Role of 1, 4-benzothiazine derivatives in medicinal chemistry.

R Fringuelli, L Milanese, F Schiaffella - Mini Reviews in Medicinal …, 2005 - europepmc.org
1, 4-Benzothiazine (1, 4-BT) derivatives have been reported to exhibit a wide range of
pharmacological properties including antifungal, immunostimulating, anti-aldoso-reductase, anti-…

1, 4-Benzothiazine and 1, 4-benzoxazine imidazole derivatives with antifungal activity: a docking study

…, A Vecchiarelli, F Schiaffella, R Fringuelli - Bioorganic & medicinal …, 2002 - Elsevier
… free hydroxyl group, favor the binding of the R isomer over the S. Since both isomers adopt
… binding energy of the R isomer is likely due to a better conformational strain energy of (R)-3 (…

Quinolonecarboxylic acids. 2. Synthesis and antibacterial evaluation of 7-oxo-2, 3 dihydro-7H-pyrido [1, 2, 3-de][1, 4] benzothiazine-6-carboxylic acids

V Cecchetti, A Fravolini, R Fringuelli… - Journal of medicinal …, 1987 - ACS Publications
A series of pyridobenzothiazine acid derivatives was synthesized and their in vitro
antibacterial activity was evaluated. The 1, 4-benzothiazine intermediates, which by Gould-Jacobs …

Antifungal and immunomodulating activities of 1, 4-benzothiazine azole derivatives

R Fringuelli, F Schiaffella… - Journal of Chemotherapy …, 2001 - europepmc.org
We reviewed the studies on the in vitro and in vivo antifungal activity of 1, 4-benzothiazine
azole derivatives (1, 4-BT). A number of different 1, 4-BT have been tested for anti-Candida …

Anti-Candida albicans properties of novel benzoxazine analogues

R Fringuelli, D Pietrella, F Schiaffella, A Guarraci… - Bioorganic & medicinal …, 2002 - Elsevier
We previously reported that azole 1,4-benzothiazine derivatives have appreciable anti-Candida
activity. In this study, we synthesized 1,4-benzoxazine analogues and examined their …

Design, Synthesis, and Microbiological Evaluation of New Candida albicans CYP51 Inhibitors

…, G Costantino, D Pietrella, R Fringuelli - Journal of medicinal …, 2005 - ACS Publications
… , being shifted from 1-S to 1-R. This behavior is explained by the accommodation of the alkyl/…
BT and BO rings to adopt a slightly different pose that is best fitted by the 1-R stereoisomers. …

Azole derivatives of 1, 4-benzothiazine as antifungal agents

R Fringuelli, F Schiaffella, F Bistoni, L Pitzurra… - Bioorganic & medicinal …, 1998 - Elsevier
A series of azole derivatives of 1,4-benzothiazine 7–14 was synthesized and evaluated for
the in vitro and in vivo activity against Candida albicans. Secondary alcohol 10 and its ether …

Bulky 1, 4-benzoxazine derivatives with antifungal activity

R Fringuelli, N Giacchè, L Milanese, E Cenci… - Bioorganic & medicinal …, 2009 - Elsevier
… As far as it concerns compound 13, docking experiments reveal that the S isomer fits
better the enzymatic site along channel 2 then the R isomer. The adopted binding pose of …

Novel ketoconazole analogues based on the replacement of 2, 4-dichlorophenyl group with 1, 4-benzothiazine moiety: Design, synthesis, and microbiological …

…, L Milanese, A Vecchiarelli, R Fringuelli - Bioorganic & medicinal …, 2006 - Elsevier
As a part of a program to develop novel antifungal agents, new compounds which incorporate
the 1,4-benzothiazine moiety into the structure of ketoconazole (KTZ) were prepared. …

β-Keto esters from the rhodium (II) acetate catalysed conversion of α-diazo-β-hydroxy esters

R Pellicciari, R Fringuelli, P Ceccherelli… - Journal of the Chemical …, 1979 - pubs.rsc.org
A new and efficient procedure for the transformation of α-diazo-β-hydroxy esters into the
corresponding β-keto esters, which involves the use of Rh2 (OAc) 4, is described.