Purine Analogues as Amplifiers of Phleomycin. VI. The Synthesis and Metabolism of Some Benzothiazole, Benzoxazole and s-Triazolopyrimidine Amplifiers

1979 ◽  
Vol 32 (12) ◽  
pp. 2727 ◽  
Author(s):  
DJ Brown ◽  
Y Iwai
Keyword(s):  
Escherichia Coli ◽  
In Vitro Cultures ◽  
Purine Analogues

The metabolisms of four 14C-tagged amplifiers of phleomycin are followed in mice. 2-(Benzothiazol- 2'-ylthio)acetamide (1c) gives mainly the corresponding acid (1e) in the urine; 2-(benzoxazol-2'- ylthio)acetamide (1d) likewise gives the acid (1f); N-methyl-2-(s-triazolo[4,3-a]pyrimidin- 3'-ylthio)propionamide (2b) gives unchanged material (c. 20%) plus not the corresponding acid (2c), but its [1,5-a] isomer (3c) in 60% yield; and 2-(5',7'-diethyl-s-triazolo[4,3- a]pyrimidin-3'-ylthio)-acetamide (2i) proves much more stable by giving mainly unchanged material (>60%). Minor metabolites are formed in each case. ��� Syntheses and N.M.R. spectra of the above substrates and related derivatives are reported as well as their activities as amplifiers of phleomycin against in vitro cultures of Escherichia coli.

Purine Analogues as Amplifiers of Phleomycin. V. Thioethers of Several Heterocyclic Systems with One or Two Rings

1979 ◽  
Vol 32 (12) ◽  
pp. 2713 ◽  
Author(s):  
DJ Brown ◽  
GW Grigg ◽  
Y Iwai ◽  
KN McAndrew ◽  
T Nagamatsu ◽  
...  
Keyword(s):  
Escherichia Coli ◽  
Biological Activities ◽  
In Vitro Cultures ◽  
Purine Analogues

Thioethers, appropriate for testing as amplifiers of phleomycin against in vitro cultures of Escherichia coli, are prepared via corresponding thiones in the purine, imidazo[4,5-b(and 4,5-c)]pyridine, pyrazolo[3,4-d]pyrimidine, quinazoline, benzothiazole, benzoxazole, pyrimidine, imidazole, thiazoline, 1,2,4-triazole, s-triazolo[4,3-c(and 1,5-c)]pyrimidine, oxazolo[4,5-b]pyridine, quinoline and 1,3,5-triazine series. Structures are confirmed by N.M.R. spectra. Biological activities are tabulated and discussed in terms of structure.

Purine analogues as amplifiers of phleomycin. III. Some 2-alkylthio derivatives of imidazole, benzimidazole, benzoxazole and benzothiazole

1978 ◽  
Vol 31 (2) ◽  
pp. 447 ◽  
Author(s):  
DJ Brown ◽  
WC Dunlap ◽  
GW Grigg ◽  
L Danckwerts
Keyword(s):  
Escherichia Coli ◽  
Maximal Activity ◽  
Purine Analogues ◽  
Derivatives Of

Some 2-methylthio and 2-carbamoylalkylthio derivatives of 1-methylimidazole, benzimidazole, benzoxazole, benzothiazole and 6-dimethylaminobenzothiazole have been synthesized by alkylation of the corresponding thiones. Their in vitro activities, as amplifiers of phleomycin against Escherichia coli, varied from slight to high but none was outstanding. 2-(Benzothiazol-2'-ylthio)acetamide (2j)showed maximal activity at c. 0.04 mM with progressive decreases at both higher and lower concentrations.

Unfused heterobicycles as amplifiers of phleomycin. I. Some pyridinyl- and pyrazolyl-pyrimidines, bithiazoles and thiazolylpyridines

1980 ◽  
Vol 33 (10) ◽  
pp. 2291 ◽  
Author(s):  
DJ Brown ◽  
WB Cowden ◽  
GW Grigg ◽  
D Kavulak
Keyword(s):  
Escherichia Coli ◽  
Biological Activities ◽  
In Vitro Cultures ◽  
Derivatives Of

Syntheses are reported for some simple derivatives of 2-(pyridin-2'- yl)pyrimidine; 4-(pyrazol-1'- yl)pyrimidine; 4-(pyrazol-4'- yl)pyrimidine; 4,5'-bithiazole; 2-, 3-, and 4-(thiazol-4'-yl)pyridine and 2-, 3-, and 4-(thiazol-2'-yl)pyridine. Biological activities, as amplifiers of phleomycin against in vitro cultures of Escherichia coli, are tabulated and discussed.

Lignans from in vitro cultures of transgenic roots of Taxus x media var. Hicksii

Planta Medica ◽  
2012 ◽  
Vol 78 (11) ◽  
Author(s):  
K Sykłowska-Baranek ◽  
A Pietrosiuk ◽  
M Grech-Baran ◽  
M Bonfill ◽  
P Mistrzak
Keyword(s):  
In Vitro Cultures ◽  
Transgenic Roots ◽  
Taxus X Media

Phenolic compounds from in vitro cultures of Rindera graeca Boiss. & Feldr.

Planta Medica ◽  
2013 ◽  
Vol 79 (13) ◽  
Author(s):  
K Sykłowska-Baranek ◽  
A Pietrosiuk ◽  
K Graikou ◽  
H Damianakos ◽  
M Jeziorek ◽  
...  
Keyword(s):  
Phenolic Compounds ◽  
In Vitro Cultures

HPTLC determination of catechins in in-vitro cultures of two species of the genusPhyllanthus

2008 ◽  
Vol 21 (2) ◽  
pp. 103-106 ◽  
Author(s):  
Barbara Sparzak ◽  
Mirosława Krauze-Baranowska ◽  
Loretta Pobłocka-Olech
Keyword(s):  
In Vitro Cultures
Sign in / Sign up

Export Citation Format

Share Document