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Showing 1 to 12 of 53 entries
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Intracellular pharmacokinetic study of zidovudine and its phosphorylated metabolites.

Acta pharmaceutica Sinica. B

Mu L, Zhou R, Tang F, Liu X, Li S, Xie F, Xie X, Peng J, Yu P.
PMID: 27006900
Acta Pharm Sin B. 2016 Mar;6(2):158-62. doi: 10.1016/j.apsb.2015.10.002. Epub 2015 Dec 21.

Zidovudine (AZT), the first drug approved by the US Food and Drug Administration for the treatment of human immunodeficiency virus (HIV) infection, is metabolized in the host cells to 5'-AZT triphosphate (AZT-TP) which inhibits HIV reverse transcriptase. As the...

Antimycobacterial and HIV-1 Reverse Transcriptase Activity of Julianaceae and Clusiaceae Plant Species from Mexico.

Evidence-based complementary and alternative medicine : eCAM

Gómez-Cansino R, Espitia-Pinzón CI, Campos-Lara MG, Guzmán-Gutiérrez SL, Segura-Salinas E, Echeverría-Valencia G, Torras-Claveria L, Cuevas-Figueroa XM, Reyes-Chilpa R.
PMID: 25983849
Evid Based Complement Alternat Med. 2015;2015:183036. doi: 10.1155/2015/183036. Epub 2015 Apr 23.

The extracts of 14 Julianaceae and 5 Clusiaceae species growing in Mexico were tested in vitro (50 µg/mL) against Mycobacterium tuberculosis H37Rv and HIV reverse transcriptase (HIV-RT). The Julianaceae bark and leaf extracts inhibited M. tuberculosis (>84.67%) and HIV-RT...

Total Synthesis of Quinoxapeptin A-C: Establishment of Absolute Stereochemistry.

Angewandte Chemie (International ed. in English)

Boger DL, Ledeboer MW, Kume M, Jin Q.
PMID: 10458810
Angew Chem Int Ed Engl. 1999 Aug;38(16):2424-2426. doi: 10.1002/(sici)1521-3773(19990816)38:16<2424::aid-anie2424>3.0.co;2-9.

The relative and absolute stereochemistry of the naturally occurring potent HIV reverse transcriptase (RT) inhibitors 1 and 2, quinoxapeptin A and B, were established by total synthesis. Their synthetic precursor 3 (dubbed quinoxapeptin C) was found to be a...

An Efficient Asymmetric Approach to Carbocyclic Nucleosides: Asymmetric Synthesis of 1592U89, a Potent Inhibitor of HIV Reverse Transcriptase.

The Journal of organic chemistry

Crimmins MT, King BW.
PMID: 11667311
J Org Chem. 1996 Jun 26;61(13):4192-4193. doi: 10.1021/jo960708p.

No abstract available.

HIV resistance to zidovudine: the role of pyrophosphorolysis.

Drug resistance updates : reviews and commentaries in antimicrobial and anticancer chemotherapy

Arion D, Parniak MA.
PMID: 11504476
Drug Resist Updat. 1999 Apr;2(2):91-95. doi: 10.1054/drup.1999.0076.

Zidovudine-resistant strains of HIV became apparent in many patients soon after advent of zidovudine (AZT) monotherapy. While this resistance could be unequivocally correlated with multiple mutations in HIV reverse transcriptase (D67N, K70R, T215F/Y, K219Q), the mechanism or phenotype for...

Use of Organosilicon Compounds towards the Rational Design of Antiparasitic and Antiviral Drugs.

Metal-based drugs

Déléris G.
PMID: 18472760
Met Based Drugs. 1995;2(3):143-51. doi: 10.1155/MBD.1995.143.

One of the major problems met for the conception of antiviral or antiparasitic drugs is to reach a high level of selectivity towards the pathogenic agent versus the host. We shall describe two synthetic approaches where main group organometallics...

In vitro studies of the toxicity of nucleoside analogues used in the treatment of HIV infection.

Toxicology in vitro : an international journal published in association with BIBRA

Flint OP.
PMID: 20692986
Toxicol In Vitro. 1994 Aug;8(4):677-83. doi: 10.1016/0887-2333(94)90042-6.

