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Targeting delavirdine/atevirdine resistant HIV-1: identification of (alkylamino)piperidine-containing bis(heteroaryl)piperazines as broad spectrum HIV-1 reverse transcriptase inhibitors. 1996
D L Romero, and
R A Olmsted, and
T J Poel, and
R A Morge, and
C Biles, and
B J Keiser, and
L A Kopta, and
J M Friis, and
J D Hosley, and
K J Stefanski, and
D G Wishka, and
D B Evans, and
J Morris, and
R G Stehle, and
S K Sharma, and
Y Yagi, and
R L Voorman, and
W J Adams, and
W G Tarpley, and
R C Thomas
DDR&D Pharmaceutics, Pharmacia & Upjohn, Inc, Kalamazoo, Michigan 49001, USA.
A novel class of bis(heteroaryl)piperazine (BHAP) analogs which possesses the ability to inhibit NNRTI (non-nucleoside reverse transcriptase inhibitor) resistant recombinant HIV-1 reverse transcriptase (RT) and NNRTI resistant variants of HIV-1 has been identified via targeted screening. Further investigation of the structure-activity relationships of close congeners of these novel (alkylamino)piperidine BHAPs (AAP-BHAPs) led to the synthesis of several compounds possessing the desired phenotype (e.g., activity against recombinant RTs carrying the Y181C and P236L substitutions). Further structural modifications were required to inhibit metabolism and modulate solubility in order to obtain compounds with the desired biological profile as well as appropriate pharmaceutical properties. The AAP-BHAPs with the most suitable characteristics were compounds 7, 15, and 36.
Related Publications
D L Romero, and
R A Olmsted, and
T J Poel, and
R A Morge, and
C Biles, and
B J Keiser, and
L A Kopta, and
J M Friis, and
J D Hosley, and
K J Stefanski, and
D G Wishka, and
D B Evans, and
J Morris, and
R G Stehle, and
S K Sharma, and
Y Yagi, and
R L Voorman, and
W J Adams, and
W G Tarpley, and
R C Thomas
January 2010,
Mini reviews in medicinal chemistry,
D L Romero, and
R A Olmsted, and
T J Poel, and
R A Morge, and
C Biles, and
B J Keiser, and
L A Kopta, and
J M Friis, and
J D Hosley, and
K J Stefanski, and
D G Wishka, and
D B Evans, and
J Morris, and
R G Stehle, and
S K Sharma, and
Y Yagi, and
R L Voorman, and
W J Adams, and
W G Tarpley, and
R C Thomas
April 1994,
Journal of medicinal chemistry,
D L Romero, and
R A Olmsted, and
T J Poel, and
R A Morge, and
C Biles, and
B J Keiser, and
L A Kopta, and
J M Friis, and
J D Hosley, and
K J Stefanski, and
D G Wishka, and
D B Evans, and
J Morris, and
R G Stehle, and
S K Sharma, and
Y Yagi, and
R L Voorman, and
W J Adams, and
W G Tarpley, and
R C Thomas
October 2010,
Bioorganic & medicinal chemistry letters,
D L Romero, and
R A Olmsted, and
T J Poel, and
R A Morge, and
C Biles, and
B J Keiser, and
L A Kopta, and
J M Friis, and
J D Hosley, and
K J Stefanski, and
D G Wishka, and
D B Evans, and
J Morris, and
R G Stehle, and
S K Sharma, and
Y Yagi, and
R L Voorman, and
W J Adams, and
W G Tarpley, and
R C Thomas
June 2014,
European journal of medicinal chemistry,
D L Romero, and
R A Olmsted, and
T J Poel, and
R A Morge, and
C Biles, and
B J Keiser, and
L A Kopta, and
J M Friis, and
J D Hosley, and
K J Stefanski, and
D G Wishka, and
D B Evans, and
J Morris, and
R G Stehle, and
S K Sharma, and
Y Yagi, and
R L Voorman, and
W J Adams, and
W G Tarpley, and
R C Thomas
November 2022,
Molecules (Basel, Switzerland),
D L Romero, and
R A Olmsted, and
T J Poel, and
R A Morge, and
C Biles, and
B J Keiser, and
L A Kopta, and
J M Friis, and
J D Hosley, and
K J Stefanski, and
D G Wishka, and
D B Evans, and
J Morris, and
R G Stehle, and
S K Sharma, and
Y Yagi, and
R L Voorman, and
W J Adams, and
W G Tarpley, and
R C Thomas
August 2017,
Journal of medicinal chemistry,
D L Romero, and
R A Olmsted, and
T J Poel, and
R A Morge, and
C Biles, and
B J Keiser, and
L A Kopta, and
J M Friis, and
J D Hosley, and
K J Stefanski, and
D G Wishka, and
D B Evans, and
J Morris, and
R G Stehle, and
S K Sharma, and
Y Yagi, and
R L Voorman, and
W J Adams, and
W G Tarpley, and
R C Thomas
July 1997,
Drug metabolism and disposition: the biological fate of chemicals,
D L Romero, and
R A Olmsted, and
T J Poel, and
R A Morge, and
C Biles, and
B J Keiser, and
L A Kopta, and
J M Friis, and
J D Hosley, and
K J Stefanski, and
D G Wishka, and
D B Evans, and
J Morris, and
R G Stehle, and
S K Sharma, and
Y Yagi, and
R L Voorman, and
W J Adams, and
W G Tarpley, and
R C Thomas
October 2011,
Nucleic acids research,
D L Romero, and
R A Olmsted, and
T J Poel, and
R A Morge, and
C Biles, and
B J Keiser, and
L A Kopta, and
J M Friis, and
J D Hosley, and
K J Stefanski, and
D G Wishka, and
D B Evans, and
J Morris, and
R G Stehle, and
S K Sharma, and
Y Yagi, and
R L Voorman, and
W J Adams, and
W G Tarpley, and
R C Thomas
July 2013,
ChemMedChem,
D L Romero, and
R A Olmsted, and
T J Poel, and
R A Morge, and
C Biles, and
B J Keiser, and
L A Kopta, and
J M Friis, and
J D Hosley, and
K J Stefanski, and
D G Wishka, and
D B Evans, and
J Morris, and
R G Stehle, and
S K Sharma, and
Y Yagi, and
R L Voorman, and
W J Adams, and
W G Tarpley, and
R C Thomas
April 2008,
Chembiochem : a European journal of chemical biology,
