SYNTHESIS OF PYRRYL ARYL SULFONES TARGETED AT THE HIV-1 REVERSE-TRANSCRIPTASE

被引：35

作者：

ARTICO, M

SILVESTRI, R

STEFANCICH, G

MASSA, S

SCINTU, F

PAGNOZZI, E

MASU, D

PINNA, E

TINTI, E

LACOLLA, P

机构：

[1] UNIV TRIESTE,DIPARTIMENTO SCI FARMACEUT,I-34127 TRIESTE,ITALY

[2] UNIV CAGLIARI,DIPARTIMENTO BIOL SPERIMENTALE,I-09124 CAGLIARI,ITALY

来源：

ARCHIV DER PHARMAZIE | 1995年 / 328卷 / 03期

关键词：

D O I：

10.1002/ardp.19953280304

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Various aryl 1-pyrryl sulfones were synthesized and tested as inhibitors of HIV-1, 2-Nitrophenyl-2-ethoxycarbonyl-1-pyrryl sulfone, the most active among test derivatives, was selected as lead compound of the aryl pyrryl sulfone series. The in vitro anti-HIV-1 activity and cytotoxicity of 41 compounds is reported. Some structure-activity relationships are discussed also in comparison with the known NPPS (2-nitorphenyl phenyl sulfone).

引用

页码：223 / 229

页数：7

共 19 条

[11] RAPID AND AUTOMATED TETRAZOLIUM-BASED COLORIMETRIC ASSAY FOR THE DETECTION OF ANTI-HIV COMPOUNDS
PAUWELS, R
BALZARINI, J
BABA, M
SNOECK, R
SCHOLS, D
HERDEWIJN, P
DESMYTER, J
DECLERCQ, E
[J]. JOURNAL OF VIROLOGICAL METHODS, 1988, 20 (04) : 309 - 321
[12] HETEROCYCLES WITH A BENZOTHIADIAZEPINE MOIETY .3. SYNTHESIS OF IMIDAZO[5,1-D]PYRROLO[1,2-B][1,2,5]BENZOTHIADIAZEPINE 9,9-DIOXIDE
SILVESTRI, R
ARTICO, M
PAGNOZZI, E
[J]. JOURNAL OF HETEROCYCLIC CHEMISTRY, 1994, 31 (04) : 1033 - 1036
[13] HETEROCYCLES WITH A BENZOTHIADIAZEPINE MOIETY .4. SYNTHESIS OF NOVEL TETRACYCLIC RINGS BY INTRAMOLECULAR CYCLIZATION OF 10-BROMOACETYL-10,11-DIHYDRO-11-ETHOXYCARBONYLPYRROLO[1,2-B] [1,2,5] BENZOTHIADIAZEPINE 5,5-DIOXIDE AND ITS DERIVATIVES
SILVESTRI, R
PAGNOZZI, E
STEFANCICH, G
ARTICO, M
[J]. SYNTHETIC COMMUNICATIONS, 1994, 24 (19) : 2685 - 2695
[14] STEFANCICH G, 1983, SYNTHESIS-STUTTGART, P757
[15] STEFANCICH G, 1990, FARMACO, V45, P7
[16] RESEARCH ON NITROGEN-CONTAINING HETEROCYCLIC-COMPOUNDS .19. SYNTHESIS OF 8H-IMIDAZO[2,1-C]-S-TRIAZOLO[4,3-A]-[1,4]BENZODIAZEPINE AND ITS 1-DERIVATIVES
STEFANCICH, G
SILVESTRI, R
ARTICO, M
[J]. JOURNAL OF HETEROCYCLIC CHEMISTRY, 1993, 30 (02) : 529 - 532
[17] RESEARCH ON NITROGEN CONTAINING HETEROCYCLIC-COMPOUNDS .18. SYNTHESIS OF 9H-PYRROLO[2,1-C]-SYM-TRIAZOLO[4,3-A][1,4]BENZODIAZEPINE, A NOVEL TETRACYCLIC RING OF PHARMACEUTICAL INTEREST
STEFANCICH, G
ARTICO, M
SILVESTRI, R
[J]. JOURNAL OF HETEROCYCLIC CHEMISTRY, 1992, 29 (04) : 1005 - 1007
[18] STEFANCICH G, 1990, FARMACO, V45, P817
[19] TRAMONTANO E, 1992, BIOCHEM PHARMACOL, V43, P1371

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