NDLI: In vivo Pharmacokinetics and Toxicity of a Novel Hydrophilic Oral Formulation of the Potent Non-Nucleoside Reverse Transcriptase Inhibitor Compound N'-[2-(2-Thiophene)ethyl]-N'-[2-(5-bromopyridyl)]-thiourea (HI-443)

Please wait, while we are loading the content...

In vivo Pharmacokinetics and Toxicity of a Novel Hydrophilic Oral Formulation of the Potent Non-Nucleoside Reverse Transcriptase Inhibitor Compound N'-[2-(2-Thiophene)ethyl]-N'-[2-(5-bromopyridyl)]-thiourea (HI-443)

Content Provider	Scilit
Author	Uckun, Fatih M. Tibbies, Heather Erbeck, Douglas Venkatachalam, Taracad K. Qazi, Sanjive
Copyright Year	2007
Description	The thiophene ethyl thiourea (TET) compound N'-[2-(2-thiophene) ethyl]-N'- [2-(5-bromopyridyl)]-thiourea (HI-443) is a potent non-nucleoside reverse transcriptase inhibitor (NNRTI). The pharmacokinetics of 17 different novel oral formulations of HI-443 were compared in an attempt to identify the most suitable dosage form for clinical use in HIV-infected persons. Plasma concentrations of HI-443 were monitored in mice after administration of the drug using these 17 different formulations at three time points. Two-way ANOVA showed highly significant formulation (p<0.0001), time (p<0.0001) and formulation*time interaction effects (p=0.0003). Planned linear contrasts were performed to identify which formulations showed the highest bioavailability at 10, 30, 60 min and at all time points relative to DMSO alone. A significant positive regression was observed comparing bioavailibility of HI-443 at 10 min and hy-drophilic-lipophilic balance (HLB) values of the formulations $(R^{2}$ = 26%, p<0.0001). The results showed that formulations that were hydrophilic, containing PEG400 and propylene glycol, gave the highest overall drug concentrations over the 60-min time period. The lead oral formulation of HI-443 exhibited a very favorable toxicity profile in BALB/c mice.
Related Links	http://www.thieme-connect.de/products/ejournals/pdf/10.1055/s-0031-1296608.pdf
Ending Page	226
Page Count	9
Starting Page	218
ISSN	00044172
e-ISSN	16167066
DOI	10.1055/s-0031-1296608
Journal	Arzneimittelforschung
Issue Number	04
Volume Number	57
Language	English
Publisher	Georg Thieme Verlag KG
Publisher Date	2007-04-01
Access Restriction	Open
Subject Keyword	Journal: Arzneimittelforschung Pharmacology and Pharmacy in Vivo Pharmacokinetics Non-nucleoside Reverse Transcriptase Inhibitor N'-[2-(2-thiophene)ethyl]-n'-[2-(5-bromopyridyl)]-thiourea
Content Type	Text
Resource Type	Article
Subject	Drug Discovery

Sl.	Authority	Responsibilities	Communication Details
1	Ministry of Education (GoI), Department of Higher Education	Sanctioning Authority	https://www.education.gov.in/ict-initiatives
2	Indian Institute of Technology Kharagpur	Host Institute of the Project: The host institute of the project is responsible for providing infrastructure support and hosting the project	https://www.iitkgp.ac.in
3	National Digital Library of India Office, Indian Institute of Technology Kharagpur	The administrative and infrastructural headquarters of the project	Dr. B. Sutradhar bsutra@ndl.gov.in
4	Project PI / Joint PI	Principal Investigator and Joint Principal Investigators of the project	Dr. B. Sutradhar bsutra@ndl.gov.in Prof. Saswat Chakrabarti will be added soon
5	Website/Portal (Helpdesk)	Queries regarding NDLI and its services	support@ndl.gov.in
6	Contents and Copyright Issues	Queries related to content curation and copyright issues	content@ndl.gov.in
7	National Digital Library of India Club (NDLI Club)	Queries related to NDLI Club formation, support, user awareness program, seminar/symposium, collaboration, social media, promotion, and outreach	clubsupport@ndl.gov.in
8	Digital Preservation Centre (DPC)	Assistance with digitizing and archiving copyright-free printed books	dpc@ndl.gov.in
9	IDR Setup or Support	Queries related to establishment and support of Institutional Digital Repository (IDR) and IDR workshops	idr@ndl.gov.in

In vivo Pharmacokinetics, Metabolism, Toxicity, and Anti-HIV Activity of N'-[2-(2-Thiophene)ethyl]-N'-[2-(5-bromopyridyl)]thiourea (HI-443), a Potent Non-nucleoside Inhibitor of HIV Reverse Transcriptase

