Journal ArticleDOI
2,4-Diaminothieno(2,3-d)pyrimidines as antifolates and antimalarials. 2. Synthesis of 2,4-diaminopyrido(4',3':4,5)thieno(2,3-d)pyrimidines and 2,4-diamino-8H-thiopyrano(4',3':4,5)thieno(2,3-d)pyrimidines.
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This article is published in Journal of Medicinal Chemistry.The article was published on 1973-03-01. It has received 62 citations till now.read more
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2-aminothiophenes by the gewald reaction
TL;DR: In this paper, the authors present the most elegant and promising set of synthetic routes for the synthesis of 2-aminothiophenes by the Gewald reaction applications of this facile methodology to pharmaceuticals and dyestuffs have been demonstrated
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Activation of NFκB is inhibited by curcumin and related enones
Waylon M. Weber,Lucy A. Hunsaker,C. Nathaniel Roybal,Ekaterina V. Bobrovnikova-Marjon,Steve F. Abcouwer,Robert E. Royer,Lorraine M. Deck,David L. Vander Jagt +7 more
TL;DR: The data suggest that the abilities of curcumin and analogues to prevent the stress-induced activation of NFkappaB result from the inhibition of specific targets rather than from activity as anti-oxidants.
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Thienopyridines: synthesis, properties, and biological activity
TL;DR: The current state and prospects of development of the chemistry of isomeric thienopyridines (synthesis, chemical transformations, and biological activities) are analyzed in this paper.
Journal ArticleDOI
2,4-Diaminothieno[2,3-d]pyrimidine analogues of trimetrexate and piritrexim as potential inhibitors of Pneumocystis carinii and Toxoplasma gondii dihydrofolate reductase.
Andre Rosowsky,Clara E. Mota,Joel E. Wright,James H. Freisheim,James J. Heusner,John J. McCormack,Sherry F. Queener +6 more
TL;DR: A series of eight previously undescribed 2,4-diaminothieno[2,3-d]pyrimidine analogues of the potent dihydrofolate reductase (DHFR) inhibitors trimetrexate and piritrexim were synthesized as potential drugs against Pneumocystis carinii and Toxoplasma gondii, which are major causes of severe opportunistic infections in AIDS patients.
Journal ArticleDOI
Novel inhibitors of InhA efficiently kill Mycobacterium tuberculosis under aerobic and anaerobic conditions
Catherine Vilchèze,Anthony D. Baughn,Jo Ann A. Tufariello,Lawrence W. Leung,Mack Kuo,Christopher F. Basler,David Alland,James C. Sacchettini,Joel S. Freundlich,William R. Jacobs +9 more
TL;DR: This study provides the TB drug development community with two chemical scaffolds that are suitable for structure-activity relationship study to improve on their cytotoxicities and bactericidal activities in vitro and in vivo.