苔黑酚及苔色酸丁酯诱发微核的效应

苔黑酚(Orcinol),又名3,5～二羟基甲苯,为中草药地衣植物梅花科石花经加热水解、降解脱羧分得的二元酚性化合物,除有抗辐射损伤作用外,对多种霉菌有明显抗菌作用。苔黑酚经醇解酯化反应得苔色酯丁酯。两者体外有明显的杀精子作用。为了解两种药物对人体有无潜在危害,我们按文献方法,观察了其诱发微核的效应。 苔黑酚和苔色酸丁酯均为白色针状结晶颗粒纯     

苔黑酚和苔色酸丁酯对中国仓鼠肺细胞染色体畸变的影响

苔黑酚(Orcinol),又名3,5—二羟基甲苯,为中草药地衣植物梅衣科石花经加热水解、降解脱羧分得二元酚性化合物。苔黑酚除有抗辐射损伤外,对多种霉菌有明显的抗菌作用。苔黑酚经醇解脂化反应可获得苔色酸丁酯(Butyl Ors-ellinate)。这两种药物在体外杀精实验中表明,苔黑酚抑制人精子活动的最低浓度为4mg/ml,苔色酸丁酯为2mg/ml,体外杀精作用明显。为了解两种药物对人体有无潜在危害,我们按文献进行了CHL细胞染色体试验。     

盐酸西曲酸酯的合成方法研究

以４－羟基苯丙酸２和反式４－氨甲环己烷羧酸４为起始原料，以丙酮基为保护基团，合成盐酸曲酸酯１，总收率为４０％左右，质量达到ＪＰⅩⅢ要求。     

硫色(满)酮衍生物的合成及抗真菌活性研究

设计并合成了８个硫色（满）酮及其衍生物，其中７个化合物未见文献报道，其结构均经红外光谱、核磁共振、氢谱及元素分析证实．体外抑菌试验表明：８个化合物均有不同程度的抑菌活性．化合物９４０２，９４０３效果最好，有开发前景．     

毫火针联合异维A酸及抗真菌药治疗马拉色菌毛囊炎疗效观察

目的:研究马拉色菌毛囊炎病患实行毫火针+异维A酸+萘替芬酮康唑乳膏治疗的临床疗效。方法:本研究入组观察对象总计100例,均为2021年4月—2022年6月本院收治的马拉色菌毛囊炎患者,按照随机抽样法进行分组,参照组实行异维A酸联合萘替芬酮康唑乳膏治疗,研究组基于对照组联合毫火针治疗,比对两组治疗效果、皮肤病生活质量、复发率及不良反应发生率。结果:研究组治疗有效率较参照组显著较高,组间差异明显(P<0.05);研究组较参照组皮肤病生活质量评分、评皮损与症状积分在治疗后明显降低,组间差异明显(P<0.05);研究组较参照组的复发率明显较低,组间差异明显(P<0.05)。结论:马拉色菌毛囊炎病患以毫火针、异维A酸、萘替芬酮康唑乳膏联合治疗,能够减轻病患皮肤病,预防复发,提升治疗有效率,预防复发,实践价值较高。     

色酮及硫色酮类抗真菌化合物的研究进展

本文综述了近年来色酮及硫色酮类抗真菌化合物的研究进展,分别对色酮和硫色酮两种化合物进行详细介绍。文章重点阐述了色酮及硫色酮类化合物在抗真菌方面的研究进展及开发现状,介绍了色酮及硫色酮类化合物不同位置的化学修饰及其生物活性,并对其机理和构效关系的进行了分析研究。通过对色酮及硫色酮化合物的抗真菌活性的研究,以期得到更多的有效作用靶点,合成和开发出更多高效、低毒、广谱的抗真菌类药物。     

利拉萘酯的合成

用5,6,7,8-四氢-2-萘酚与硫光气反应得到的硫代氯甲酸5,6,7,8-四氢-2-萘酯和2-甲氧基-6-甲胺基吡啶在异丙醇-水中于室温反应2h得到抗真菌药物利拉萘酯,总收率70%.     

