The rate and equilibrium constants for the formation of a number of metmyoglobin species Mb+X (X = imidazole, imidazole-H-, 1-methylimidazole, 2-methylimidazole, 4-6 troimidazole, 2-methyl-5-nitroimidazole, pyridine, 2-, 3-, and 4-picoline) and the rates of their reduction by dithionite have been measured at 25”. Several different kinds of kinetic behavior for the reduction were observed. In al...

Bioavailability File: Metronidazole Summary Metronidazole is an antimicrobial nitroimidazole derivative, which was originally introduced to treat Trichomonas vaginalis but nowadays is used for the treatment of anaerobic and protozoal infections. Metronidazole is bactericidal through toxic metabolites, which cause deoxyribonucleic acid (DNA) strand breakage. It has a bioavailability of more than...

two series (a and b) of n- substituted heteroaromatic compounds related to clotrimazole were synthesized. imidazole ring of the clotrimazole was replaced by 2-methylimidazole in series a, and by 2-methyl-4-nitroimidazole in series b. o-cholortrityl moiety of clotrimazole was also replaced by trityl, mono or dimethoxy trityl. chemical structures of all the new compounds were confirmed by spec-tr...

the 1,4-dihydropyridine (dhp) derivatives are a known class of calcium channel blockers. some derivatives of dhp showed significant cytotoxicity. it was shown that this effect may not be the result of interaction with ca2+ channels. in this study, we performed an investigation about the intrinsic cytotoxicity of some derivatives of dhp containing nitroimidazole moiety on their c4 position on fo...

Tuberculosis (TB) remains a significant cause of death worldwide, and emergence of drug-resistant TB requires lengthy treatments with toxic drugs that are less effective than their first-line equivalents. New treatments are urgently needed. Delamanid, previously OPC-67863, is a novel drug of the dihydro-nitroimidazole class with potent anti-TB activity and great promise to be effective in the t...

D IMETRIDAZOLE (1,2-dimethyl-5-nitroimidazole) 2 is presently used in the United States and Canada for the prevention and treatment of histomoniasis in poultry. A stimulatory effect of dimetridazole on the growth of chickens and turkeys has been reported by Condren et al. (1963), Lucas (1963) and McGuire et al. (1964). In addition, dimetridazole has an inhibitory effect on the growth of certain...

The 1,4-dihydropyridine (DHP) derivatives are a known class of calcium channel blockers. Some derivatives of DHP showed significant cytotoxicity. It was shown that this effect may not be the result of interaction with Ca(2+) channels. In this study, we performed an investigation about the intrinsic cytotoxicity of some derivatives of DHP containing nitroimidazole moiety on their C4 position on ...

For 10 years vaginal trichomoniasis has been treated by oral chemotherapy. Some cases appear not to respond satisfactorily to the drug used, and it is important to know whether or not the patient is taking the drug, and if so, whether or not it is being absorbed from the alimentary tract. A simple method for detecting these drugs in urine may be of use in such cases. Two antitrichomonal drugs i...

Cocrystallization of 1-hydroxy-ethyl-2-methyl-5-nitroimidazole (metronidazole) and 5-sulfosalicylic acid (5-H(2)SSA) from methanol solution yields the title salt, C(6)H(10)N(3)O(3) (+)·C(7)H(5)O(6)S(-). In the crystal structure, the ions are linked by a combination of inter-molecular O-H⋯O, N-H⋯O and C-H⋯O hydrogen bonds, forming a three-dimensional framework. The hydroxyl group of the cation i...

We investigated the in vitro action of an hydrosoluble 2-nitroimidazole, Etanidazole (EZL), against Trypanosoma cruzi, the etiologic agent of Chagas disease. EZL displayed lethal activity against isolated trypomastigotes as well as amastigotes of T. cruzi (RA strain) growing in Vero cells or J774 macrophages, without affecting host cell viability. Although not completely equivalent to Benznidaz...