Zobrazeno 1 - 10
of 28
pro vyhledávání: '"Takashi, Kawasuji"'
Autor:
Yoshiyuki, Taoda, Toshiyuki, Akiyama, Kenji, Tomita, Misato, Fujiwara-Kitamura, Yoshinori, Tamura, Takashi, Kawasuji, Eriko, Matsuoka, Erika, Akihisa, Takahiro, Seki, Tomokazu, Yoshinaga
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 64:128664
We have been conducting exploratory research to develop human immunodeficiency virus type-1 (HIV-1) integrase-LEDGF/p75 allosteric inhibitors (INLAIs). Here, we report on a newly designed compound with a tricyclic scaffold that shows promise as an in
Autor:
Felix DeAnda, Kendra E Hightower, Robert T Nolte, Kazunari Hattori, Tomokazu Yoshinaga, Takashi Kawasuji, Mark R Underwood
Publikováno v:
PLoS ONE, Vol 8, Iss 10, p e77448 (2013)
Signature HIV-1 integrase mutations associated with clinical raltegravir resistance involve 1 of 3 primary genetic pathways, Y143C/R, Q148H/K/R and N155H, the latter 2 of which confer cross-resistance to elvitegravir. In accord with clinical findings
Externí odkaz:
https://doaj.org/article/c236911bda2245a0833c118568cf3e4c
Autor:
Tamura Yoshinori, Kenji Tomita, Tomokazu Yoshinaga, Shuhei Arita, Shuichi Sugiyama, Takahiro Seki, Tsutomu Iwaki, Eriko Matsuoka, Takashi Kawasuji
Publikováno v:
Bioorganicmedicinal chemistry. 28(17)
We report herein the discovery of novel integrase-LEDGF/p75 allosteric inhibitors (INLAIs) based on a benzene scaffold 3. This scaffold can extend substituents from the C1 position unlike the common pyridine scaffolds 2. Structure-activity relationsh
Autor:
Takahiro Seki, Toshiyuki Akiyama, Yoshiyuki Taoda, Eriko Matsuoka, Tsutomu Iwaki, Takashi Kawasuji, Tomokazu Yoshinaga, Shuichi Sugiyama, Erika Akihisa
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 33:127742
We have discovered HIV-1 novel integrase-LEDGF/p75 allosteric inhibitors (INLAIs) based on a pyridine scaffold forming an intramolecular hydrogen bond. Scaffolds containing a pyridine moiety have been studied extensively and we have already reported
Autor:
Takashi Kawasuji, Brian A. Johns, Hiroshi Yoshida, Jason G. Weatherhead, Toshiyuki Akiyama, Teruhiko Taishi, Yoshiyuki Taoda, Minako Mikamiyama-Iwata, Hitoshi Murai, Ryuichi Kiyama, Masahiro Fuji, Norihiko Tanimoto, Tomokazu Yoshinaga, Takahiro Seki, Masanori Kobayashi, Akihiko Sato, Edward P. Garvey, Tamio Fujiwara
Publikováno v:
Journal of Medicinal Chemistry. 56:1124-1135
This work is a continuation of our initial discovery of a potent monocyclic carbamoyl pyridone human immunodeficiency virus type-1 (HIV-1) integrase inhibitor that displayed favorable antiviral and pharmacokinetic properties. We report herein a serie
Autor:
Brian A. Johns, Takashi Kawasuji, Jason G. Weatherhead, Eric E. Boros, James B. Thompson, Cecilia S. Koble, Edward P. Garvey, Scott A. Foster, Jerry L. Jeffrey, Tamio Fujiwara
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 23:422-425
Substituent effects of a series of N1 protio and methyl naphthyridinone HIV-1 integrase strand-transfer inhibitors has been explored. The effects of combinations of the N1 substituent and C3 amide groups was extensively studied to compare enzyme inhi
Autor:
Brian A. Johns, Takashi Kawasuji, Jason G. Weatherhead, Eric E. Boros, James B. Thompson, Edward P. Garvey, Scott A. Foster, Jerry L. Jeffrey, Wayne H. Miller, Noriyuki Kurose, Kenichi Matsumura, Tamio Fujiwara
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 21:6461-6464
A series of naphthyridinone HIV-1 integrase strand-transfer inhibitors have been designed based on a psdeudo-C2 symmetry element present in the two-metal chelation pharmacophore. A combination of two distinct inhibitor binding modes resulted in poten
Autor:
Tomokazu Yoshinaga, Ryuichi Kiyama, Takashi Kawasuji, Masahiro Fuji, Tamio Fujiwara, Akihiko Sato
Publikováno v:
Bioorganic & Medicinal Chemistry. 15:5487-5492
The two-metal binding model we previously reported as an inhibition mechanism of HIV integrase (HIV IN) produced a new direction in modification of 2-hydroxy-3-heteroaryl acrylic acid inhibitors (HHAAs). Here we present a novel series of HIV IN inhib
Autor:
Brian A. Johns, Takashi Kawasuji, Jason G. Weatherhead, Eric E. Boros, James B. Thompson, Cecilia S. Koble, Edward P. Garvey, Scott A. Foster, Jerry L. Jeffrey, Tamio Fujiwara
Publikováno v:
Bioorganicmedicinal chemistry letters. 24(14)
A series of N1 acetamide substituted naphthyridinone HIV-1 integrase inhibitors have been explored to understand structure-activity relationships (SAR) with various C3 amide groups. Investigations were evaluated using integrase enzyme inhibition, ant
Autor:
Brian A. Johns, Takashi Kawasuji, Jason G. Weatherhead, Teruhiko Taishi, David P. Temelkoff, Hiroshi Yoshida, Toshiyuki Akiyama, Yoshiyuki Taoda, Hitoshi Murai, Ryuichi Kiyama, Masahiro Fuji, Norihiko Tanimoto, Jerry Jeffrey, Scott A. Foster, Tomokazu Yoshinaga, Takahiro Seki, Masanori Kobayashi, Akihiko Sato, Matthew N. Johnson, Edward P. Garvey, Tamio Fujiwara
Publikováno v:
Journal of medicinal chemistry. 56(14)
We report herein the discovery of the human immunodeficiency virus type-1 (HIV-1) integrase inhibitors dolutegravir (S/GSK1349572) (3) and S/GSK1265744 (4). These drugs stem from a series of carbamoyl pyridone analogues designed using a two-metal che