1,3-bis(4-chlorobenzoyl)imidazolidine-2-thione

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 英文名称: 1,3-bis(4-chlorobenzoyl)imidazolidine-2-thione
• 英文别名: 1,3-Bis-(4-chlor-benzoyl)-imidazolidin-2-thion；[3-(4-Chlorobenzoyl)-2-sulfanylideneimidazolidin-1-yl]-(4-chlorophenyl)methanone
• 化学式: C₁₇H₁₂Cl₂N₂O₂S
• 分子量: 379.266
• InChiKey: LQHUSKDJEFLKIS-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.2
• 重原子数：
  24
• 可旋转键数：
  2
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.12
• 拓扑面积：
  72.7
• 氢给体数：
  0
• 氢受体数：
  3

反应信息

• 作为产物：
  描述：

  亚乙基硫脲 、 4-氯苯甲酰氯 在 吡啶 作用下， 反应 0.5h， 以93%的产率得到1,3-bis(4-chlorobenzoyl)imidazolidine-2-thione
  参考文献：
  名称：

  N-Acylated and N,N′-diacylated imidazolidine-2-thione derivatives and N,N′-diacylated tetrahydropyrimidine-2(1H)-thione analogues: Synthesis and antiproliferative activity

  摘要：

  Fifty-one acylthioureas (ATUs) incorporating imidazolidine-2-thione or its upper cyclohomologue were prepared by parallel synthesis and evaluated against a high number of human cancer cell lines for antiproliferative activity. ATUs 1o (3,5-dichlorobenzoyl), 1s (2-furoyl), 3s (2-furoyl) and 1t (2-thenoyl) displayed activity against leukemia, melanoma LOX IMVI, non-small cell lung NCI-H522, renal 786-0, CAKI-1, SN12C, UO-31 and breast MCF7, MDA-MB-435, T-47D cancer cell lines in the 0.3-9.7 mu M concentration range. Compound 14s exhibited selectivity for melanoma SK-MEL-5 (GI(50) < 5 nM); 1s for leukemia MOLT-4 (GI(50): 300 nM); 1q, 3b and 3q for renal cancer UO-31 (GI(50): 70200 nM); 8s, 9s for non-small cell lung cancer EKVX (GI(50): 300, 10 nM) and 3j for HOP-92 (GI(50): 700 nM) cell line. (C) 2008 Elsevier Masson SAS. All rights reserved.

  DOI：

  10.1016/j.ejmech.2008.06.010

文献信息

• Clinical Characteristics and Six-Month Outcomes of Nursing Home Residents With Low Activities of Daily Living Dependency
  作者：A. Buttar、C. Blaum、B. Fries

  DOI：10.1093/gerona/56.5.m292

  日期：2001.5.1

  Background. Up to 30% of nursing home residents have very little dependency in activities of daily living (ADLs). We compared the characteristics and six-month outcomes of a sample of low-ADL-dependent nursing home residents (LDR) with other residents.Methods. This is a cross-sectional, six-month follow-up study using secondary data analysis. We combined the separate 1990 and 1993 cohorts in the Resident Assessment Instrument evaluation study. In each case these data were collected in the same 254 nursing homes in 10 states. We studied residents with a length of stay greater than 60 days and age 65 years and older (N = 3955). We compared the baseline characteristics of LDR (n = 985) with all other residents. We then compared six-month outcomes of LDR with other residents and characteristics of LDR with poor outcomes (death or worsened ADL disability) with LDR who remained stable.Results. The LDR had a significantly decreased frequency of geriatric syndromes (i.e., cognitive impairment, urinary incontinence, under-nutrition, vision problems, poor balance, and pressure ulcers) and neurological disease but had the same frequency of non-neurological chronic diseases and were on more medications. Thirty-one percent had poor six-month outcomes associated with baseline poor cognition, incontinence, poor appetite, and presence of vascular disease, daily pain, shortness of breath, and multiple medications.Conclusion. Our research identified 29% of nursing home residents with higher physical function (LDR) who had fewer geriatric syndromes and neurological disease diagnoses; 69% of these remained stable at 6 months. Those LDR with a higher risk of poor outcomes could be prospectively identified. LDR who remained stable for 6 months may represent a group who could potentially be maintained in the community.