154355-83-6

Upstream product

• 63877-96-3 2-(4-fluorophenylmethyl)thiophene 
• 459-46-1 4-Fluorobenzyl bromide 
• 1003-09-4 2-bromothiophene 
• 352-13-6 4-flourophenylmagnesium bromide 
• 4701-17-1 5-bromo-2-thiophencarboxaldehyde 
• 848413-49-0 (5-bromothiophen-2-yl)(4-fluorophenyl)methanol 

Downstream Products

• 173095-30-2 4-<5-<(4-fluorophenyl)methyl>-2-thienyl>-3-butyn-2-ol 
• 154355-75-6 N-{3-[5-(4-fluorophenylmethyl)-thien-2-yl]-1-methyl-2-propynyl}-N-hydroxyurea 
• 173095-31-3 C₂₉H₂₂FNO₅S 
• 1026236-96-3 C₂₈H₂₀FNO₅S 
• 1026596-32-6 3-[5-(4-Fluoro-benzyl)-thiophen-2-yl]-prop-2-yn-1-ol 

Relevant academic research and scientific papers

INHIBITORS OF HUMAN IMMUNODEFICIENCY VIRUS REPLICATION

The disclosure generally relates to compounds of formula I, including compositions and methods for treating human immunodeficiency virus (HIV) infection. The disclosure provides novel inhibitors of HIV, pharmaceutical compositions containing such compound

7-HETEROARYLSULFONYL-TETRAHYDRO-3-BENZAZEPINE DERIVATIVES AS ANTIPSYCHOTIC AGENTS

The invention provides compounds of formula (I): wherein A and B represent the groups -(CH2)m- and -(CH2)n- respectively; R1 represents hydrogen or C1-6alkyl; R2 represents hydro

Substituted arylalkynyl-and heteroarylalkynl-N-hydroxyurea inhibitors of leukotriene biosynthesis

The invention relates to compounds having activity to inhibit lipoxygenase enzyme activity, to pharmaceutical compositions comprising these compounds, and to a medical method of treating. More particularly, this invention concerns certain substituted arylalkynyl- and ((heteroaryl)alkynyl)-N-hydroxy-ureas which inhibit leukotriene biosynthesis, to pharmaceutical compositions of these compounds and to a method of inhibiting leukotriene biosynthesis.

(R)-(+)-N-[3-[5-[(4-fluorophenyl)methyl]-2-thienyl]-1-methyl-2-propynyl]- N-hydroxyurea (ABT-761), a second-generation 5-lipoxygenase inhibitor

Structure-activity optimization of inhibitory potency and duration of action of N-hydroxyurea containing 5-lipoxygenase inhibitors was conducted. The lipophilic heteroaryl template and the link group connecting the template to the N-hydroxyurea pharmacophore were modified. Inhibition of 5- lipoxygenase was evaluated in vitro in a human whole blood assay. An in vitro assay using liver microsomes from monkey was used to evaluate congeners for comparative rates of glucuronidation. (3-Heteroaryl-1-methyl-2-propynyl)-N- hydroxyureas were found to be more resistant to in vitro glucuronidation. The promising inhibitor N-[3-[5-(4-fluorophenoxy)-2-furyl]-1-methyl-2-propynyl]- N-hydroxyurea (6) was found to have stereoselective glucuronidation in monkey and man. The R enantiomer 7 provided longer duration of inhibition as evaluated by an ex vivo whole blood assay. Further optimization of the lipophilic template led to the discovery of (R)-(+)-N-[3-[5-[(4- fluorophenyl)methyl]-2-thienyl]-1-methyl-2-propynyl]-N-hydroxyurea (11) with more effective and prolonged inhibition of leukotriene biosynthesis than zileuton (1) and 7 in monkey and man. The optimized 5-lipoxygenase inhibitor 11 was selected for development as an investigational drug for leukotriene- mediated disorders.

[(SUBSTITUTED) PHENYALKYL]FURYLALKYNYL-AND [SUBSTITUTED)PHENYALKYL]THIENYLALKYNYL-N-HYDROXYUREA INHIBITORS OR LEUKOTRIENE BIOSYNTHESIS

The present invention relates to compounds of the formula and the pharmaceutically acceptable salts thereof wherein Z is selected from optionally substituted phenyl, furyl, thienyl or thiazolyl; which inhibits leukotriene biosynthesis and is useful in the treatment of inflammatory disease states; also disclosed are leukotriene biosynthesis inhibiting compositions and a method for inhibiting 5-lipoxygenase activity and leukotriene biosynthesis