University of Saskatchewan

University of Texas System

Wayne State University

Jonathan R Dimmock

Umashankar Das

Rosa Maldonado

Miguel A Vasquez

Elias K Manavathu

Embodiments are directed to compositions and methods for treating parasitic infections. Compounds have been identified from a library of anti-cancer drugs that serve as suitable agents for targeting trypanosomatids.

Antiparasitic effect of Bis[3,5-Bis(Benzylidene)-4-Oxo-1-Piperidinyl]amide Derivatives

The present invention relates to 4-piperidone derivatives represented by the following formula (I) and the acid addition salts thereof. The method of preparation and antineoplastic activity of the said compounds are disclosed. A number of the compounds possess submicromolar ICand CCvalues and have a selective toxicity for colon cancers and leukemic cells. In addition, many of the compounds are able to reverse multidrug resistance.

Antineoplastic compounds

Mannich bases of conjugated styryl ketones have been developed which are effective as cytotoxicity and anticancer agents, and which also have antifungal activity. Preferred compounds are those of the formula ##STR1## where R.sub.1 is Cl, CH.sub.3 or OCH.sub.3 and R.sub.2 is H or Cl. A compound of particular interest is (3-[3-(4-chlorophenyl)-2-propenoyl]-4-[2-(4-chlorophenyl)vinylene]-1-ethyl -4-piperidinol hydrochloride.

Mannich bases of conjugated styryl ketones

A compound of general formula I below useful as an anticonvulsant for disorders of the central nervous system: ##STR1## wherein: R.sup.1, R.sup.2, R.sup.3 and R.sup.4 may be the same or different and each represents a hydrogen or halogen atom, or a C.sub.1-9 alkyl, C.sub.3-9 cycloalkyl, cyano, C.sub.1-9 alkoxy or C.sub.6-10 aryloxy group; R.sup.5 represents a hydrogen atom or a C.sub.1-9 alkyl, C.sub.3-9 cycloalkyl or C.sub.6-10 aryl group; and X is oxygen or sulfur; or a pharmaceutically-acceptable salt thereof. The compound may be adimistered orally for treating convulsions in humans or animals.

Growing community of inventors

Saskatoon, Canada

Jonathan R Dimmock