Studies of non-nucleoside HIV-1 reverse transcriptase inhibitors. Part 2: synthesis and structure-activity relationships of 2-cyano and 2-hydroxy thiazolidenebenzenesulfonamide derivatives.

@article{Masuda2005StudiesON,
  title={Studies of non-nucleoside HIV-1 reverse transcriptase inhibitors. Part 2: synthesis and structure-activity relationships of 2-cyano and 2-hydroxy thiazolidenebenzenesulfonamide derivatives.},
  author={Naoyuki Masuda and Osamu Yamamoto and Masahiro Fujii and Tetsuro Ohgami and Jiro Fujiyasu and Toru Kontani and Ayako Moritomo and Masaya Orita and Hiroyuki Kurihara and Hironobu Koga and Shunji Kageyama and Mitsuaki Ohta and Hiroshi Inoue and T Hatta and Masafumi Shintani and Hiroshi Suzuki and Kenji Sudo and Yasuaki Shimizu and Eiichi N Kodama and Masao Matsuoka and Masatoshi Fujiwara and Tomoyuki Yokota and Shiro Shigeta and Masanori Baba},
  journal={Bioorganic \& medicinal chemistry},
  year={2005},
  volume={13 4},
  pages={
          949-61
        }
}
Binding Modes of Two Novel Non-Nucleoside Reverse Transcriptase Inhibitors, YM-215389 and YM-228855, to HIV Type-1 Reverse Transcriptase
TLDR
Structural information is provided for optimizing the TBS derivatives in an attempt to construct ideal NNRTIs that maintain anti-HIV-1 activity to various HIV-1 variants.
Virtual screening, identification, and biochemical characterization of novel inhibitors of the reverse transcriptase of human immunodeficiency virus type-1.
TLDR
A large chemical library of compounds was screened against two crystal structures of HIV-1 RT to identify novel inhibitors and a combination of substituents from two structurally related inhibitors in a single molecule improved the inhibition efficacy.
Identification of a Novel Sulfonamide Non-Nucleoside Reverse Transcriptase Inhibitor by a Phenotypic HIV-1 Full Replication Assay
TLDR
The development of a cell-based assay that uses a phenotypic drug discovery approach based on automated high-content screening is described, and one sulfonamide compound showed strong anti-HIV activity against wild-type and clinically relevant multidrug resistant HIV strains.
Oxazole-Benzenesulfonamide Derivatives Inhibit HIV-1 Reverse Transcriptase Interaction with Cellular eEF1A and Reduce Viral Replication
TLDR
A sensitive, live-cell split-luciferase complementation assay (NanoBiT) is developed to quantitatively measure inhibition of HIV-1 RT interaction with eEF1A, and a novel mechanism of action involving inhibition of the HIV- 1 RT-e EF1A interaction is suggested and a potential new way to combat drug-resistant HIV-2 strains in infected people.
HIV‐1 NNRTIs: structural diversity, pharmacophore similarity, and impliations for drug design
TLDR
This review covers two decades of research and development for various NN RTI families based on their chemical scaffolds, and describes the structural similarity of NNRTIs.
Novel, One-Pot, Three-Component, Regioselective Synthesis of Fluorine-Containing Thiazole and Bis-3H-thiazole Derivatives Using Polyvinyl Pyridine as Heterogeneous Catalyst, and Evaluation of Their Antibacterial Activity
Abstract A convenient, one-pot, three-component regioselective synthesis of novel 2,2′-(1,4-phenylene)-bis-(3-aryl-2-substituted imino-4-aryl-3H-thiazole) derivatives from 1,4-phenylene
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