不同的苔色如何分辨

白苔白苔是最常见的苔色，各种苔色均由白苔转化而来。白苔可见于正常人，也可见于疾病初期或疾病恢复期及一些相对较轻的病症。白苔一般主表证、寒证，提示病情较轻，预后较好。常见的白苔包括薄白苔、白滑苔、白腻苔、积粉苔、白燥苔等。     

没食子酰哌嗪类化合物的合成及抗真菌作用研究

目的 设计合成没食子酰哌嗪衍生物,考察其对耐药真菌的抗菌活性。方法 以三甲氧基没食子酸为原料,在PyBOP/DIEA存在下与哌嗪反应得到中间体,在脱保护后与相应的酸缩合,最后脱甲基得到目标化合物。采用美国国家临床实验室标准委员会（CLSI）推荐方法,将目标化合物对2株临床分离的耐药白色念珠菌株进行体外抗真菌活性试验,进而与氟康唑（8 μg/ml）联用,开展协同抗真菌活性试验。结果 共合成了11个化合物,其中6个化合物表现出优于没食子酸的抗真菌活性。结论 没食子酰哌嗪可以提高没食子酸的抗真菌活性,没食子酸酰结构是重要的药效团,若引入桂皮酸或2,3-二氯苯甲酸可以进一步提高活性。     

Halogenated benzoate derivatives of altholactone with improved anti-fungal activity

Altholactone exhibited the anti-fungal activity with a high MIC value of 128 μg ml^?1 against Cryptococcus neoformans and Saccharomyces cerevisiae. Fifteen ester derivatives of altholactone 1–15 were modified by esterification and their structures were confirmed by spectroscopic methods. Most of the ester derivatives exhibited stronger anti-fungal activities than that of the precursor altholactone. 3-Bromo- and 2,4-dichlorobenzoates (7 and 15) exhibited the lowest minimal inhibitory concentration (MIC) values against C. neoformans at 16 μg ml^?1_, while the 4-bromo-, 4-iodo-, and 1-bromo-3-chlorobenzoates (11–13) displayed potent activity against S. cerevisiae with MIC values of 1 μg ml^?1. In conclusion, this analysis indicates that the anti-fungal activity of altholactone is enhanced by addition of halogenated benzoyl group to the 3-OH group.     

5个丹皮酚酯的合成和体外抗肿瘤活性研究

丹皮酚与相应的酰氯反应得到5个新的丹皮酚酯,其结构通过光谱法确证.它们的体外抗肿瘤活性通过MTT法和集落形成法进行了评价.初步的体外生物试验结果表明,5-硝基-2-呋喃甲酸的丹皮酚酯对人肿瘤细胞有一定抑制作用,其结果和临床上常用的抗肿瘤药5-Fu相近.     

苯并吡喃酯类化合物的合成及其生物活性

为寻找活性更高、降压作用更理想的钾通道开放剂 ,合成了 10个苯并吡喃酯类衍生物及3个中间体 ,并对它们进行了体外低钾诱导的血管收缩抑制试验 .结果表明 :化合物浓度为 1×10 -4 mol/L时对低钾 (2 0mmol/L)引起的血管收缩有不同程度的抑制作用 ,化合物 (Ⅰ )和 (Ⅱa)的活性较好 ,抑制率分别为 86 .4%和 79.3 %     

邪蒿素及其衍生物的合成及镇痛活性

本文报道了合成天然产物邪蒿素及其衍生物的新方法，以7-羟基-8-乙酰基香豆素或取代香豆素为原料，经与丙酮缩合、还原、脱水得到单一的角型三环邪蒿素类化合物。三步反应条件温和，各步收率均>80%。12个邪蒿素类衍生物的小鼠醋酸扭体镇痛试验结果表明合成的邪蒿素(4a)和4，8，8-三甲基-9，9-二氢-吡喃［2，3-f］色烯-2，10-二酮(2b)具有明显的镇痛活性，抑制率分别为85%和50%，明显优于或相当于同试验中的对照药阿司匹林。     

