Nitroimidazoles are characterized by a wide range of biological activity and many them used as therapeutics. Moreover, some bicyclic nitroimidazooxazoles show considerable potency against Mycobacterium tuberculosis. Some authors noticed that in the case chiral derivatives nitroimidazodihydrooxazoles, (R) form shows greater tuberculostatic than (S) enantiomer. This work describes procurement new...

Making use of the extended kinetic method and the alternative method for data analysis, we have experimentally determined ΔH°acid (kcal/mol) for six mononitrated azole species (2-nitropyrrole = 337.0, 3-nitropyrrole = 335.8, 3-nitropyrazole = 330.5, 4-nitropyrazole = 329.5, 2-nitroimidazole = 327.4, and 4-nitroimidazole = 325.0). We report an absolute uncertainty of ±2.2 kcal/mol that arises fr...

A rapid liquid chromatography-mass spectrometric method for the determination of five nitroimidazoles in water from different sources is described. The extraction procedure was based on HLB solid-phase extraction with acetonitrile followed by an evaporation step. Ternidazol, another nitroimidazole, was used as the internal standard. The liquid chromatographic separation was made on a C18 bonded...

Metronidazole (Mz)-resistant Giardia and Trichomonas were inhibited by 1 of 30 new 5-nitroimidazole drugs. Another five drugs were effective against some but not all of the Mz-resistant parasites. This study provides the incentive for the continued design of 5-nitroimidazole drugs to bypass cross-resistance among established 5-nitromidazole antiparasitic drugs.

reaction of readily available 2-formyl -1-methyl-5-nitroimidazole (1) with 4-substituted-2-hydrazinothiazoles (2) afforded 2-formyl-l-methyl-5- nitroimidazole 4-substituted -2- thiazolylhydrazones (3). reaction of thiochromitn-4-one (4) with thiosemicarbazide gave thiochroman-4- one thiosemicarbazone (5). reaction of compound 5 with clc- haloaldehyde or ketones y ielded thiochroman--#-one 4-sub...

In continuation of our research program to develop original synthetic methods using TDAE methodology on nitroheterocyclic substrates, we were able generate for the first time a stable carbanion in position 2 5-nitroimidazole scaffold. Starting from 2-chloromethyl-4-phenylsulfonylmethyl-5-nitroimidazole intermediate, prepared by vicarious nucleophilic substitution hydrogen (VNS) reaction, select...

Starting from 2-(2-pyridyl) imidazole a series of substituted imidazoles (2-5) were prepared. From the reaction of 2-(3-pyridyl) -4-(or 5) nitroimidazole (15) with dimethyl sulfate in alkaline medium 1-methyl-2-(3- pyridy1)-4-nitroimidazole (6,)w as prepared. Reaction of compound 15 with diazomethane gave I-methyl-2-(3-pyridy1)-5- nitroimidazol(e7 ) in addition to 6. The antibacterial and an...

A method for the synthesis of N-aryl-C-nitroazoles is presented. A coupling reaction between variously substituted arylboronic acids and 3(5)-nitro-1H-pyrazole catalyzed by copper salt has been carried out in methanol in the presence of sodium hydroxide to afford the desired N-aryl-C-nitroazoles in good yields. This synthetic route has also been successfully applied to obtain N-phenyl derivativ...

Hypoxia has been known be an important physiological parameter for tumor growth and has been reported to be the cause for poor response to chemotherapy. Mechanistically, tumor hypoxia results from an imbalance between oxygen delivery and oxygen consumption. The identification and quantification of tumor hypoxia may predict the out come and may identify patients who might benefit from concomitan...

Tritrichomonas foetus KV(1), a nitroimidazole-susceptible strain, and KV(1)/M100, its nitroimidazole-resistant daughter strain, differed markedly in their in vivo susceptibility to metronidazole. In vitro susceptibility testing in multiwell plates and tubes with different trichomonad media containing no, or low concentrations of, ascorbate demonstrated that the resistant strain behaves like the...