Within the past ten years, a huge volume of research on the synthesis, structure-activity relationships (SAR), and anticancer activities of the urea derivatives was reported. Many aromatic urea derivatives such as N-phenyl-N'-(2-chloroethyl)ureas (CEUs) and benzoylureas (BUs) show good anticancer ac …

Urea containing compounds are increasingly used in medicinal chemistry and drug design in order to establish key drug-target interactions and fine-tune crucial drug-like properties. In this perspective, we highlight physicochemical and conformational properties of urea derivatives.

2011年9月9日 · In this study, clear structure activity relationships (SAR) for anti-tubercular activity of urea-based inhibitors has emerged with the best compounds containing a 1-cycloalkyl-3-phenyl disubstituted urea structure. The 1–3 disubstituted urea moiety was shown to be most active over other urea substitution patterns and urea bioisosteres.

2021年10月15日 · The SAR led to the identification of a novel quinoxaline urea analog 84 that reduced the levels of p-IKKβ in dose- and time-dependent studies. When compared to 13–197, analog 84 was ∼2.5-fold more potent in TNFα-induced NFκB inhibition and ∼4-fold more potent in inhibiting pancreatic cancer cell growth.

2018年12月15日 · Urea carboxylic acids, products of aryl hydantoin hydrolysis, were recently identified as a new antischistosomal chemotype. We now describe a baseline structure-activity relationship (SAR) for this compound series. With one exception, analogs of lead urea carboxylic acid 2 were quite polar with Log …

2023年10月16日 · To explain the relationship between the chemical structure and the biological properties of the newly synthesized compounds, the Structure–Activity Relationship (SAR) of urea derivatives 7–11...

2017年1月5日 · synthesized analogues of urea showed activity against the entire strain of microorganisms. In SAR study the relationship between the functional . roup variation and the biological activity of the evaluated compounds were well discussed. Based on the results obtained, all analogues were found to be very active compared.

2008年10月15日 · The structure-activity relationships (SAR) and optimization of the tyrosine urea series are described. SAR exploration of multiple regions of a tyrosine urea template led to the identification of very potent muscarinic acetylcholine receptor antagonists such as 10b with good subtype selectivity for M (3) over M (1).

2018年2月1日 · Expansion of antischistosomal N, N ′-diaryl urea SAR. 3-Trifluoromethyl-4-pyridyl and 2,2-difluorobenzodioxole improve exposure. 4-Fluoro-3-trifluoromethylphenyl required for best antischistosomal activity. N, N ′-Diaryl ureas have recently …

2017年4月3日 · A sequence of symmetrical and unsymmetrical urea derivatives 1–24 were synthesized and characterized by standard spectroscopic techniques. The synthesized analogues were tested for their in vitro H+/K+-ATPase and anti-inflammatory activities.