Antifilarial agents

Perhydropyrazino[l,2-c]pyrimidincs were all synthesized by formation of the pyrimidine ring. The antifilarial agent, Centperazine, 166, was built from [6+0] fragments by bond formation a to the ring junction nitrogen (Scheme 21). Compound 165 was prepared in two steps from 2-vinylpyrazine and the yield over five steps was 23% < 1998IJB1149>. 

Benzimidazoles have been identified as antifilarial agents [1-5] based on an extensive series of studies in jirds (a kind of gerbil) and cats. The mechanism of action of benzimidazoles has been extensively studied in many laboratories and, in general, three possible modes of action have been suggested for these drugs. 

The proton chemical shifts of 2-organyl-5(6)-nitrobenzimidazoles [712, 713], mono- and polysubstituted nitrobenzimidazoles [714], 2-benzyl derivatives of 5(6)-nitrobenzimidazoles as potential antifilarial agents [715], l-substituted-2-methyl-5-nitrobenzimidazoles [716], mono- and dinitro-substituted 2-alkylbenzimidazoles... 

A dithiocarbamate antifilarial agent and its active isothiocyanate derivative in biological fluids were analysed by HPLC. ... 

Kumar Y, Green R, Borysko K. Z, Wise D. S, Wotring L. L, Townsend L. B. Synthesis of 2,4-disubstituted thiazoles and selenazoles as potential antitumor and antifilarial agents. 1. Methyl 4-(isothiocyanatomethyl)thiazole-2-carbamates, -selenazole-2-car-bamates, and related derivatives, J. Med. Chem. 1993. p. 3843 - 3848. DOI 10.1021/ jm00076a012... 

Rao, U.R., Mehta, K., Subrahmanyam, D. and Vickery, A.C. (1991) Brugia malayi and Acanthocheilonema viteae- antifilarial activity of transglutaminase inhibitors in vitro. Antimicrobial Agents and Chemotherapy 35, 2219-2224. 

Antiemetic drugs, 27 (1990) 297 Antifilarial benzimidazoles, 25 (1988) 233 Antifolates as anticancer agents, 25 (1988)... 

Following the discovery of antileishmanial and antifilarial activities of tartar emetic [3], a number of organoantimonials were prepared as possible antiparasitic agents. 

Recent studies evaluated Sesamum indicum L., sesame (Pedaliaceae) gum for its useful properties in the drug industry as a binder/hydrophilic polymer in the formulation of sustained release paracetamol granules and tablets, compared with standard binders Arabic gum, gelatin, and sodium carboxymethylcellulose [277] for the intestinal delivery of antifilarial drug diethylcarbamazine tablets [278] as an accessible, cost-effective and eco-friendly suspending agent in a pediatric pharmaceutical suspensions, compared with Arabic gum and tragacanth [279]. 

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