Theodora Siatra-Papastaikoudi

Synthesis, lipophilicity and biological evaluation of indole-containing derivatives of 1,3,4-thiadiazole and 1,2,4-triazole

3-[(2-Methyl-1H-3-indolyl) methyl]-4-aryl-4, 5-dihydro-1H-1,2,4-triazole-5-thiones 6a-c and their respective N-¿5-[2-methyl-1H-3-indolyl) methyl]-1,3,4-thiadiazol-2-yl¿-N-arylamines 7a,b have been prepared. The antidepressant profile of 6a,c and 7a was studied on mice with respect to that of the analogous 3-(1H-1-indolylmethyl)-4-aryl-4,5-dihydro-1H-1,2,4-triazole-5-thio nes 1a-c and the respective N-¿5-[(2-methyl-1H-3-indolyl) methyl]-1,3,4-thiadiazole-2-yl¿-N-arylamines 2a-c, the synthesis and antimicrobial potency of which we have recently reported. Behavioral effects, induced by the members of both series, in conjunction with their activity in some specific tests (forced swim, pentetrazole convulsions) on mice, show that these derivatives cross the blood-brain barrier and could develop an antidepressant activity comparable to that of imipramine. Blood-brain barrier penetration is also supported by the lipophilicity data obtained for all analogs.

Synthesis of new alkylaminoalkyl thiosemicarbazones of 3-acetylindole and their effect on DNA synthesis and cell proliferation

Summary The preparation of a number of thiosemicarbazones of 3-acetylindole is described. These compounds were evaluated in vitro for their effect on proliferation and cell-division delays in cultured human peripheral blood lymphocytes, and their effect on DNA synthesis in T-cell leukemia Molt-4 cells.

A Critical Appraisal of logP Calculation Procedures Using Experimental Octanol-Water and Cyclohexane-Water Partition Coefficients and HPLC Capacity Factors for a Series of Indole Containing Derivatives of 1,3,4-Thiadiazole and 1,2,4-Triazole

The accumulation of several heteroatoms in hybrid molecules may affect the safe prediction of lipophilicity, while such compounds may differentiate in their hydrogen bonding capability, also important in the manifestation of drug action. The title compounds, which belong to the general types 1,2,3,4 (Figure 1) have shown CNS and antimicrobial activities.1,2 In this study their lipophilicity was investigated and compared to the values obtained by different calculative procedures. Their hydrogen bonding capability was also assessed through the ΔlogP approach.3