Dihydro(alkylthio)(naphthylmethyl)oxopyrimidines:  Novel Non-Nucleoside Reverse Transcriptase Inhibitors of the S-DABO Series

A Mai, M Artico, G Sbardella, S Quartarone… - Journal of Medicinal …, 1997 - ACS Publications
Novel compounds related to 2-(cyclohexylthio)-3, 4-dihydro-5-methyl-6-(3-methylbenzyl)-4-
oxopyrimidine (3c, MC 639) have been synthesized and tested as inhibitors of human …

Design strategies of novel NNRTIs to overcome drug resistance

P Zhan, X Liu, Z Li, C Pannecouque… - Current medicinal …, 2009 - ingentaconnect.com
Nonnucleoside reverse transcriptase inhibitors (NNRTIs) are very potent and most
promising anti-AIDS drugs that specifically inhibit HIV-1 reverse transcriptase (RT) …

S-1153 inhibits replication of known drug-resistant strains of human immunodeficiency virus type 1

T Fujiwara, A Sato, M El-Farrash, S Miki… - Antimicrobial agents …, 1998 - Am Soc Microbiol
ABSTRACT S-1153 is a new imidazole compound that inhibits human immunodeficiency
virus (HIV) type 1 (HIV-1) replication by acting as a nonnucleoside reverse transcriptase …

Non-nucleoside HIV-1 reverse transcriptase (RT) inhibitors: past, present, and future perspectives

G Campiani, A Ramunno, G Maga… - Current …, 2002 - ingentaconnect.com
Along with nucleoside reverse transcriptase inhibitors (NRTIs) and protease inhibitors (PIs),
nonnucleoside reverse transcriptase inhibitors (NNRTIs) have gained a definitive and …

Doravirine and islatravir have complementary resistance profiles and create a combination with a high barrier to resistance

MT Lai, M Feng, M Xu, W Ngo… - Antimicrobial Agents …, 2022 - Am Soc Microbiol
ABSTRACT Doravirine (DOR), a non-nucleoside reverse transcriptase inhibitor (NNRTI),
was approved for treatment of HIV-1 infection in 2018. In the pivotal phase 3 trials, DRIVE …

Structure-based design, synthesis, and biological evaluation of conformationally restricted novel 2-alkylthio-6-[1-(2, 6-difluorophenyl) alkyl]-3, 4-dihydro-5 …

A Mai, G Sbardella, M Artico, R Ragno… - Journal of medicinal …, 2001 - ACS Publications
5-Alkyl-2-(alkylthio)-6-(2, 6-difluorobenzyl)-3, 4-dihydropyrimidin-4 (3 H)-ones (S-DABOs, 2)
have been recently described as a new class of human immunodeficiency virus type 1 (HIV …

Rationally designed dual inhibitors of HIV reverse transcriptase and integrase

Z Wang, EM Bennett, DJ Wilson… - Journal of medicinal …, 2007 - ACS Publications
Bifunctional inhibitors were designed and synthesized based on 1-[(2-hydroxyethoxy)
methyl]-6-(phenylthio) thymine (HEPT) a non-nucleoside reverse transcriptase (RT) …

Rational design and synthesis of phenethyl-5-bromopyridyl thiourea derivatives as potent non-nucleoside inhibitors of HIV reverse transcriptase

R Vig, C Mao, TK Venkatachalam… - Bioorganic & medicinal …, 1998 - Elsevier
A series of novel phenethylthiazolylthiourea (PETT) derivatives targeting the nonnucleoside
inhibitor (NNI) binding site of HIV reverse transcriptase (RT) have been designed based on …

Combining docking, molecular dynamics and the linear interaction energy method to predict binding modes and affinities for non-nucleoside inhibitors to HIV-1 …

J Carlsson, L Boukharta, J Åqvist - Journal of medicinal chemistry, 2008 - ACS Publications
Docking, scoring, molecular dynamics (MD), and the linear interaction energy (LIE) method
are used here to predict binding modes and affinities for a set of 43 non-nucleoside …

Cutting into the substrate dominance: pharmacophore and structure-based approaches toward inhibiting human immunodeficiency virus reverse transcriptase …

L Wang, SG Sarafianos, Z Wang - Accounts of chemical research, 2019 - ACS Publications
Conspectus Human immunodeficiency virus (HIV) reverse transcriptase (RT) contains two
distinct functional domains: a DNA polymerase (pol) domain and a ribonuclease H (RNase …