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Overview of Recent Strategic Advances in Medicinal Chemistry.
TLDR
This Perspective aims to present a "big-picture" overview of recent strategic innovations in medicinal chemistry and drug discovery.
Identification of Dihydrofuro[3,4- d]pyrimidine Derivatives as Novel HIV-1 Non-Nucleoside Reverse Transcriptase Inhibitors with Promising Antiviral Activities and Desirable Physicochemical Properties.
TLDR
The dihydrofuro[3,4- d]pyrimidine derivatives 13c2 and 13c4 proved to be exceptionally potent against a wide range of HIV-1 strains carrying single NNRTI-resistant mutations and showed favorable pharmacokinetic properties, which suggested that 13 c2 is worth further investigation as a novel NN RTI to circumvent drug resistance.
Current insights into anti-HIV drug discovery and development: a review of recent patent literature (2014–2017)
TLDR
Current medicinal chemistry strategies are inadequate, and appropriate and new methodologies and technologies should be exploited to identify novel anti-HIV drug candidates in a time- and cost- effective manner.
Discovery of Thiophene[3,2-d]pyrimidine Derivatives as Potent HIV-1 NNRTIs Targeting the Tolerant Region I of NNIBP.
TLDR
A series of thiophenepyrimidine derivatives with various substituents in the right wing region of the structure are designed and synthesized with the aim of developing new interactions with the tolerant region I of the binding pocket of the HIV-1 non-nucleoside reverse transcriptase (NNRTI).
Discovery of novel 1,4-disubstituted 1,2,3-triazole phenylalanine derivatives as HIV-1 capsid inhibitors
TLDR
The design, synthesis and biological evaluation of a series of novel phenylalanine derivatives as HIV-1 CA protein inhibitors using the Cu(i)-catalyzed azide and alkyne 1,3-dipolar cycloaddition (CuAAC) reaction are reported.
Recent applications of click chemistry in drug discovery
TLDR
To explore new chemical spaces for drug-like molecules containing a high degree of structural diversity, it may be useful to merge the diversity-oriented synthesis and ‘privileged’ substructure-based strategy with bioorthogonal reactions using sophisticated automation and flow systems to improve productivity.
Design, synthesis and biological evaluation of tacrine-1,2,3-triazole derivatives as potent cholinesterase inhibitors.
TLDR
The design and synthesis of a series of 11 novel tacrine-1,2,3-triazole derivatives via a Cu(i)-catalyzed alkyne-azide 1, 3-dipolar cycloaddition (CuAAC) reaction are reported, which were evaluated for their inhibition activity against Electrophorus electricus acetylcholinesterase and horse serum butyrylcholinease as potential drug targets for Alzheimer's disease.
Structure-Based Optimization of Thiophene[3,2-d]pyrimidine Derivatives as Potent HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors with Improved Potency against Resistance-Associated Variants.
TLDR
The results indicate that 25a is a promising new drug candidate for treatment of HIV-1 infection, and was exceptionally potent against the whole viral panel.
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