The title compounds were prepared by acylation of piperazine with maleic acid ester chlorides in methylene chloride medium in the presence of K2CO3. In preliminary screening some of them showed marked antimitotic activity on plant materials.

Acylation↗

PubMedDate not supplied

Synthesis and effect of asymmetric 1,4-bis(aminoacyl) piperazines on neuromuscular transmission.

The condensation of asymmetrically substituted 1,4-bis(haloacyl) piperazines with secondary amines yielded asymmetric 1,4-bis (aminoacyl) piperazines 3-6, which were further transformed into the respective dimethiodides 3b-6b by treatment with methyl iodide. Those compounds were found to inhibit the neuromuscular transmission by blocking the motor end-plate receptors. Compounds containing piperidine moiety and branched acyl chain 4b displayed enhanced activity.

Acetylcholine↗

PubMedDate not supplied

Synthesis and antileukemic properties of 2-methyl and 2,5-dimethylpiperazides.

New piperazides 1-15 were synthesized as analogues of an agent active against Leukemia 1210, 4.4'-(2-methyl-1,4- piperazinediyl )-bis-(4-oxo)-2- butenoic acid diethyl ester, NG (NSC 337310). The piperazides were synthesized by treatment of 2-methyl or 2,5-dimethyl-piperazine with maleic acid ester chlorides in CH2Cl2 or in aqueous medica in the presence of anhydr . K2CO3 . The influence of compound NG (NSC 337310) and several new derivatives on P 388 Lymphocytic Leukemia was tested: only compound NG have demonstrated a satisfactory activity.

Animals↗

PubMedDate not supplied

Pyridazino[1,2-a] 1,2,5-triazepines.

By the condensation of 1,2-di(chloracetyl)piperidazine with primary amines 3-substituted derivatives of 1,5-diketoperhydropyridazino[1,2-a] 1,2,5-triazepine (1--8, Fig. 1) were obtained. Some of them show sedative action at the 25--100 mg/k dosis level and are of low ip toxicity.

Animals↗