A new series of nortopsentin analogues, in which the imidazole ring of the natural product was replaced by thiazole and the indole unit bound to position 2 of the thiazole ring was substituted by a 7-azaindole moiety, was efficiently synthesized. Two of the new nortopsentin analogues showed good antiproliferative effect against the totality of the NCI full panel of human tumor cell lines (~60) ...

In Salmonella typhimurium, thiamine is a required nutrient that is synthesized de novo. Labeling studies have demonstrated probable precursors for both the 4-amino-5-hydroxymethyl-2-methylpyrimidine pyrophosphate moiety and the 4-methyl-5-(beta-hydroxyethyl) thiazole monophosphate moiety. The isolation of thiamine auxotrophs with mutations in at least five different genetic loci is reported. Th...

Starting from epothilone A±D (1a±2b) obtained by large scale fermentation of the myxobacterium Sorangium cellulosum the thiazole side-chain was extensively modi®ed by substitution, oxidation and replacement. Metallation afforded the C-19 carbanion 4 which was quenched by various carbon and heteroatom electrophiles to give C-19 substituted epothilones 5. Thiazole N-oxides 9 were obtained by trea...

A series of four donor aryl alkynyl substituted thiazole derivatives 3a-d and three similar aryl donor-acceptor systems 6a-c have been synthesized. All compounds bear different electron-donating groups in the 5-position of the thiazole core. The influence of both electron donor strength and the additional phenylethynyl unit on photophysical properties, i.e. UV/Vis absorption, fluorescence emiss...

The 2-aminothiazole series has anti-bacterial activity against the important global pathogen Mycobacterium tuberculosis. We explored the nature of the activity by designing and synthesizing a large number of analogs and testing these for activity against M. tuberculosis, as well as eukaryotic cells. We determined that the C-2 position of the thiazole can accommodate a range of lipophilic substi...

Two independent methods for quantitating reticulocyte counts were compared. One used a modified thiazole orange technique and a flow cytometer (Becton Dickinson FACS); the other was a fully automated whole blood analyser (Sysmex R1000). Both methods gave comparable results with a coefficient of variation of less than 5%. Samples measured using the R1000 showed a negligible decrease in the retic...

Solutions of 5-N-arylaminothiazoles containing pyridyl groups exhibited clear halochromism and halofluorism upon addition of Brønsted and Lewis acids. The addition of triflic acid to solutions of 5-N-arylaminothiazoles in Et2O induced bathochromic shifts of the absorption and emission bands. DFT calculations suggested that the spectral changes arise from the protonation of the pyridyl group of ...

New thiazole hybrids were synthesized and evaluated for their in vitro cytotoxicity against a panel of human malignant cell lines. The key steps the synthesis 3?7 involved initial condensation appropriate aldononitriles with cysteine ethyl ester hydrochloride, followed by subsequent treatment resulting thiazolines diazabicycloundecene to form ring. Bioisosteres 8 14 have been prepared after ste...

Kauçuk, hem doğal yollarla elde edilen, de petrol ve alkolün bileşiminden suni olarak edilebilen bir malzeme olup üzerine belirli kuvvet uygulanıp bırakıldığında eski konumuna dönen malzemeler için kullanılan terimdir. Kauçuk yapısal yapışkanlık içermektedir ancak vulkanizasyon prosesi ile azaltılıp, kuvvetli mekanik değerlere sahip olmaktadır. Vulkanizasyon en metot olan kükürt çok tercih edil...