Biomedical subjects

D L Klayman

Publications and source records attributed to D L Klayman.

52 records · Page 3Linked to original sources

PubMed1980

Inhibition of clinically significant bacterial organisms in vitro by 2-acetylpyridine thiosemicarbazones.

Antibacterial activity of 65 2-acetylpyridine thiosemicarbazones and related compounds was determined by using clinical isolates of nine bacterial genera. Minimal inhibitory concentrations (MICs) of 0.002 to 0.062 micrograms/ml were obtained with 23% of the compounds for Neisseria gonorrhoeae and 0.016 to 0.062 micrograms/ml with 17% of the compounds for N. meningitidis. Staphylococcus aureus was inhibited in the MIC range of 0.125 to 0.5 micrograms/ml by 18% of the thiosemicarbazones, whereas 26% inhibited group D enterococcus with an MIC of 0.25 to 2.0 micrograms/ml. Poor antibacterial activity was shown toward the gram-negative bacilli, i.e., Pseudomonas, Klebsiella-Enterobacter, Shigella, Escherichia coli, and Proteus.

Bacteria↗

PubMed1980

Activity of 2-acetylpyridine thiosemicarbazones against Trypanosoma rhodesiense in vitro.

Twenty-seven 2-acetylpyridine thiosemicarbazones and analogs were tested for antitrypanosomal activity against Trypanosoma rhodesiense using a semiautomated in vitro assay system. Activity was determined by relative inhibition of uptake of two radiolabeled macromolecular precursors, [methyl-3H]thymidine and L-[U-14C]leucine, as compared to untreated controls. It was observed that the nitrogen atom of the pyridyl moiety of the 2-acetylpyridine thiosemicarbazones was essential for antitrypanosomal activity. The 2-acetylpyridine thiosemicarbazones generally inhibited the uptake of L-[U-14C]leucine to a greater extent than they inhibited [methyl-3H]thymidine uptake. Twenty-four of the 27 compounds tested exhibited activity comparable to that found for the antitrypanosomal agent ethidium bromide.

Animals↗

PubMed1979

2-Acetylpyridine thiosemicarbazones. 1. A new class of potential antimalarial agents.

Based on the antimalarial properties observed for 2-acetylpyridine 4-phenyl-3-thiosemicarbazone (1), an extensive series of related thiosemicarbazones was prepared and tested against Plasmodium berghei in mice. Screening results indicated that the presence of the 2-pyridylethylidene group was critical and that certain phenyl, benzyl, phenethyl, or cycloalkyl groups at N4 of the thiosemicarbazone moiety also contribute to antimalarial activity.

Animals↗

PubMed1979

Primaquine analogues: derivatives of 4-amino-2-methoxyacridine.

Based on the antimalarial activity of primaquine (1a) and its 4-methyl analogue 1b, 4-aminoacridinyl analogues, 4-[(4-amino-1-methylbutyl)amino]-2-methoxyacridine (2a) and 4-[(4-amino-1-methylbutyl)amino]-2-methoxy-9-methylacridine (2b), were prepared and evaluated as potential tissue schizonticidal agents. These compounds were found to be substantially less active than primaquine against Plasmodium cynomolgi in the rhesus monkey. The antileishmanial activity in hamsters of 4-[[6-(diethylamino)hexyl]amino]-2-methoxy-9-methylacridine (2d) was found to be considerably less than that of 8-[[6-(diethylamino)hexyl]amino]-6-methoxy-4-methylquinoline (1c).

Animals↗

PubMed1973