A One-Step Ring Transformation/Ring Annulation Approach to Pyrrolo[2,3-d]pyrimidines. A New Synthesis of the Potent Dihydrofolate Reductase Inhibitor TNP-351

1995 ◽  
Vol 60 (21) ◽  
pp. 6684-6687 ◽  
Author(s):  
Edward C. Taylor ◽  
Hemantkumar H. Patel ◽  
Jong-Gab Jun
Keyword(s):  
Dihydrofolate Reductase ◽  
Reductase Inhibitor ◽  
Ring Transformation ◽  
New Synthesis ◽  
One Step

scholarly journals High-throughput Screening and Sensitized Bacteria Identify an M. tuberculosis Dihydrofolate Reductase Inhibitor with Whole Cell Activity

PLoS ONE ◽  
2012 ◽  
Vol 7 (6) ◽  
pp. e39961 ◽  
Author(s):  
Anuradha Kumar ◽  
Meng Zhang ◽  
Linyun Zhu ◽  
Reiling P. Liao ◽  
Charles Mutai ◽  
...  
Keyword(s):  
High Throughput ◽  
Dihydrofolate Reductase ◽  
High Throughput Screening ◽  
Reductase Inhibitor ◽  
Cell Activity ◽  
Whole Cell

Antiherpesvirus Activity of the Combination of 5-iodo-2′-deoxycytidine with methotrexate: An in vitro and in vivo Study

1994 ◽  
Vol 5 (5) ◽  
pp. 283-289
Author(s):  
C. Cremonesi ◽  
C. Scarpini ◽  
R. Bianchi ◽  
A. Radaelli ◽  
M. Gimelli ◽  
...  
Keyword(s):  
Antiviral Activity ◽  
Dihydrofolate Reductase ◽  
Reductase Inhibitor ◽  
Cellular Viability ◽  
Cutaneous Lesions ◽  
Guinea Pig Model ◽  
Simplex Virus ◽  
Hsv 1

We evaluated the in vitro and in vivo antiviral activity of the deoxyribonucleoside analogue 5-iodo-2′-deoxycytidine (IDC) combined with the dihydrofolate reductase inhibitor methotrexate (MTX) on herpes simplex virus types 1 and 2 (HSV-1, HSV-2). The IDC-MTX combination synergistically inhibited HSV-1 and HSV-2 replication in vitro at concentrations that did not reduce cellular viability and was very effective in reducing the severity of cutaneous lesions in the experimental guinea pig model in vivo. The antiviral activity of the IDC-MTX combination in guinea pigs was also compared with that of acyclovir and was demonstrated to be higher.

Thermodynamic study of dihydrofolate reductase inhibitor selectivity

1994 ◽  
Vol 1207 (1) ◽  
pp. 74-79 ◽  
Author(s):  
Sophie P. Sasso ◽  
Robert M. Gilli ◽  
Jean Claude Sari ◽  
Odile S. Rimet ◽  
Claudette M. Briand
Keyword(s):  
Dihydrofolate Reductase ◽  
Reductase Inhibitor ◽  
Thermodynamic Study ◽  
Inhibitor Selectivity

Reactions of Ketene Acetals. IV. A New Synthesis of α-Pyrones. III

1975 ◽  
Vol 53 (2) ◽  
pp. 201-208 ◽  
Author(s):  
Alain Bélanger ◽  
Paul Brassard
Keyword(s):  
New Synthesis ◽  
One Step ◽  
Ketene Acetals ◽  
Mechanism Of The Reaction

A simple one-step synthesis of α-pyrones and 3-chloro-α-pyrones from β-functionalized α, β-enones and ketene acetals has been devised. The method has also been adapted to the preparation of some 4-methoxy-α-pyrones. Finally the mechanism of the reaction has been investigated.

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