Heterocyclic Compounds, 2-Ring 22 articles
- Bicyclo Compounds, Heterocyclic
CNS effects of a series of 1,2,4-triazolyl heterocarboxylic derivatives.
A series of 1,2,4-triazolyl heterocarboxylic derivatives were tested for acute toxicity and CNS effects in mice. Several of these compounds demonstrated clear psychostimulant effects. Other components of the series, however, showed a definite central depressant activity. Some of the screened derivat...
Cinnoline derivatives as chemotherapeutic agents for Trypanosoma congolense infections.
Synthesis and structure-activity relationships of phenylenebis(methylene)-linked bis-azamacrocycles that inhibit HIV-1 and HIV-2 replication...
We synthesized a series of analogues in which the ring size of the bis-pyridyl macrocycles was varied between 12 and 16 members per ring including the py[iso-14]aneN(4) ring system, an isomer of the pyaneN(4) macrocycle. The p-phenylenebis(methylene)-linked dimer of the py[iso-14]aneN(4) (AMD332...
Enantioselective oxidative biaryl coupling reactions catalyzed by 1,5-diazadecalin metal complexes.
A versatile synthesis of diverse 3,4-fused cinnolines via the base-catalysed condensation of 2-amino-2'-nitrobiaryls.
Benzo[c]cinnolines, thieno[3,2-c]cinnolines, pyrido[3,2-c]cinnolines and the previously undescribed quinoxalino[6,7-c]cinnoline ring system are conveniently prepared by a short synthetic route comprised of Suzuki coupling, base-catalysed cyclisation and deoxygenation. The use of tandem borylation-Su...
Total synthesis of the marine alkaloids (-)-lepadins a, b, and c based on stereocontrolled intramolecular acylnitroso-Diels-Alder reaction.
The first syntheses of (-)-lepadins A and C, as well as a new synthesis of (-)-lepadin B, have been achieved from commercially available (S)-malic acid. The methodology is based on an intramolecular hetero-Diels--Alder reaction of the acylnitroso compound, affording the bicyclic oxazino lactam with...
Inhibition of heterocyclic amine formation in beef patties by ethanolic extracts of rosemary.
Heterocyclic amines (HCAs) are mutagenic compounds formed during cooking muscle foods at high temperature. Inhibition of HCAs by rosemary extracts were evaluated with beef patties cooked at 191 degrees C (375 degrees F) for 6 min each side and 204 degrees C (400 degrees F) for 5 min...
Triazabicyclodecene: an effective isotope exchange catalyst in CDCl(3).
We describe the first effective H/D exchange reaction with acidic substrates in CDCl(3) at room temperature. The particularly mild reaction conditions involved (solvent, base, and temperature) allow the chemoselective deuteration of ketones over esters. An NMR study was conducted with the aim of rat...
Total syntheses of conformationally locked difluorinated pentopyranose analogues and a pentopyranosyl phosphate mimetic.
Trifluoroethanol has been elaborated, via a telescoped sequence involving a metalated difluoroenol, a difluoroallylic alcohol, [2,3]-Wittig rearrangement, and ultimately an RCM reaction and requiring minimal intermediate purification, to a number of cyclooctenone intermediates. Epoxidation of these...
Cytotoxic terpenoids from the Formosan soft coral Nephthea brassica.
Two new cytotoxic cembranoid diterpenes, brassicolide (1) and brassicolide acetate (2); a new cytotoxic sesquiterpene, (-)-4alpha-O-acetyl-selin-11-en (3); and six cytotoxic terpenoids, (-)-selin-11-en-4alpha-ol (4), 2-hydroxynephthenol (5), nephthenol (6), cembrene A (7), epoxycembrene A (8), and (...