Synthesis and anti-oomycete activity of novel quinazolin- and benzothiazol-6-yloxyacetamides: Potent aza-analogs and five-ring analogs of quinoline fungicides

Novel quinazolin- and benzothiazol-6-yloxyacetamides show excellent in vivo activity against the three economically most important Oomycete pathogens Phytophthora infestans, Plasmopara viticola and Pythium ultimum. They are polar analogs of known quinolin-6-yloxyacetamides, which are not active against the soil-borne damping-off disease caused by Pythium ultimum. The Bogert quinazoline synthesis, an almost forgotten heterocyclization technique, proved to be highly useful for the concise construction of required quinazolin-6-ol building blocks.     

风景园林视角下的南粤古驿道规划设计研究

游径系统一直是广东城乡规划建设的亮点,也是推动高质量发展与高水平保护的重要手段。以广东省绿道建设和古驿道建设为例,通过厘清两类游径的缘起和作用,总结风景园林专业力量在绿道建设实施过程中形成的风景园林遗产保护、大地景观规划、园林与景观设计、园林工程与技术、园林植物应用、景观生态学等专业设计之“道”,提出在南粤古驿道建设的大背景下,风景园林人应充分发挥风景园林专业优势,以“道”传“道”,将绿道专业设计之“道”传承到南粤古驿道建设中去,推动南粤古驿道建设高质量发展,同时为风景园林专业设计人员以南粤古驿道为载体进行景观创作提供路径与方法。     

郊野公园植物多样性的生态恢复与重建——以上海滨江森林公园为例

植物作为自然界生态系统的重要组成部分,其多样性的保护与发展是人类可持续发展的物质基础之一,对维护生态环境的平衡与稳定具有重要意义,也是当今中国生态园林城市建设的重要内容。以上海滨江森林公园一期工程为例,通过总结建设过程中自然生境的恢复与重建、现状植物保护和开发的经验,探索郊野公园设计建造中植物多样性保护的有效措施,为今后城市郊野公园的建设和原有绿地的绿化改造等提供参考借鉴。     

生脉注射液联合曲美他嗪治疗缺血性心肌病合并肾功能不全的临床疗效分析

目的:研究生脉注射液联合曲美他嗪治疗缺血性心肌病合并肾功能不全的临床疗效。方法:选取2015年3月至2017年3月我院收治的100例缺血性心肌病合并肾功能不全患者,按照随机数表法分为观察组(n=50)和对照组(n=50)。对照组采用曲美他嗪治疗,观察组采用生脉注射液联合曲美他嗪治疗。观察和比较两组的治疗疗效、治疗前后心功能指标(左心室射血分数(LVEF)、左室收缩末径(LVESD)、左室舒张末期内径(LVEDD))、肾功能指标(血肌酐(Scr),尿素氮(BUN))、心肌损伤标志物(血清胱抑素(Cys C)、同型半胱氨酸(HCY)、脑钠肽(BNP))水平的变化。结果:治疗后,观察组总有效率显著高于对照组[92.30%(48/52) vs.70.83%(34/48)](P0.05),LVEDD、LVESD水平均显著低于对照组[(51.21±8.54)mm vs.(56.63±10.83)mm,(42.91±6.30)mm vs.(45.86±7.32)mm](P0.05),LVEF水平均显著高于对照组[(46.02±7.85)%vs.(41.20±8.84)%](P0.05),Scr、BUN水平均显著低于对照组[(164.30±17.95)μmol/L vs.(211.75±19.31)μmol/L;(8.12±0.76)mmol/L vs.(11.74±1.72)mmol/L](P0.05)。血清Cys C、HCY、NT-Pro BNP水平均显著低于对照组[(0.90±0.21)mg/L vs 1.52±0.34)mg/L (12.34±3.89)μmol/L vs.(20.86±5.28)μmol/L,(298.47±78.41)ng/L vs.(402.35±92.76)ng/L](P0.05)。结论:生脉注射液联合曲美他嗪治疗缺血性心肌病合并肾功能不全的的临床疗效显著优于单用曲美他嗪治疗,其可有效改善患者心、肾功能,减轻心肌细胞损伤。     

Prdm9 and Meiotic Cohesin Proteins Cooperatively Promote DNA Double-Strand Break Formation in Mammalian Spermatocytes

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The aspartimide problem persists: Fluorenylmethyloxycarbonyl‐solid‐phase peptide synthesis (Fmoc‐SPPS) chain termination due to formation of N‐terminal piperazine‐2,5‐diones

Aspartimide (Asi) formation is a notorious side reaction in peptide synthesis that is well characterized and described in literature. In this context, we observed significant amounts of chain termination in Fmoc‐SPPS while synthesizing the N‐terminal Xaa‐Asp‐Yaa motif. This termination was caused by the formation of piperazine‐2,5‐diones. We investigated this side reaction using a linear model peptide and independently synthesizing its piperazine‐2,5‐dione derivative. Nuclear magnetic resonance (NMR) data of the side product present in the crude linear peptide proves that exclusively the six‐membered ring is formed whereas the theoretically conceivable seven‐membered 1,4‐diazepine‐2,5‐dione is not found. We propose a mechanism where nucleophilic attack of the N‐terminal amino function takes place at the α‐carbon of the carbonyl group of the corresponding Asi intermediate. In addition, we systematically investigated the impact of (a) different adjacent amino acid residues, (b) backbone protection, and (c) side chain protection of flanking amino acids. The side reaction is directly related to the Asi intermediate. Hence, hindering or avoiding Asi formation reduces or completely suppresses this side reaction.     

BRCA1 Haploinsufficiency Is Masked by RNF168-Mediated Chromatin Ubiquitylation

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木麻黄海防林种子雨的时空动态

为了解木麻黄(Casuarina equisetifolia)种子雨的时空间分布格局和萌发性能对其天然更新的影响,对海口木麻黄海防林种子雨的时空分布特征和种子雨的萌发动态进行了研究。结果表明,木麻黄种子落雨时间始于7月中旬,结束于次年4月中旬,持续长达9个月,期间种子雨年际平均密度为1 764.63 grain m~(-2)a~(-1);种子雨高峰期在12月上中旬,落种量占总散落量的43.38%;种子雨呈聚集分布,且种子雨密度与附近球果数量呈极显著正相关;种子雨萌发率较低,仅为11.31%,但由于种子雨密度较大,可萌发的种子雨密度仍然较大,为199.58grainm~(-2)a~(-1)。因此,种子数量和质量均不是制约木麻黄天然更新困难的主要障碍因子,但聚集分布特征使木麻黄种子在林内扩散能力十分有限。     

江西庐山国家级自然保护区珍稀濒危植物优先保护定量研究

为制定江西庐山国家级自然保护区珍稀濒危植物的保护策略,采用濒危系数、遗传系数及物种价值系数等评价指标对58种珍稀植物的濒危程度和优先保护顺序进行评估。结果表明,自然保护区珍稀植物的综合评价值(VS)为0.153～0.742,濒危等级为安全的11种,占该区珍稀保护植物总数的19%;稀有的28种(48%);渐危的18种(31%);濒危的1种(2%)。优先保护顺序为Ⅰ级的8种,占该区珍稀保护植物总数的14%,急需保护;Ⅱ级的22种(38%),需要保护;Ⅲ级的23种(40%),可以一般保护;IV级的5种(8%),较为安全。生境破坏和人为干扰是该区珍稀植物保护面临的主要威胁。