No abstract

Forty-two analogues and reaction products derived from T-2 toxin or neosolaniol were assayed for their cytotoxicity to cultured mouse lymphoma cells. Structure-activity relationships confirmed the stereospecific nature of the cytotoxic action of T-2. Cytotoxicity was particularly susceptible to changes at C3, C4, C9, and C10 but was relatively unaffected by changes at C8, which appears to represent a region of steric tolerance in the interaction of T-2 with a cellular constituent. The most potent compounds were T-2, diacetoxyscirpenol, and a series of C8 ester analogues 11 and 31-35.

The synthesis of the title compound (10) in eight stages is described. A procedure for the reductive acylation of a pyridyl nitro-group is presented. The use of rhodium as a catalyst for nuclear reduction of pyridines in aqueous solution a t room temperature is discussed and examples of this procedure are given. N.m.r. data are presented for a number of 2,5-disubstituted pyridines and piperidines and the formation (and n.m.r. spectrum) of 2 3-bis-(5-nitro-2-pyridyl) butane ( 6) in the preparation of 1 -(5-nitro-Z-pyridyI)acetaldehyde oxirne (4) is reported.

. Several 1‐ and 2‐substituted, and 1,2‐disubstituted, 1,4,5,6‐tetrahydropyrimidines have been prepared and their toxicological and pharmacological properties have been investigated. . In general the compounds were neuromuscular blocking agents with the monosubstituted members of the series showing a depolarizing type of activity and the disubstituted compounds a non‐depolarizing type. . The toxicity to mice of some of the monosubstituted compounds was increased by pretreatment of the animals with SKF 525A, but the toxicity of the disubstituted compounds was unaffected. . The results obtained with these compounds are not at variance with a suggestion made previously that nicotinic action at the neuromuscular junction can result from an interaction between drug and receptor at two points separated by about 4 Å.

Dimethyl sulphate (2.85 nil., 3-68 g.) was added dropwise to a stirred solution of l-acetyl-5-hydroxyindoline (6.3 g.) in N-sodium hydroxide (40 ml.), the temperature of the mixture being kept a t 40". On 111. p. 203-205'.