The nucleoside analogues, 3'-azido-3'-deoxythymidine (AZT, zidovudine), 2',3'-dideoxyinosine (ddI, didanosine) and 2',3'-dideoxycytidine (ddC, zalcitabine), used in the treatment of human immunodeficiency virus (HIV) infection, have been associated with a number of dose-limiting toxicities in clinical studies. These include myelotoxicity (AZT),...

Aryl Substituted Benzimidazolones as Potent HIV-1 Non-Nucleoside Reverse Transcriptase Inhibitors.

ACS medicinal chemistry letters

Pribut N, Basson AE, van Otterlo WAL, Liotta DC, Pelly SC.
PMID: 30783503
ACS Med Chem Lett. 2019 Jan 17;10(2):196-202. doi: 10.1021/acsmedchemlett.8b00549. eCollection 2019 Feb 14.

Since the discovery of HIV as the etiological agent of AIDS, the virus has infected millions of people each year. Fortunately, with the use of HAART, viremia can be suppressed to below detectable levels in the infected individuals, which...

A Novel, Highly Enantioselective Ketone Alkynylation Reaction Mediated by Chiral Zinc Aminoalkoxides.

Angewandte Chemie (International ed. in English)

Tan L, Chen CY, Tillyer RD, Grabowski EJJ, Reider PJ.
PMID: 29711532
Angew Chem Int Ed Engl. 1999 Mar 01;38(5):711-713. doi: 10.1002/(SICI)1521-3773(19990301)38:5<711::AID-ANIE711>3.0.CO;2-W.

Kilogram-scale synthesis of the HIV reverse transcriptase inhibitor efavirenz was achieved by means of a highly enantioselective alkynylation of prochiral ketones 1 with alkynyllithium or alkynylmagnesium reagents in the presence of chiral zinc aminoalkoxides as mediators. With the achiral...

Synthesis and Evolution of a Threose Nucleic Acid Aptamer Bearing 7-Deaza-7-Substituted Guanosine Residues.

Journal of the American Chemical Society

Mei H, Liao JY, Jimenez RM, Wang Y, Bala S, McCloskey C, Switzer C, Chaput JC.
PMID: 29667819
J Am Chem Soc. 2018 May 02;140(17):5706-5713. doi: 10.1021/jacs.7b13031. Epub 2018 Apr 23.

In vitro selection experiments carried out on artificial genetic polymers require robust and faithful methods for copying genetic information back and forth between DNA and xeno-nucleic acids (XNA). Previously, we have shown that Kod-RI, an engineered polymerase developed to...

N-3 Hydroxylation of Pyrimidine-2,4-diones Yields Dual Inhibitors of HIV Reverse Transcriptase and Integrase.

ACS medicinal chemistry letters

Tang J, Maddali K, Dreis CD, Sham YY, Vince R, Pommier Y, Wang Z.
PMID: 21499541
ACS Med Chem Lett. 2011 Jan;2(1):63-67. doi: 10.1021/ml1002162.

A new molecular scaffold featuring an N-hydroxyimide functionality and capable of inhibiting both reverse transcriptase (RT) and integrase (IN) of Human Immunodeficiency Virus (HIV) was rationally designed based on 1-[(2-hydroxyethoxy) methyl]-6-(phenylthio)-thymine (HEPT) non-nucleoside RT inhibitors (NNRTIs). The design involves...

Anti-HIV reverse transcriptase plant polyphenolic natural products with in silico inhibitory properties on seven non-structural proteins vital in SARS-CoV-2 pathogenesis.

Journal, genetic engineering & biotechnology

de Leon VNO, Manzano JAH, Pilapil DYH, Fernandez RAT, Ching JKAR, Quimque MTJ, Agbay JCM, Notarte KIR, Macabeo APG.
PMID: 34272647
J Genet Eng Biotechnol. 2021 Jul 16;19(1):104. doi: 10.1186/s43141-021-00206-2.

BACKGROUND: Accessing COVID-19 vaccines is a challenge despite successful clinical trials. This burdens the COVID-19 treatment gap, thereby requiring accelerated discovery of anti-SARS-CoV-2 agents. This study explored the potential of anti-HIV reverse transcriptase (RT) phytochemicals as inhibitors of SARS-CoV-2...

Showing 1 to 12 of 53 entries