Zobrazeno 1 - 10
of 35
pro vyhledávání: '"Trovirdine"'
Publikováno v:
Medicinal Chemistry. 3:513-519
A series of thioamides were designed as bio-isosteres to the non-nucleoside reverse transcriptase inhibitor trovirdine by replacement of the thiourea NH groups with methylene groups. Eight thioamides were synthesized and in vitro tested for inhibitor
Autor:
Anne-Marie Aubertin, E. Sugeac, Sylvie Schmidt, D. Laduree, Christine Fossey, Geraldine Laumond
Publikováno v:
Journal of Enzyme Inhibition and Medicinal Chemistry. 18:175-186
Expected for their ability to inhibit HIV replication, four heterodimers with a Nucleoside Reverse Transcriptase Inhibitor (NRTI) and a Non-Nucleoside Reverse Transcriptase Inhibitor (NNRTI) bound by a linker arm were designed and synthesized. For th
Autor:
A. Ciurea, D. Laduree, Anne-Marie Aubertin, E. Sugeac, Z. Delbederi, Christine Fossey, Sylvie Schmidt, Geraldine Laumond, D. Gavriliu
Publikováno v:
Nucleosides, Nucleotides and Nucleic Acids. 21:505-533
A series of eleven heterodimers containing both a nucleoside analogue (d4U, d4T) and a non-nucleoside type inhibitor (Trovirdine analogue) were synthesized and evaluated for their ability to inhibit HIV replication. Unfortunately, the (N-3)d4U-Trovir
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 10:2071-2074
Chiral derivatives of two cyclohexylethyl halopyridyl thiourea compounds (HI-509 and HI-510), two α-methyl benzyl halopyridyl compounds (HI-511 and HI-512), and a cyclohexyl ethyl thiazolyl thiourea compound (HI-513) were synthesized as nonnucleosid
Autor:
Iain Morrison, Marita Högberg
Publikováno v:
Expert Opinion on Therapeutic Patents. 10:1189-1199
Two classes of anti-HIV drugs are currently marketed which target the HIV-1 reverse transcriptase (RT). The first explored class was the nucleoside RT inhibitors (NRTIs), such as AZT, ddI, ddC, 3TC, D4T and abacavir, whereas the more recently launche
Autor:
Ole S. Pedersen, Erik B. Pedersen
Publikováno v:
Antiviral Chemistry and Chemotherapy. 10:285-314
Non-nucleoside reverse transcriptase inhibitors (NNRTIs) are promising drugs for the treatment of HIV when used in combination with other anti-HIV drugs such as nucleoside reverse transcriptase (RT) inhibitors and protease inhibitors. The first gener
Publikováno v:
Antiviral Chemistry and Chemotherapy. 10:233-240
A computer model of reverse transcriptase (RT) from human immunodeficiency virus type 1 (HIV-1) was used to design thiourea compounds that were predicted to inhibit RT. The RT model was used to approximate how changes in binding pocket shape, volume
Autor:
Erik De Clercq
Publikováno v:
Il Farmaco. 54:26-45
Non-nucleoside reverse transcriptase inhibitors (NNRTIs) have, in addition to the nucleoside reverse transcriptase inhibitors (NRTIs) and protease inhibitors (PIs), gained a definitive place in the treatment of HIV-1 infections. Starting from the HEP
Autor:
Rakesh Vig, Elise A. Sudbeck, Fatih M. Uckun, Taracad K. Venkatachalam, Lisa Tuel-Ahlgren, Chen Mao
Publikováno v:
Bioorganic & Medicinal Chemistry. 6:1789-1797
A series of novel phenethylthiazolylthiourea (PETT) derivatives targeting the nonnucleoside inhibitor (NNI) binding site of HIV reverse transcriptase (RT) have been designed based on the structure of the NNI binding pocket. The structure-based design
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 8:2213-2218
A novel computer model of the HIV reverse transcriptase (RT) non-nucleoside inhibitor (NNI) binding pocket, which was generated using high resolution crystal structure information from 9 individual RT/NNI complexes, revealed previously unrecognized l