Pyridazino[3,4-b][1,5]benzoxazepin-5(6H)-ones: Synthesis and biological evaluation

被引：16

作者：

Barth, B

Dierich, M

Heinisch, G

Jenny, V

Matuszczak, B

Mereiter, K

Planer, R

Schopf, I

Stoiber, H

Traugott, T

vonAufschnaiter, P

机构：

[1] UNIV INNSBRUCK, INST PHARMACEUT CHEM, A-6020 INNSBRUCK, AUSTRIA

[2] UNIV INNSBRUCK, INST HYG, LUDWIG BOLTZMANN INST AIDS RES, A-6020 INNSBRUCK, AUSTRIA

[3] VIENNA TECH UNIV, INST MINERAL CRYSTALLOG & STRUCT CHEM, A-1060 VIENNA, AUSTRIA

来源：

ANTIVIRAL CHEMISTRY & CHEMOTHERAPY | 1996年 / 7卷 / 06期

关键词：

HIV; non-nucleosides; pyridazino[3,4-b][1,5]benzoxazepin-5(6H)-ones; reverse transcriptase inhibitors;

D O I：

10.1177/095632029600700603

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

Starting from 3,6-dichloro-4-pyridazinecarboxylic acid chloride a series of novel pyridazino[3,4-b][1,5]benzoxazepin-5(6H)-ones as 1,2-diazine isosters of non-nucleoside reverse transcriptase inhibitors was prepared via N-(2-hydroxyphenyl)-3,6-dichloro-4-pyridazinecarboxamides, The inhibition of HIV-1 reverse transcriptase was evaluated.

引用

页码：300 / 312

页数：13

共 17 条

[1]

Adams Julian, 1993, P45

[2]

BARTH B, 1996, UNPUB ARCH PHARM MED

[3] SYNTHESIS AND ANTIVIRAL EVALUATION OF FLUORINATED DIPYRIDODIAZEPINONES AND DIPYRIDODIAZEPINES (NEVIRAPINE DERIVATIVES) [J].

BOYODE, BP ;

SINET, M ;

FARESE, A ;

FORESTIERROUX, MA ;

CONDOM, R ;

AYI, IA ;

KIRN, A ;

MOOG, C ;

GUEDJ, R .

ANTIVIRAL CHEMISTRY & CHEMOTHERAPY, 1995, 6 (03) :162-168

[4]

De Clercq E., 1994, EXPERT OPIN INV DRUG, V3, P253

[5]

DECLERCQ E, 1994, INT J IMMUNOTHER, V10, P145

[6] ANTIVIRAL THERAPY FOR HUMAN-IMMUNODEFICIENCY-VIRUS INFECTIONS [J].

DECLERCQ, E .

CLINICAL MICROBIOLOGY REVIEWS, 1995, 8 (02) :200-239

[7] NOVEL NONNUCLEOSIDE INHIBITORS OF HIV-1 REVERSE-TRANSCRIPTASE .1. TRICYCLIC PYRIDOBENZODIAZEPINONES AND DIPYRIDODIAZEPINONES [J].

HARGRAVE, KD ;

PROUDFOOT, JR ;

GROZINGER, KG ;

CULLEN, E ;

KAPADIA, SR ;

PATEL, UR ;

FUCHS, VU ;

MAULDIN, SC ;

VITOUS, J ;

BEHNKE, ML ;

KLUNDER, JM ;

PAL, K ;

SKILES, JW ;

MCNEIL, DW ;

ROSE, JM ;

CHOW, GC ;

SKOOG, MT ;

WU, JC ;

SCHMIDT, G ;

ENGEL, WW ;

EBERLEIN, WG ;

SABOE, TD ;

CAMPBELL, SJ ;

ROSENTHAL, AS ;

ADAMS, J .

JOURNAL OF MEDICINAL CHEMISTRY, 1991, 34 (07) :2231-2241

[8] SYNTHESES AND REACTIONS OF PYRIDAZINE DERIVATIVES .1. A) NEW SYNTHESIS OF PYRIDAZINE-4-CARBOXYLIC ACID, B) SYNTHESIS AND REACTIONS OF ETHYL-3-OXO-3-(4'-PYRIDAZINYL)-PROPIONATE [J].

HEINISCH, G .

MONATSHEFTE FUR CHEMIE, 1973, 104 (04) :953-962

[9] PYRIDAZINES .71. A NOVEL TYPE OF 1,2-DIAZINE -] 1,2-DIAZOLE RING CONTRACTION [J].

HEINISCH, G ;

MATUSZCZAK, B ;

MEREITER, K .

HETEROCYCLES, 1994, 38 (09) :2081-2089

[10] NOVEL NONNUCLEOSIDE INHIBITORS OF HUMAN-IMMUNODEFICIENCY-VIRUS TYPE-1 REVERSE-TRANSCRIPTASE .5. 4-SUBSTITUTED AND 2,4-DISUBSTITUTED ANALOGS OF NEVIRAPINE [J].

KELLY, TA ;

PROUDFOOT, JR ;

MCNEIL, DW ;

PATEL, UR ;

DAVID, E ;

HARGRAVE, KD ;

GROB, PM ;

CARDOZO, M ;

AGARWAL, A ;

ADAMS, J .

JOURNAL OF MEDICINAL CHEMISTRY, 1995, 38 (24) :4839-4847

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