancer, or a Mycobacterium infection; killing or inhibiting the growth of a Plasmodium species; inhibiting the growth of a Mycobacterium species; modulating an immune response in a mammal; or antagonizing unfractionated heparin, low molecular weight heparin, or a heparin/low molecular weight heparin derivative.

Structurally simple, potent, Plasmodium selective farnesyltransferase inhibitors that arrest the growth of malaria parasites

Third world nations require immediate access to inexpensive therapeutics to counter the high mortality inflicted by malaria. Here, we report a new class of antimalarial protein farnesyltransferase (PFT) inhibitors, designed with specific emphasis on simple molecular architecture, to facilitate easy access to therapies based on this recently validated antimalarial target. This novel series of compounds represents the first Plasmodium falciparum selective PFT inhibitors reported (up to 145-fold selectivity), with lead inhibitors displaying excellent in vitro activity (IC50 50 100 nM). Initial studies of absorption, metabolism, and oral bioavailability are reported.

COMPOUNDS AND METHODS FOR THE TREATMENT OF MALARIA AND CANCER

Formula (I): Where R1 is an optionally substituted C3-C12 hydrocarbyl group (preferably a cyclic alkyl group), an optionally substituted heterocyclic group, an optionally substituted aromatic group or an optionally substituted heteroaromatic group; R is a C(O)yR' group (preferably forming an optionally substituted C2-C5 acyl group), or a S(O)xR' group, where y is 0 or 1 and x is 0, 1 or 2 and R' is H or an optionally substituted C1-C12 alkyl group, or R' is an optionally substituted C5-C12 cycloalkyl group, an optionally substituted heterocyclic group, an optionally substituted aromatic group or an optionally substituted heteroaromatic group; R5, R6, R7, R8, R9 and R10 are each independently selected from H, an optionally substituted C1-C12 hydrocarbyl group, including a C5-C12 cycloalkyl group, an optionally substituted heterocyclic group, an optionally substituted aromatic group or an optionally substituted heteroaromatic group, or R5 and R6, R7 and R8 or R9 and R10 together form a keto (C=O) group; RN is H, an optionally substituted C1-C12 hydrocarbyl group, an optionally substituted heterocyclic group, an optionally substituted aromatic group, or an optionally substituted heteroaromatic group; A is Formula (II): a Formula (III): group, or a Formula (IV) or Formula (V) group, where Z is N, O or S; Ra is H, a C1-C12 optionally substituted hydrocarbyl group or an optionally substituted aromatic group; n is from 0 to 3; and pharmaceutically acceptable salts thereof. Compounds according to the invention are useful in one or more aspects to inhibit farnesyl transferase, or to treat malaria, neoplasia, a hyperproliferative disease state or arthritis, including rheumaroid arthritis or osteoarthritis.

Structurally simple farnesyltransferase inhibitors arrest the growth of malaria parasites

(Chemical Equation Presented) Antimalarial compounds: Structurally simple acyclic inhibitors of protein farnesyltransferase (active-site model shown) from the malaria parasite Plasmodium falciparum may allow third world countries access to an effective and inexpensive antimalarial therapy to counter the estimated half billion infections that occur annually.