Antitrichomonal activity

Vermeersch, H., J. P. Remon, D. Permentier, and E. Schacht. ItSQfto antitrichomonal activity of water-soluble prodrug esters of metronidazdht J. Pharm.60 253-260. 

Antischistosomal activity, of 5-nitro-2-aminothiazoles, 72 Antispasmodic activity, 150, 439 Antitrichomonal activity, 138 of 5-nitro-2-aminothiazoles, 72 Antitubercular activity, 139, 140,441,442 Antitumor activity, 149, 152 Antitussive, 144, 148 Antiulcer properties, 148 Antiviral, 138, 139, 140, 144,438 Appetite depressant, 147 Aprotic solvent, see Solvent effect Aromatic aldehydes, with aminothiazoles, 40... 

Radiosensitizing effect in hypoxic cells [84, 91, 123—126], in normal tissue [123] toxicity to hypoxic cells [112, 113, 115, 116, 124, 125, 127], toxicity in vivo [128] antimicrobial drugs (effect on single- or double-stranded DNA Escherichia coli) [112] antiprotozoan, antibacterial (Salmonella typhimurium cells [123] and antitrichomonal activity [128, 129]) inhibition of ribonucleotide-reductase [130] structure—activity [115, 116, 127]... 

Radiosensitizing effect in hypoxic cells [89] toxicity to hypoxic cells [102, 112, 115, 116] DNA damage [112], antitrichomonal activity [137], structure-activity [115, 116] inhibition of T. cruzi growth at concentrations that do not stimulate 0 and H202 production (reduced metabolites of benznidazole are involved through covalent binding to macromolecules in its trypanocidal and toxic effects) [133]... 

Radiosensitizing effect in hypoxic cells [151], toxicity to hypoxic cells [103, 115, 116, 151], toxicity in vivo [103], DNA damage [103,118,151], antitrichomonal activity [103], prevention of histomoniasis in turkeys [152, 153] and ocular hypertension, ischemia [154], structure—activity [115, 116] Antimicrobial effect, inhibition of purine biosynthesis [155]... 

Toxicity in hypoxic cells, toxicity in vivo, DNA damage, antitrichomonal activity [103]... 

Like nitrofurans, the compounds of this class have been found to possess a wide-spectrum of antiparasitic activity. The first compound which exhibited potent antitrichomonal activity is entramin (13) [13]. Acylation of entramin gave a number of active compounds the most effective compound was 2-acetylamino-5-nitrothia-zole (acinitrazole, 14). This compound exhibited high in vitro and in vivo activity against Trichomonas vaginalis and T. foetus in animals, but did not prove to be of value in clinical trials [13-16]. Acinitrazole has, however, been found to be effective against intestinal amoebiasis in rats and dogs [13]. 

In the first edition it was reported that compounds of these series were useful as coronary dilators and ulcer inhibitors. Similar claims have also been made for different compounds with (186) reported to be a potent coronary dilator <8lMl 8l0-0l> and (187) to be useful in the treatment of ulcers <81USP4289697>. In addition, analgesic activity has been shown for (188) <81BRP1588166> and potent in vitro antitrichomonal activity demonstrated for (189). Unfortunately in vivo activity was not comparable and the compounds were generally too toxic to be useful <85JMC1673>. 

Most papers referred to in this section are concerned with cocaine. N-Demethyl-ation of C-labelled cocaine in isolated hepatocytes was monitored in vivo by measuring the exhalation of CO2. A summary paper on the pharmacology of cocaine has appeared. Furylglyoxylic esters of the tropine type (35) have been synthesized and screened for antiamoebic, antiprotozoal, and antitrichomonal activities. 

Loiseau, P. M. Bories, C. Sanon, A. A new photometric assay with bromocresol purple for testing in vitro antitrichomonal activity in aerobic environment. Arzneim.-Foracfi. 1999, 49, 51-55. 

In a series of thirty four 2-amino -5-nitrothiazoles good in vitro antitrichomonal activity was found in 12 but in vivo against T. vaginali s in mice none was more than 1/4 as potent as metronidazole. 

Strips cut into 4-cm sections and exposed to ethylene oxide vapors for 1 h. Each section dropped into a tube containing 10 ml Trichomonas vaginalis culture containing 10 cell /ml. After incubation at 37 C for 48 h, cells counted on a hemacytometer. Low counts indicated antitrichomonal activity... 

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