Microwave Assisted Synthesis and Biological Activity of N-Aryl-N'-nicotinoyl Thiourea

Abstract

Research on the synthesis and biological activity of heterocyclic compounds is an important developmental oriental in pesticide and medicine chemistry 1. It is well known that nicotinic acid and their derivatives exhibit excellent biological activity. Novel pyridine and related derivatives 2 are attractive molecules because their structure is present in several natural compounds, drugs or argochemicals. Additionally, various types of acyl-thiourea derivatives had comprehensive bioactivities, due to they held amide group 3 and thioamide group. Microwave technique, meanwhile, has been widely used for a variety of organic reactions, such as Claisen, heterocyclic synthesis, oxidation, hydrolysis, esterification, etherification and so on. Many reports 4 have been published in favour of its considerable accelerations of the reaction rates and satisfactory yields. In order to search for new compounds with good biological activity, ten thiourea derivatives (3a-j) were synthesized under microwave irradiation. Their structures are confirmed by 1 H NMR, IR, MS and elemental analysis. The preliminary biological tests show that these compounds had moderate fungicidal activity. EXPERIMENTAL Nicotinic acid, substituted aniline were commercially available. Melting points were determined using a X-4 melting apparatus and were uncorrected. Infrared spectra were recorded on a Bruker Equinox55 spectrophotometer as potassium

Synthesis of New Thiourea-Metal Complexes with Promising Anticancer Properties

“…Moreover, among the antitumor compounds discovered in recent years thiourea rivatives have exhibited potent anticancer properties [49][50][51][52][53][54][55][56][57]. These ligands, due to presence of hydrogen bonding NH moieties, can favor the formation of such bonds, th increasing their solubility in an aqueous medium and allowing a better cellular upta The great versatility of thioureas is noteworthy, since some of their derivatives ha proven to be agents with a great diversity of biological properties, ranging from bacte cidal to herbicidal or insecticides [58][59][60][61][62][63].…”

Screening of in vitro and in silico effect of Fluorophenylthiourea compounds on glucose 6‐phosphate dehydrogenase and 6‐phosphogluconate dehydrogenase enzymes

“…Because of the presence of hydrogen bonding ‐NH moieties, these ligands can increase their solubility in an aqueous medium. The versatility of thioureas is notable, as several of its derivatives have been shown to have a wide range of biological properties, including herbicidal, antibacterial, and insecticidal capabilities 91,92 …”

“…The versatility of thioureas is notable, as several of its derivatives have been shown to have a wide range of biological properties, including herbicidal, antibacterial, and insecticidal capabilities. 91,92 G6PD inhibition may help cancer cells become more sensitive to chemotherapy. Hence, inhibition of PPP enzymes has been proposed as a promising cancer treatment strategy.…”

Synthesis and biological evaluation of 3-amino-1,2,4-triazole derivatives as potential anticancer compounds

“…Compounds 1.1-32 were synthesized by following the previously described procedures [28][29][30][31][32][33][34][35][36][37][38][39] . The NMR spectral data of compounds 1.1-32 were in accordance with those reported in the literature N,5-diphenyl-1H-1,2,4-triazol-3-amine 40 (2.…”