N'-[2-(2-Thiophene)ethyl]-N'-[2-(5-bromopyridyl)]thiourea (HI-443), a Rationally Designed Non-Nucleoside Reverse Transcriptase Inhibitor Compound with Potent Anti-HIV Activity

Improved Oral Bioavailability of Anti-HIV Agent N'-[2-(2-Thiophene)ethyl]-NT-[2-(5-bromopyridyl)]-thiourea (HI-443) in a Novel Lipophilic Formulation

Large-scale Synthesis of GMP Grade N'-[2-(2-Thiophene)ethyl]-N'-[2-(5-bromopyridyl)]-thiourea (HI-443), a New Anti-HIV Drug Candidate

In vivo Toxicity, Pharmacokinetic Features and Tissue Distribution of N-[2-(2,5-Dimethoxyphenylethyl)]-N’-[2-(5-bromopyridyl)]-thiourea (HI-236), a Potent Non-nucleoside Inhibitor of HIV-1 Reverse Transcriptase

Stampidine as a Novel Nucleoside Reverse Transcriptase Inhibitor with Potent Anti-HIV Activity

A novel vaginal microbicide containing the rationally designed anti-HIV compound HI-443 (N'-[2-(2-thiophene)ethyl]-N'-[2-(5-bromopyridyl)] thiourea]).

Evaluation of the Pharmacokinetic Features and Tissue Distribution of the Potent Nonnucleoside Inhibitor of HIV-1 Reverse Transcriptase, N-[2-(2-fluorophenethyl)]-N′-[2-(5-bromopyridyl)]-thiourea (HI-240) with an Analytical HPLC Method

Discovery of 2,5-dimethoxy-substituted 5-bromopyridyl thiourea (PHI-236) as a potent broad-spectrum anti-human immunodeficiency virus microbicide

In vivo Pharmacokinetics and Toxicity of a Novel Hydrophilic Oral Formulation of the Potent Non-Nucleoside Reverse Transcriptase Inhibitor Compound N'-[2-(2-Thiophene)ethyl]-N'-[2-(5-bromopyridyl)]-thiourea (HI-443)

Similar Documents

In vivo Pharmacokinetics, Metabolism, Toxicity, and Anti-HIV Activity of N'-[2-(2-Thiophene)ethyl]-N'-[2-(5-bromopyridyl)]thiourea (HI-443), a Potent Non-nucleoside Inhibitor of HIV Reverse Transcriptase

N'-[2-(2-Thiophene)ethyl]-N'-[2-(5-bromopyridyl)]thiourea (HI-443), a Rationally Designed Non-Nucleoside Reverse Transcriptase Inhibitor Compound with Potent Anti-HIV Activity

Improved Oral Bioavailability of Anti-HIV Agent N'-[2-(2-Thiophene)ethyl]-NT-[2-(5-bromopyridyl)]-thiourea (HI-443) in a Novel Lipophilic Formulation

Large-scale Synthesis of GMP Grade N'-[2-(2-Thiophene)ethyl]-N'-[2-(5-bromopyridyl)]-thiourea (HI-443), a New Anti-HIV Drug Candidate

In vivo Toxicity, Pharmacokinetic Features and Tissue Distribution of N-[2-(2,5-Dimethoxyphenylethyl)]-N’-[2-(5-bromopyridyl)]-thiourea (HI-236), a Potent Non-nucleoside Inhibitor of HIV-1 Reverse Transcriptase

Stampidine as a Novel Nucleoside Reverse Transcriptase Inhibitor with Potent Anti-HIV Activity

A novel vaginal microbicide containing the rationally designed anti-HIV compound HI-443 (N'-[2-(2-thiophene)ethyl]-N'-[2-(5-bromopyridyl)] thiourea]).

Evaluation of the Pharmacokinetic Features and Tissue Distribution of the Potent Nonnucleoside Inhibitor of HIV-1 Reverse Transcriptase, N-[2-(2-fluorophenethyl)]-N′-[2-(5-bromopyridyl)]-thiourea (HI-240) with an Analytical HPLC Method

Discovery of 2,5-dimethoxy-substituted 5-bromopyridyl thiourea (PHI-236) as a potent broad-spectrum anti-human immunodeficiency virus microbicide

In vivo Pharmacokinetics and Toxicity of a Novel Hydrophilic Oral Formulation of the Potent Non-Nucleoside Reverse Transcriptase Inhibitor Compound N'-[2-(2-Thiophene)ethyl]-N'-[2-(5-bromopyridyl)]-thiourea (HI-443)