New rifabutin analogs:: Synthesis and biological activity against Mycobacterium tuberculosis

被引：27

作者：

Barluenga, Jose

Aznar, Fernando

Garcia, Ana-Belen

Cabal, Maria-Paz

Palacios, Juan J.

Menendez, Maria-Angela

机构：

[1] Univ Oviedo, Inst Univ Quim Organomet Enrique Moles, Unidad Asociada, CSIC, E-33006 Oviedo, Spain

[2] Hosp Univ Cent Asturias, Unidad Referencia Reg Micobacterias, E-33006 Oviedo, Spain

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2006年 / 16卷 / 22期

关键词：

rifamycins; rifabutin; Rifastures; Mycobacterium tuberculosis;

D O I：

10.1016/j.bmcl.2006.08.090

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The synthesis, structure, and biological evaluation of a series of novel rifamycin derivatives, Rifastures (RFA) with potent anti-tuberculosis activity are presented. Some of these derivatives showed higher in vitro activity than rifabutin and rifampicin against not only Mycobacterium tuberculosis strains but also against MAC and Mycobacterium kansasii. (c) 2006 Elsevier Ltd. All rights reserved.

引用

页码：5717 / 5722

页数：6

共 40 条

[1]

[Anonymous], 1976, ANAL PROFILES DRUG S

[2] STEREOSELECTIVE SYNTHESIS OF 4-PIPERIDONE AND 4-AMINOTETRAHYDROPYRIDINE DERIVATIVES BY THE IMINO DIELS-ALDER REACTION OF 2-AMINO-1,3-BUTADIENES [J].

BARLUENGA, J ;

AZNAR, F ;

VALDES, C ;

CABAL, MP .

JOURNAL OF ORGANIC CHEMISTRY, 1993, 58 (12) :3391-3396

[3]

Barluenga JM, 2005, Spanish patent ES, Patent No. [2 246 155 A1, 2246155]

[4]

BARTOLUCCI C, 1992, FARMACO, V47, P1367

[5]

BARTOLUCCI C, 1993, PHARM PHARM LETT, V3, P1

[6]

CANETTI G, 1963, Rev Tuberc Pneumol (Paris), V27, P217

[7] MECHANISM OF INHIBITION OF DNA-DEPENDENT RNA-POLYMERASE OF ESCHERICHIA-COLI BY RIFAMYCINS [J].

CELLAI, L ;

HEUMANN, H ;

BAER, G ;

WEREL, W .

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 1989, 24 (02) :105-110

[8]

DELLABRUNA C, 1983, J ANTIBIOT, V36, P1502

[9] Standard short-course chemotherapy for drug-resistant tuberculosis -: Treatment outcomes in 6 countries [J].

Espinal, MA ;

Kim, SJ ;

Suarez, PG ;

Kam, KM ;

Khomenko, AG ;

Migliori, GB ;

Baéz, J ;

Kochi, A ;

Dye, C ;

Raviglione, MC .

JAMA-JOURNAL OF THE AMERICAN MEDICAL ASSOCIATION, 2000, 283 (19) :2537-2545

[10] Rifamycin-mode of action, resistance, and biosynthesis [J].

Floss, HG ;

Yu, TW .

CHEMICAL REVIEWS, 2005, 105 (02) :621-632

← 1 2 3 4 →