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Swami Swaminathan

Explore the profile of Swami Swaminathan including associated specialties, affiliations and a list of published articles. Areas
Snapshot
Articles 14
Citations 1558
Followers 0
Related Specialties
Biochemistry
Pharmacology
Microbiology
Top 10 Co-Authors
Tomas Cihlar
Lijun Zhang
Xiaohong Liu
William A Lee
Richard L Mackman
Kirsten M Stray
Gong-Xin He
Christian Callebaut
William Lee
Michel Perron
Published In
Antimicrob Agents Chemother
Nature
Bioorg Med Chem Lett
J Virol
Bioorg Med Chem
Affiliations
Soon will be listed here.
Recent Articles
1.
Discovery and development of oseltamivir at Gilead Sciences
Schmitz U, Swaminathan S
Antivir Ther . 2022 May; 27(2):13596535211067598. PMID: 35499178
John Martin's untimely death in March 2021 was a huge loss for us personally, Gilead Sciences, the company he built over 30 years and the scientific community concerned with antiviral...
2.
Clinical targeting of HIV capsid protein with a long-acting small molecule
Link J, Rhee M, Tse W, Zheng J, Somoza J, Rowe W, et al.
Nature . 2020 Jul; 584(7822):614-618. PMID: 32612233
Oral antiretroviral agents provide life-saving treatments for millions of people living with HIV, and can prevent new infections via pre-exposure prophylaxis. However, some people living with HIV who are heavily...
3.
Discovery and Synthesis of a Phosphoramidate Prodrug of a Pyrrolo[2,1-f][triazin-4-amino] Adenine C-Nucleoside (GS-5734) for the Treatment of Ebola and Emerging Viruses
Siegel D, Hui H, Doerffler E, Clarke M, Chun K, Zhang L, et al.
J Med Chem . 2017 Jan; 60(5):1648-1661. PMID: 28124907
The recent Ebola virus (EBOV) outbreak in West Africa was the largest recorded in history with over 28,000 cases, resulting in >11,000 deaths including >500 healthcare workers. A focused screening...
4.
Therapeutic efficacy of the small molecule GS-5734 against Ebola virus in rhesus monkeys
Warren T, Jordan R, Lo M, Ray A, Mackman R, Soloveva V, et al.
Nature . 2016 Mar; 531(7594):381-5. PMID: 26934220
The most recent Ebola virus outbreak in West Africa, which was unprecedented in the number of cases and fatalities, geographic distribution, and number of nations affected, highlights the need for...
5.
Discovery of β-D-2'-deoxy-2'-α-fluoro-4'-α-cyano-5-aza-7,9-dideaza adenosine as a potent nucleoside inhibitor of respiratory syncytial virus with excellent selectivity over mitochondrial RNA and DNA polymerases
Clarke M, Mackman R, Byun D, Hui H, Barauskas O, Birkus G, et al.
Bioorg Med Chem Lett . 2015 May; 25(12):2484-7. PMID: 25978965
Novel 4'-substituted β-d-2'-deoxy-2'-α-fluoro (2'd2'F) nucleoside inhibitors of respiratory syncytial virus (RSV) are reported. The introduction of 4'-substitution onto 2'd2'F nucleoside analogs resulted in compounds demonstrating potent cell based RSV inhibition,...
6.
Structure-activity relationships of diamine inhibitors of cytochrome P450 (CYP) 3A as novel pharmacoenhancers. Part II: P2/P3 region and discovery of cobicistat (GS-9350)
Xu L, Liu H, Hong A, Vivian R, Murray B, Callebaut C, et al.
Bioorg Med Chem Lett . 2014 Jan; 24(3):995-9. PMID: 24412072
The HIV protease inhibitor (PI) ritonavir (RTV) has been widely used as a pharmacoenhancer for other PIs, which are substrates of cytochrome P450 3A (CYP3A). However the potent anti-HIV activity...
7.
In vitro characterization of GS-8374, a novel phosphonate-containing inhibitor of HIV-1 protease with a favorable resistance profile
Callebaut C, Stray K, Tsai L, Williams M, Yang Z, Cannizzaro C, et al.
Antimicrob Agents Chemother . 2011 Jan; 55(4):1366-76. PMID: 21245449
GS-8374 is a novel bis-tetrahydrofuran HIV-1 protease (PR) inhibitor (PI) with a unique diethylphosphonate moiety. It was selected from a series of analogs containing various di(alkyl)phosphonate substitutions connected via a...
8.
Synthesis and anti-HIV activity of cyclic pyrimidine phosphonomethoxy nucleosides and their prodrugs: a comparison of phosphonates and corresponding nucleosides
Mackman R, Zhang L, Prasad V, Boojamra C, Chen J, Douglas J, et al.
Nucleosides Nucleotides Nucleic Acids . 2007 Dec; 26(6-7):573-7. PMID: 18066858
Cyclic phosphonomethoxy pyrimidine nucleosides that are bioisosteres of the monophosphate metabolites of HIV reverse transcriptase (RT) inhibitors AZT, d4T, and ddC have been synthesized. The RT inhibitory activities of the...
9.
Synthesis, anti-HIV activity, and resistance profile of thymidine phosphonomethoxy nucleosides and their bis-isopropyloxymethylcarbonyl (bisPOC) prodrugs
Mackman R, Zhang L, Prasad V, Boojamra C, Douglas J, Grant D, et al.
Bioorg Med Chem . 2007 Jun; 15(16):5519-28. PMID: 17562366
Phosphonomethoxy nucleoside analogs of the thymine containing nucleoside reverse transcriptase inhibitors (NRTIs), 3'-azido-2',3'-dideoxythymidine (AZT), 2',3'-didehydro-2',3'-dideoxythymidine (d4T), and 2',3'-dideoxythymidine (ddT), were synthesized. The anti-HIV activity against wild-type and several major nucleoside-resistant...
10.
Cathepsin A is the major hydrolase catalyzing the intracellular hydrolysis of the antiretroviral nucleotide phosphonoamidate prodrugs GS-7340 and GS-9131
Birkus G, Wang R, Liu X, Kutty N, MacArthur H, Cihlar T, et al.
Antimicrob Agents Chemother . 2006 Dec; 51(2):543-50. PMID: 17145787
GS-7340 and GS-9131 {9-[(R)-2-[[(S)-[[(S)-1-(isopropoxycarbonyl)ethyl]amino]phenoxyphosphinyl]methoxy]-propyl]adenine and 9-(R)-4'-(R)-[[[(S)-1-[(ethoxycarbonyl)ethyl]amino]phenoxyphosphinyl]methoxy]-2'-fluoro-1'-furanyladenine, respectively} are novel alkylalaninyl phenyl ester prodrugs of tenofovir {9-R-[(2-phosphonomethoxy)propyl]adenine} (TFV) and a cyclic nucleotide analog, GS-9148 (phosphonomethoxy-2'-fluoro-2', 3'-dideoxydidehydroadenosine), respectively. Both prodrugs exhibit potent...