The complete transformation of a racemate into one single enantiomer is defined as a deracemization. In amino acid chemistry, chemo-enzymatic deracemization is possible due to the ease of racemization of α-amino acids and the numerous enantioselective enzymatic systems operating on this class o...
A series of structurally novel aryl ureas was derived from optimization of the HTS lead as selective histamine H3 receptor (H3R) antagonists. The SAR was explored and the data obtained set up the starting point and foundation for further optimization. The most potent tool compounds, as exemplifi...
A series of N-10 urea derivatives of phenothiazine was synthesized and each compound was evaluated for its ability to inhibit human cholinesterases. Most were specific inhibitors of BuChE. However, the potent inhibitory effects on both cholinesterases of one sub-class, the cationic aminoureas, p...
Human APOBEC3G (apolipoprotein B mRNA-editing enzyme, catalytic polypeptide-like 3G, A3G) is a potent restriction factor against human immunodeficiency virus type 1 (HIV-1) by inducing hypermutation of G to A in viral genome after its incorporation into virions. HIV-1 Vif (Virion Infectivity Fac...
A new oxazole scaffold showing great promise in HIV-1 inhibition has been discovered by cell-based screening of an in-house library and scaffold modification. Follow-up SAR study focusing on the 5-aryl substituent of the oxazole core has identified 4k (EC50 = 0.42 μM, TI = 50) as a potent inhib...
A series of N-mustard–quinoline conjugates bearing a urea or hydrazinecarboxamide linker was synthesized for antitumor evaluation. The in vitro cytotoxicity studies revealed that compounds with hydrazinecarboxamide linkers were generally more cytotoxic than the corresponding urea counterparts i...
The oral activity and antithrombotic efficacy of BMY 42393 was examined in ex vivo platelet aggregation studies and arterial thrombosis animal models. In a heterologous ex vivo platelet aggregation assay, ADP-induced human platelet aggregation was inhibited when washed human platelets were combi...
BMY 42393, (2-[3-[2-(4,5-diphenyl-2-oxazolyl)ethyl]phenoxy]acetic acid), is a new prostacyclin partial agonist that inhibited ADP, collagen and thrombin-induced platelet aggregation (IC50 range 0.3 - 2.0 μM). BMY 42393 stimulated platelet adenylate cyclase activity (EC50 = 25 μM), however, the...
[3-(4-(4,5-diphenyl-2-oxazolyl)-5-oxazolyl]phenoxy]acetic acid (BMY 45778) inhibits human (IC50 = 35 nM), rabbit (136 nM) and rat (1.3 μm) platelet aggregation. This compound activates adenylyl cyclase (ED50= 6−10 nM) and stimulates GTPase in human platelet membrane preparations. The potency (E...
The distribution of ditazole in blood and tissues of rats was determined by a simple GLC technique. Ditazole, after intravenous injection in rats (20 mg/kg), entered preferentially into the brain, the liver, and the heart in decreasing order. In the epididymal adipose tissue, the drug was presen...
Ditazole (4,5-diphenyl-2-bis-(2-hydroxyethyl)-aminoxazol) is a weak anti-inflammatory drug and has been shown to inhibit thrombus formation following electrically stimulated vascular damage in the microcirculation of the hamster cheek pouch. The drug was found to inhibit thromboxane A2 (TXA2) pr...
This chapter covers fundamental aspects of solid acid and base catalysis and applications of solid acid and solid base catalysts in 18 acid- or base-catalyzed reactions. The fundamental aspects include advantage of heterogeneous acid and base catalysis over homogeneous ones in industrial process...
The Brønsted acid-catalyzed Diels-Alder reaction was examined. Phosphoric acids were effective Brønsted acids for the Diels-Alder reaction of cyclohexadienones and activated by the internal hydrogen-bonding of the adjacent hydroxy group.
A new series of donor-acceptor (P1-P3) conjugated polymers containing carbazole and quinoxaline units have been synthesized through multistep reactions. In the final step, the polymerization was carried out using Wittig reaction. The optical and potential charge –transporting properties of the ...
A series of new quinoxaline-containing compounds, namely, 2,3,6,7-tetrakis(3-(pyridin-3-yl)phenyl)quinoxaline (Tm3PyQ), 2,3,6,7-tetrakis(3-(pyridin-4-yl)phenyl)quinoxaline (Tm4PyQ), 1,4-bis(2,3-dimethyl-7-(pyridin-3-yl)quinoxalin-6-yl)benzene (3PyDQB), and 1,4-bis(2,3-dimethyl-7-(pyridin-4-yl)qu...
A series of 6-substituted-1,3-diphenyl-1H-pyrazolo[3,4-b]quinoxalines were prepared using a new synthetic pathway: reductive cyclization of appropriate 5-(o-nitrophenyl)-pyrazoles with ferrous oxalate or triphenylphosphine. The main advantage of this procedure is that, contrary to the older prot...
Two electrochromic copolymers, P1 and P2, were synthesized from Stille coupling reactions of dibrominated phenazine having branched and linear alkyl side-chains, respectively, with distannyl thiophene. The prepared donor–acceptor type electrochromic polymers showed good solution processability,...
Macrocyclic cоmpounds are some of the most interesting objects in modern synthetic chemistry and, as shown in this critical review, they provide an attractive entry into quinoxaline derivatives, which are very important heterocycles from many points of view including medicinal and pharmaceutica...
Vicinal tricarbonyl intermediates are directly synthesized from β-dicarbonyls with the aid of Cu(II) salts and air, and they are further condensed with phenylene diamine to produce a range of quinoxalines in moderate to good yields in one-pot reaction.
Quinoxaline derivatives are an important class of heterocycle compounds, where N replaces some carbon atoms in the ring of naphthalene. Its molecular formula is C8H6N2, formed by the fusion of two aromatic rings, benzene and pyrazine. It is rare in natural state, but their synthesis is easy to p...
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