75912-83-3

Upstream product

• 75912-69-5 1-[2-(4-nitro-phenoxy)ethyl]-1H-imidazole 
• 3383-72-0 1-(2-chloroethoxy)-4-nitrobenzene 
• 38519-63-0 4-[2-(diethylamino)ethoxy]aniline 
• 6160-65-2 1,1'-Thiocarbonyldiimidazole 
• 100-02-7 4-nitro-phenol 
• 16365-27-8 2-(4-nitrophenoxy)ethanol 
• 350-46-9 4-Fluoronitrobenzene 
• 13288-06-7 1-(2-bromoethoxy)-4-nitrobenzene 
• 7439-89-6 iron 
• 123-30-8 4-amino-phenol 
• 288-32-4 1H-imidazole 
• 116755-59-0 4-(2-bromoethoxy)phenylamine 

Downstream Products

• 75912-85-5 <4-<2-(1H-imidazol-1-yl)ethoxy>phenyl>urea 
• 497852-44-5 7-[4-(2-butoxyethoxy)phenyl]-N-[4-[2-(imidazol-1-yl)ethoxy]phenyl]-1-propyl-2,3-dihydro-1-benzazepine-4-carboxamide 
• 1567434-02-9 C₂₃H₁₉N₅O₃ 
• 627463-40-5 1-[2-(4-isothiocyanato-phenoxy)-ethyl]-1H-imidazole 

Relevant academic research and scientific papers

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.

Synthesis and biological evaluation of azole-diphenylpyrimidine derivatives (AzDPPYs) as potent T790M mutant form of epidermal growth factor receptor inhibitors

A series of novel azole-diphenylpyrimidine derivatives (AzDPPYs) were synthesized and biologically evaluated as potent EGFRT790Minhibitors. Among these analogues, the most active inhibitor 6e not only displayed high activity against EGFRT790M/L858Rkinase (IC50?=?3.3?nM), but also was able to repress the replication of H1975 cells harboring EGFRT790Mmutation at a concentration of 0.118?μmol/L. In contrast to the lead compound rociletinib, 6e slightly reduces the key EGFRT790M-minduced drug resistance. Significantly, inhibitor 6e demonstrates high selectivity (SI?=?299.3) for T790M-containing EGFR mutants over wild type EGFR, hinting that it will cause less side effects.

Anilino-monoindolylmaleimides as potent and selective JAK3 inhibitors

We designed a series of anilino-indoylmaleimides based on structural elements from literature JAK3 inhibitors 3 and 4, and our lead 5. These new compounds were tested as inhibitors of JAKs 1, 2 and 3 and TYK2 for therapeutic intervention in rheumatoid art

2-[1H-Benzimidazol-2(3H)-ylidene]-2-(pyrimidin-2-yl)acetamides and 2-[benzothiazol-2(3H)-ylidene]-2-(pyrimidin-2-yl)acetamides as kinase inhibitors

2-[1H-benzimidazol-2(3H)-ylidene]-2-(pyrimidin-2-yl)acetamides and 2-[benzothiazol-2(3H)-ylidene]-2-(pyrimidin-2-yl)acetamides and their salts are kinase inhibitors, useful in the treatment of cancer.

Fused pyrrolecarboxamides: GABA brain receptor ligands

Substituted pyrrolecarboxamide compounds are disclosed. These compounds are highly selective agonists, antagonists or inverse agonists for GABAA brain receptors or prodrugs of agonists, antagonists or inverse agonists for GABAA brain receptors and are therefore useful in the diagnosis and treatment of anxiety, depression, Alzheimer's dementia, sleep and seizure disorders, overdose with benzodiazepine drugs and for enhancement of memory. Pharmaceutical compositions, including packaged pharmaceutical compositions, are further provided. Compounds of the invention are also useful as probes for the localization of GABAA receptors in tissue samples.

DIAMINOTHIAZOLES

The present invention is directed to novel diaminothiazoles of formula These compounds inhibit cyclin-dependent kinase 4 (Cdk4) and are selective against Cdk2 and Cdk1. These compounds and their pharmaceutically acceptable salts and esters have antiproliferative activity and are useful in the treatment or control of cancer, in particular solid tumors. This invention is also directed to pharmaceutical compositions containing such compounds and to methods of treating or controlling cancer, most particularly the treatment 6r control of breast, lung and colon and prostate tumors.

BENZAZEPINE DERIVATIVE, PROCESS FOR PRODUCING THE SAME, AND USE

The present invention provides a novel benzazepine derivative represented by formula : wherein, R1 is a 5- or 6-membered aromatic ring, R2 is lower alkyl group, etc., Y is an optionally substituted imino group, ring A and ring B are independently an optionally substituted aromatic ring, W is formula -W1-X2-W2- (W1 and W2 are independently S(O)m1 (m1 is 0, 1 or 2), etc., and X2 is an optionally substituted alkylene groupetc. ), a preparation method and use thereof.

1-[(Aryloxy)alkyl]-1H-imidazoles as inhibitors of neuronal nitric oxide synthase

A series of 1-[(aryloxy)alkyl]-1 H-imidazoles were synthesized from imidazole and various (aryloxy)alkyl bromides and tested for inhibitory activity against the three isoforms of nitric oxide synthase. 1-[2-(4-Bromophenoxy)ethyl]-1 H-imidazole and 1-[2-[4-(trifluoromethyl)phenoxy]ethyl]-1H-imidazole showed inhibitory activity against the neuronal isoform but were less potent against the endothelial isoform. Thus they could be considered interesting for their selectivity. The remaining compounds had only modest activity.

N-(phenoxyalkyl)imidazoles as selective inhibitors of the thromboxane synthetase enzyme and pharmaceutical compositions thereof

N-(mono or disubstituted phenoxyalkyl)imidazoles and the pharmaceutically acceptable acid addition salts thereof are able to selectively inhibit the action of the thromboxane synthetase enzyme without significantly inhibiting the action of the prostacycline synthetase or cyclooxygenase enzymes and are thus useful in the treatment of ischaemic heart disease, stroke, transient ischaemic attack, thrombosis, migraine, and the vascular complications of diabetes.

Selective Thromboxane Synthetase Inhibitors. 1. 1--1H-imidazoles

1-(2-Phenoxyethyl)-1H-imidazole was found to be an inhibitor of thromboxane (TxA2) synthetase, but it also inhibited the adrenal cytochrome P-450 enzyme steroid 11β-hydroxylase.The preparation of a series of analogues is described, and activity against TxA2 synthetase, PGI2 synthetase, cyclooxygenase, and steroid 11β-hydroxylase is discussed.Potency against TxA2 synthetase was increased by introduction of a carboxyl group at a suitable distance from the imidazole ring.A distance of 8.1-8.8 Angstroem between N-1 of the imidazole and the carboxyl carbon was found to be optimal.Introduction of a carboxyl group also had the effect of reducing activity against steroid 11β-hydroxylase.The most potent and selective compound was found to be 4-benzoic acid (14).