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Three series of 4,6-dimethoxy-, 4,6-dipiperidino-and 4,6-dimorpholino-1,3,5-triazin-2-yl) amino acid derivatives were synthesized and characterized. A preliminary study for their monoamine oxidase inhibitory activity showed that compounds 7, 18, and 25 had MAO-A inhibition activity comparable to that of the standard clorgyline, with apparently more selective inhibitory activity toward MAO-A than MAO-B and no significant acute toxicity.

A library of short di-, tri-, and tetra-peptides with an s-triazine moiety at the N terminus and either an amide or ethyl ester C terminus was prepared in solution and on the solid phase. The two remaining positions of the s-triazine moiety were substituted with methoxy, morpholino, or piperidino groups. All the synthesized peptide derivatives were analyzed by HPLC and fully characterized by IR spectroscopy, H and C NMR spectroscopy, elemental analysis, and mass spectrometry (MALDI TOF/TOF). A preliminary study of the antileishmanial activity of the 1,3,5-triazinyl peptide derivatives revealed that four dipeptide amide derivatives showed higher antipromastigote or antiamastigote activity than the reference standard drug miltefosine with no significance acute toxicity.

A series of novel cyano oximino sulfonate derivatives were prepared from the reaction of arylsulfonyl chloride with different cyanoacetamide-based oximes ranging from the simplest unsubstituted amide to analogues containing N-ethyl (mimicking the Oxyma template), N-piperidinyl and N-morpholinyl chains. In addition, the cyano oximes, N-hydroxybenzimidoyl cyanide and N-hydroxypicolinimidoyl cyanide were also used in the synthesis of the novel cyano oximino sulfonate derivatives. The structures of the prepared compounds were confirmed by 1 H-NMR, 13 C-NMR, and elemental analysis. The preliminary bioassays showed that some of the title compounds, such as 2-oxo-2-(piperidin-1-yl)-N-(tosyloxy)acetimidoyl cyanide (TsPipOx), N-(tosyloxy)benzimidoyl cyanide (TsPhOX), N-(naphthalen-2-ylsulfonyloxy)-2-oxo-2-(piperidin-1-yl)acetimidoyl cyanide (NpsPipOx), 2-amino-N-(naphthalen-2-ylsulfonyloxy)-2-oxoacetimidoyl cyanide (NpsAmOx), N-(naphthalen-2-ylsulfonyloxy)benzimidoyl cyanide (NpsPhCN), and N-(naphthalen-2-ylsulfonyloxy)picolinimidoyl cyanide (NpsPyCN), showed anti-proliferation effect on the mouse fibroblast L929. The calculated IC 50 -values were ranging between 36.5 µg/mL and 0.235 mg/mL. However the anti-proliferation effects seem to be cytostatic rather than cytotoxic. The compounds only minimize the growth activity without completely killing the cells.Key words phenylsulfonate; naphthylsulfonate; oxime; anti-proliferation; 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide assay (MTT-assay) Oximes are one of the most versatile building blocks in organic and organometallic chemistry. The substituent pending at α-position account for the specific properties of each oxime, such as dissociation constant, solubility, chelating ability, etc.1-3) Their multifaceted nature derives in a broad range of applications in chemistry in addition to be biologically relevant moieties. 4-7)Biologically active heterocyclic compounds containing amine moiety, specifically piperidine and morpholine skeletons are attractive targets of organic synthesis owing to their pharmacological activity and wide occurrence in nature. 8,9) Piperidines are known to have central nervous system (CNS) depressant activity at low dosage levels but stimulant activity with increased doses. In addition, the piperidine skeleton possesses analgesic, ganglionic blocking and anesthetic properties.10,11) Morpholine derivatives have been reported to possess antiinflammatory [12][13][14] antimicrobial 15,16) and central nervous system activities. 17,18)The sulfonate ester is considered an important class in the sulfonylation reaction for the synthesis of sulfonamide which exhibits a wide range of biological activities. [19][20][21][22] Sulfonylation is also used as a protection technique for OH and NH functionalities, as it enables crystallization and the protecting group can be selectively cleaved in the presence of acid-labile tert-butyl-based groups by using HCl or HBr in alcohol 23) or in aprotic solvents such as ethylacetate or dimethylformamide. 24,...

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