Synthetic thiosemicarbazones as a new class of Mycobacterium tuberculosis protein tyrosine phosphatase A inhibitors

Abstract

Bioorganic & Medicinal Chemistry publishes complete accounts of research of outstanding significance and timeliness on all aspects of molecular interactions at the interface of chemistry and biology, together with critical review articles. The journal publishes reports of experimental results in medicinal chemistry, chemical biology and drug discovery and design, emphasizing new and emerging advances and concepts in these fields. The aim of the journal is to promote a better understanding at the molecular level of life processes, and living organisms, as well as the interaction of these with chemical agents. The Journal welcomes papers on: the medicinal chemistry and associated biology (including target identification and validation) of established or new disease targets the reporting of the discovery, design or optimization of potent new compounds or biological agents the analysis and discussion of structure-activity relationships and pharmacological issues relevant to drug design and action using in vitro and in vivo models, including the use of computational techniques when closely linked to experimental data the reporting of "first-in-class" new therapeutic compounds the chemical biology or bioorganic/bioinorganic chemistry that significantly advances knowledge of a biological mechanism methodological advances that are chemistry-based and which significantly impact on medicine or biology the preparation and examination of biotherapeutics for the treatment of pathophysiological disease states the development of materials for specific therapeutic targeting All manuscripts will be rigorously peer-reviewed by independent experts following an initial assessment by the Editors. Please note that BMC is not suitable for straightforward reports of incremental advances. Above all the presentation of a rational basis and a sound underlying hypothesis for the work is of particular importance, whatever its exact field.

Importance of protein Ser/Thr/Tyr phosphorylation for bacterial pathogenesis

“…In any case, a thorough understanding of kinase structure and function as well as of the molecular basis for inhibitor specificity should be key to guide further development of both effective and species-specific drugs that could reach the clinic. It should also be mentioned that another currently pursued antibacterial strategy involves the development of inhibitors directed toward secreted bacterial tyrosine phosphatases [249,250]. In addition, host-directed therapeutics targeting host kinases represent yet another exciting branch of explored anti-infectious medicines [251].…”

Synthesis of 4-[(1H-Benzimidazol-2-yl)sulfanyl]benzaldehyde and 2-({4-[(1H-Benzimidazol-2-yl)sulfanyl]phenyl}methylidene)hydrazine-1-carbothioamide

“…Thiosemicarbazone moiety is another privileged structure that is found in several molecules with a wide range of biological activities representing several important classes in drug discovery [7][8][9][10][11][12]. Thiosemicarbazones have been postulated as biologically active compounds and display different types of biological activity, such as anticancer [11,13], anti-HIV [14,15], anticonvulsant [16,17], antimalarial [18,19], anti-inflammatory [20], enzymatic inhibition [9,10,21], antiviral [22], antioxidant [23], antifungal [24], and antibacterial [24,25]. Additionally, the flexibility of thiosemicarbazones as nitrogen and sulfur donors consents them to bring on a great diversity of coordination modes [26].…”

Synthesis, Spectroscopic Characterization, Structural Studies, and In Vitro Antitumor Activities of Pyridine-3-carbaldehyde Thiosemicarbazone Derivatives

“…For several years, thiosemicarbazones with general formula R 1 R 2 CH�N-NH-(C�S)-NH 2 have been attracting the attention of researchers, not only because of their multifunctional coordination modes to transition metal ions [1,2], but also because of their wide range of biological properties including antibacterial [3][4][5][6], antifungal [7], antimicobacterium tuberculosis [8,9], and antitumoral [10][11][12][13][14] activity.…”