Novel Thiazolidinone Derivatives with an Uncommon Mechanism of Inhibition Towards HIV-1 Reverse Transcriptase

被引：21

作者：

Pitta, Eleni ^{[2
]}

Crespan, Emmanuele ^{[1
]}

Geronikaki, Athina ^{[2
]}

Maga, Giovanni ^{[1
]}

Samuele, Alberta ^{[1
]}

机构：

[1] CNR, IGM, I-27100 Pavia, Italy

[2] Aristotle Univ Thessaloniki, Sch Pharm, Thessaloniki 54124, Greece

来源：

LETTERS IN DRUG DESIGN & DISCOVERY | 2010年 / 7卷 / 04期

关键词：

HIV-1; RT; HAART; NNRTIs; AIDS; Antiretroviral therapy; Enzyme kinetics; DRUG-RESISTANCE; AGENTS; DESIGN; INFECTION; NNRTIS;

D O I：

10.2174/157018010790945869

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Here, we show that novel 2-aryl-3-(4-adamantyl-thiazol-21,3-thiazolidin-4-one derivatives have a mixed- or fully competitive mechanism of inhibition towards HIV-1 Reverse Transcriptase with respect to the substrates of the reaction. Thus, they are interesting starting points for the development of novel NNRTIs with an uncommon mechanism of action.

引用

页码：228 / 234

页数：7

共 50 条

[21] HIV-1 reverse transcriptase inhibitors
Lloyd, AW
DRUG DISCOVERY TODAY, 1996, 1 (03) : 122 - 122
[22] Discovery of Phenylaminopyridine Derivatives as Novel HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors
Kim, Junwon
Lee, Doohyun
Park, Changmin
So, Wonyoung
Jo, Mina
Ok, Taedong
Kwon, Jeongjin
Kong, Sunju
Jo, Suyeon
Kim, Youngmi
Choi, Jihyun
Kim, Hyoung Cheul
Ko, Yoonae
Choi, Inhee
Park, Youngsam
Yoon, Jaewan
Ju, Moon Kyeong
Kim, Junghwan
Han, Sung-Jun
Kim, Tae-Hee
Cechetto, Jonathan
Nam, Jiyoun
Sommer, Peter
Liuzzi, Michel
Lee, Jinhwa
No, Zaesung
ACS MEDICINAL CHEMISTRY LETTERS, 2012, 3 (08): : 678 - 682
[23] MOLECULAR DOCKING STUDIES OF A FEW NOVEL PYRIMIDINE DERIVATIVES AS REVERSE TRANSCRIPTASE HIV-1 INHIBITORS
Halmare, R. S.
Ganatra, S. H.
INTERNATIONAL JOURNAL OF PHARMACEUTICAL SCIENCES AND RESEARCH, 2019, 10 (09): : 4201 - 4206
[24] HIV-1 reverse transcriptase inhibitors
Yazan El Safadi
Valérie Vivet-Boudou
Roland Marquet
Applied Microbiology and Biotechnology, 2007, 75 : 723 - 737
[25] Structural modification of diarylpyrimidine derivatives as HIV-1 reverse transcriptase inhibitors
Shuang-Xi Gu
Yuan-Yuan Zhu
Fen-Er Chen
Erik De Clercq
Jan Balzarini
Christophe Pannecouque
Medicinal Chemistry Research, 2015, 24 : 220 - 225
[26] Structural modification of diarylpyrimidine derivatives as HIV-1 reverse transcriptase inhibitors
Gu, Shuang-Xi
Zhu, Yuan-Yuan
Chen, Fen-Er
De Clercq, Erik
Balzarini, Jan
Pannecouque, Christophe
MEDICINAL CHEMISTRY RESEARCH, 2015, 24 (01) : 220 - 225
[27] Fullerene derivatives as dual inhibitors of HIV-1 reverse transcriptase and protease
Yasuno, Takumi
Ohe, Tomoyuki
Kataoka, Hiroki
Hashimoto, Kosho
Ishikawa, Yumiko
Furukawa, Keigo
Tateishi, Yasuhiro
Kobayashi, Toi
Takahashi, Kyoko
Nakamura, Shigeo
Mashino, Tadahiko
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2021, 31
[28] Crystal structures of HIV-1 reverse transcriptase in complex with carboxanilide derivatives
Ren, JS
Esnouf, RM
Hopkins, AL
Warren, J
Balzarini, J
Stuart, DI
Stammers, DK
BIOCHEMISTRY, 1998, 37 (41) : 14394 - 14403
[29] Derivatives of Mesoxalic Acid Block Translocation of HIV-1 Reverse Transcriptase
Bernatchez, Jean A.
Paul, Rakesh
Tchesnokov, Egor P.
Ngure, Marianne
Beilhartz, Greg L.
Berghuis, Albert M.
Lavoie, Rico
Li, Lianhai
Auger, Anick
Melnyk, Roman A.
Grobler, Jay A.
Miller, Michael D.
Hazuda, Daria J.
Hecht, Sidney M.
Goette, Matthias
JOURNAL OF BIOLOGICAL CHEMISTRY, 2015, 290 (03) : 1474 - 1484
[30] QSAR study for HEPT derivatives, inhibitors of HIV-1 reverse transcriptase
Mracec, M
Ivan, D
Mracec, M
REVUE ROUMAINE DE CHIMIE, 2004, 49 (05) : 431 - 435

← 1 2 3 4 5 →