I. The Pharmacology of No. 48-80, a Long-Acting Vasodepressor Drug. Peter B. Dews, A. Lloyd Wnuck, R. V. Fanelli, Amos E. Light, John A. Tornaben, Stata Norton, C. H. Ellis and Edwin J. De Beer 1 II. Studies on the Relationship of Metabolic Fate and Hormonal Effects of d,l-Methadone to the Development of Drug Tolerance. Chen-Y#{252} Sung, E. Leong Way and Kenneth G. Scott 12 III. The Action of ...

Reaction of 3,4,5,6-tetrahydro-2-pyrimidinethiol, prepared by cyclocondensation reaction of 1,3-diamino propane 1 and carbon disulfide, with ethyl chloroacetate and substituted aromatic aldehydes in the presence of sodium acetate and acetic acid gave 2-[(Z)-1-(aryl)]-6,7-dihydro-2H-isothiazolo[2,3-a]pyrimidine-3(5H)-one derivatives 3(a-j) in good yields. 1H-NMR spectroscopy, and elemental analy...

A new tetra-dentate chiral Schiff base ligand, C(26)H(30)N(2)O(2), has been synthesized by the reaction of 1-phenyl-butane-1,3-dione with (1S,2S)-(-)-1,2-diamino-cyclo-hexane. The chiral centers in the mol-ecule have the same S configuration, since the absolute configuration was determined by that of the starting reagent (1S,2S)-(-)-1,2-diamino-hexane. The cyclo-hexane ring is in a chair confor...

In the title compound, C(9)H(8)Cl(2)N(5) (+)·H(2)PO(4) (-)·C(9)H(11)NO [systematic name: 3,5-diamino-6-(2,3-dichloro-phen-yl)-1,2,4-triazin-2-ium dihydrogen phosphate-4-(dimethyl-amino)-benz-alde-hyde (1/1)], inter-molecular N-H⋯O and O-H⋯O hydrogen bonds produce R(2) (2)(8) and R(3) (2)(8) rings, generating a layer. Inter-molecular N-H⋯N inter-actions also occur. The dihedral angle between the...

Seven pyrimidines with a lipophilic substituent at position 5 have been investigated with respect to inhibition of both dihydrofolate reductases of Sarcoma 180 and Escherichia coli and site of inhibitory action in mammalian cells in culture. Of the 7 pyrimidines, 5 were competitive inhibitors of both dihydrofolate reductases, 1 was noncompetitive, and 1 produced no effect. The Sarcoma 180 enzym...