Synthesis and biological evaluation of nojirimycin- and pyrrolidine-based trehalase inhibitors

• Davide Bini,
• Francesca Cardona,
• Matilde Forcella,
• Camilla Parmeggiani,
• Paolo Parenti,
• Francesco Nicotra and
• Laura Cipolla

Beilstein J. Org. Chem. 2012, 8, 514–521, doi:10.3762/bjoc.8.58

• their preliminary biological evaluation as inhibitors against porcine and insect trehalase from C. riparius. Results and Discussion In previous studies by us and other research groups it was reported that 1-deoxynojirimycin (7) and its benzyl urea derivative 8 (Figure 2) [17][18] are trehalase

Synthesis of 2-amino-3-arylpropan-1-ols and 1-(2,3-diaminopropyl)-1,2,3-triazoles and evaluation of their antimalarial activity

• Matthias D’hooghe,
• Stéphanie Vandekerckhove,
• Karen Mollet,
• Karel Vervisch,
• Stijn Dekeukeleire,
• Liesbeth Lehoucq,
• Carmen Lategan,
• Peter J. Smith,
• Kelly Chibale and
• Norbert De Kimpe

Beilstein J. Org. Chem. 2011, 7, 1745–1752, doi:10.3762/bjoc.7.205

• parasite Plasmodium falciparum, too. Biological evaluation At first, compounds 6a–c, 8a–e, 9a–d, 12a,b, 14a–e, 15a–f and 16a–g were screened for in vitro antiplasmodial activity. All samples were tested in triplicate on one occasion against a chloroquine-sensitive (CQS) strain of P. falciparum (D10). Those

Efficient syntheses of 25,26-dihydrodictyostatin and 25,26-dihydro-6-epi-dictyostatin, two potent new microtubule-stabilizing agents

• María Jiménez,
• Wei Zhu,
• Andreas Vogt,
• Billy W. Day and
• Dennis P. Curran

Beilstein J. Org. Chem. 2011, 7, 1372–1378, doi:10.3762/bjoc.7.161

• ) (Figure 1). The later parts of this synthesis have been briefly communicated in a recent paper whose primary focus was biological evaluation [30]. Indeed, 3a and 3b prove to be promising anticancer agents with in vitro and cellular testing data superior to those of the 16-desmethyl analogs 2a and 2b, and

Synthesis of novel (1-alkanoyloxy- 4-alkanoylaminobutylidene)-1,1-bisphosphonic acid derivatives

• Petri A. Turhanen and
• Jouko J. Vepsäläinen

Beilstein J. Org. Chem. 2006, 2, No. 2, doi:10.1186/1860-5397-2-2

• proposed to be more lipophilic and are thus more soluble in organic solvents than alendronate and can be used as starting materials for the synthesis of new phosphorus end modified derivatives of HABBPA and which may represent as possible prodrugs of alendronate. Novel biological evaluation for selected

Total syntheses of oxygenated brazanquinones via regioselective homologous anionic Fries rearrangement of benzylic O-carbamates

• Glaucia Barbosa Candido Alves Slana,
• Mariângela Soares de Azevedo,
• Rosângela Sabattini Capella Lopes,
• Cláudio Cerqueira Lopes and
• Jari Nobrega Cardoso

Beilstein J. Org. Chem. 2006, 2, No. 1, doi:10.1186/1860-5397-2-1

• construction of these bioactive compounds for future biological evaluation. The emerging carbanionic aromatic chemistry (anionic ortho-Fries, [13] homologous anionic Fries, [14] remote anionic Fries rearrangements [15] and carbamoyl Baker-Venkataraman reaction [16]) originating from the Directed ortho

Synthesis and glycosidase inhibitory activity of new hexa- substituted C8-glycomimetics

• Olivia Andriuzzi,
• Christine Gravier-Pelletier,
• Gildas Bertho,
• Thierry Prangé and
• Yves Le Merrer

Beilstein J. Org. Chem. 2005, 1, No. 12, doi:10.1186/1860-5397-1-12

• . According to this strategy and to the nature of the ketones involved in the final reductive amination, various aminocyclitols could be synthesized. Thus, in this study two carbasugars and four aminocyclitols were obtained. Biological evaluation of these compounds towards 24 commercially available