642969-74-2Relevant academic research and scientific papers
Identification of acylthiourea derivatives as potent Plk1 PBD inhibitors
Yun, Taikangxiang,Qin, Tan,Liu, Ying,Lai, Luhua
, p. 229 - 236 (2016)
Thiourea derivatives have drawn much attention for their latent capacities of biological activities. In this study, we designed acylthiourea compounds as polo-like kinase 1 (Plk1) polo-box domain (PBD) inhibitors. A series of acylthiourea derivatives without pan assay interference structure (PAINS) were synthesized. Four compounds with halogen substituents exhibited binding affinities to Plk1 PBD in low micromole range. The most potent compound (3v) showed selectivity over other subtypes of Plk PBDs and inhibited the kinase activity of full-length Plk1.
Synthesis, molecular docking studies, and in vitro screening of sulfanilamide-thiourea hybrids as antimicrobial and urease inhibitors
Saeed, Aamer,Zaib, Sumera,Pervez, Arshid,Mumtaz, Amara,Shahid, Mohammad,Iqbal, Jamshed
, p. 3653 - 3662 (2013/07/26)
A series of novel hybrid molecules containing sulfanilamide and thiourea templates was designed and synthesized. These compounds were screened for antimicrobial and urease inhibitory activities. Some of the compounds revealed promising antibacterial and a
Synthesis, characterization of some new 1-aroyl-3-(4-aminosulfonylphenyl) thioureas and crystal structure of 1-(3,4,5-trimethoxybenzoyl)- 3-(4-aminosulfonylphenyl)thiourea
Saeed, Aamer,Mumtaz, Amara,Ishida
, p. 45 - 54 (2012/01/06)
A small library of novel 1-aroyl-3-(4-aminosulfonylphenyl)thiourea derivatives was synthesized by the reaction of sulfanilamide with substituted aroyl isothiocyanates in dry acetonitrile. The scope of the reaction was indicated by the synthesis of 1-undecanoyl-3-(4-aminosulfonylphenyl)thiourea, an acyl derivative involving alkanoyl isothiocyanate. All the compounds have been characterized by analytical and spectroscopic methods and in one case by single-crystal X-ray diffraction data.
