Synthesis, spectrometric characterization and trypanocidal activity of some 1,3,4-thiadiazolines derivatives

Abstract

Six 1,3,4-thiadiazolines derivatives were synthesized by cyclization of thiosemicarbazones under acetylating condition with yields going from 27 to 94%. The products purity was confirmed by LC/MS (Mass Spectrometry Coupled with High-Performance Liquid Chromatography) and they were characterized using spectrometry IR, NMR 1 H and 13 C (Nuclear Magnetic Resonance). These compounds were then tested in vitro on Trypanosoma brucei brucei according to the "LILIT, Alamar Blue" method to estimate their trypanocidal activity. 1,3,4-thiadiazoline 6 (IC 50 = 38,79 µM) was the most active of all compounds.

Antiparasitic Constituents of Beilschmiedia louisii and Beilschmiedia obscura and Some Semisynthetic Derivatives (Lauraceae)

“…Based on these data, compound 11b was concluded to be a new aldehyde derivative to which the trivial name beilschmiedal (Figure 1) was given. The derivatization of compound 11b with thiosemicarbazide reagent [23] led to compound 11c (Scheme 1) as a white amorphous powder. The molecular formula of 11c, C 23 H 35 N 3 S, with eight degrees of unsaturation, was deduced from its NMR data and the high-resolution electrospray ionization (HRESIMS; Figure S10), which showed the protonated molecular ion peak [M + H] + at m/z 386.2658 (calcd for C 23 H 34 N 3 S, 386.2624).…”

Physical and Spectral Characterization of Ni (II) Cu(II) Co(II) and Cd(II) Complexes with Schiff Base of Salicylaldehyde and 2-Aminopyridine Towards Potential Microbial Application

“…The in-vitro evaluation of antimicrobial activities was performed according to the diffusion technique [13]. The bacteria were grown in nutrient broth at 37°C for 24 hours according to the previous literatures [41,42]. The complexes were tested using diffusion on solid media.…”

3D Series Metal Complexes Containing Schiff Base Ligand with 2,2'-Bipyridine: Synthesis, Characterization and Assessment of Antifungal Activity

“…Metal complexes of thiosemicarbazones have been explored for nearly 50 years because of their versatile biological activity and prospective use as drugs [1]. Owing to the interest they generate through a variety of biological properties, thiosemicarbazones metal complexes have been employed in medicinal applications ranging from anticancer [2], antitumor [3], antifungal [4,5], antibacterial [6], antmalarial [7,8], antitilarial, [9], antiviral [10,11], antineoplastic [12,13], antileprotic [14], trypanocidal [15,16] and anti-HIV activities [17]. It has been proved that thiosemicarbazones block DNA synthesis in mammalian cells by inhibiting the enzyme, ribonucleoside diphosphate reductase, presumably either via chelation with iron(III) required by the enzyme or because a preferred metal chelate of the inhibitor interacts with the target enzyme [18,19].…”