Synthesis and biological activity of organosilicontitanium glycerohydrogels

A series of organosilicontitanium (OST) glycerohydrogels with the general formula 2Si(C₃H₇O₃)₄ ⋅ Ti(C₃H₇O₃)₄ ⋅ xC₃H₈O₃ ⋅ yH₂O (where 9 ≤ x ≤ 30 and 60 ≤ y ≤ 120) were synthesized and some of their pharmacological properties were studied. High percutaneous activity of the compounds was revealed by measuring the diffusion of sodium diclofenac through intact skin membranes in vitro. It was established that all of the synthesized substances are nontoxic. The wound-healing and antioxidant properties of the glycerohydrogels were studied. The experimental results show that OST glycerohydrogels can be recommended for further testing as effective percutaneous vehicles of medicines with wound-healing, burn-healing, and antioxidant action. Translated from Khimiko-Farmatsevticheskii Zhurnal, Vol. 43, No. 2, pp. 26–32, February, 2009.     

p-Chlorotetrafluorophenyl esters of N-protected amino acids

p-Chlorotetrafluorophenyl (Tfc) esters of protected amino acids and peptides are more reactive than are the well known pentafluorophenyl (Pfp) esters. Two reagents, p-chlorotetrafluorophenyltrifluoroacetate (Tfc-OTfa) and di-(p-chlorotetrafluorophenyl)carbonate (di-Tfc-carbonate), can be used for their syntheses, thereby avoiding use of the allergic dicyclohexylcarbodiimide. This is especially important for bulk preparations. Many Fmoc- and Boc-amino acid-OTfc esters have been synthesized and characterized. The hexadecameric tanden1 repeat H-(AlaAlaLysPro)₄-OH was synthesized using di-Tfc-carbonate for the preparation of Tfc-esters.     

Synthesis and anti-fungal activity of 5-aminopyrazole derivatives]

4-Thiocyanato-5-amino or acylaminopyrazoles were prepared and their antifungal activity was tested against Candida albicans and Trichophyton mentagrophytes: the 4-thiocyanato-5-aminopyrazoles were the most effective in both tests.     

Serine and d-serine position-1 substituted angiotensin II analogues Synthesis using new 2,3,5,6-tetrafluorophenyl active esters and biological activities

[Ser¹], ( 32 ), [d -Ser¹]- ( 29 ), [Ser¹, Leu⁸]- ( 31 ), and [d -Ser¹, Leu⁸] angiotensin II ( 30 ) were synthesized by a repetitive method in solution using new protected amino acid 2,3,5,6-tetrafluorophenyl active esters. 32 and 29 were agonists, and 31 and 30 were specific antagonists to angiotensin II (AII) receptors determined by the rabbit aortic strip (RAS) and rat blood pressure (RBP) assays. It was found that the hydroxymethyl side chains of serine and D-serine in position-l has an important influence on the agonistic activity of the analogues. The pressor activities of 32 and 29 were 129 and 314%, respectively, as potent as AII. On the other hand, 31 and 30 were effective in antagonizing the AII-induced contraction of RAS and rise in RBP.     

Synthesis of some novel orsellinates and lecanoric acid related depsides as α-glucosidase inhibitors

Abstract

Sixteen novel orsellinic esters (6a-l, 7a-d) along with four lecanoric acid related depsides (3a-c, 4) were synthesized and confirmed their structures by spectroscopic data (¹H, ¹³C & HRMS). The synthesized compounds were evaluated for their in vitro α-glucosidase (Saccharomyces cerevisiae) inhibitory potential. Among the tested compounds, 3c (IC₅₀: 140.9 μM) and 6c (IC₅₀: 203.9 μM) displayed potent α-glucosidase inhibitory activity and found more active than the standard drug acarbose (IC₅₀: 686.6 μM). Both the test compounds were subjected to in vivo antihyperglycemic activity using sucrose loaded model in Wistar rats and found compound 3c exhibited significant reduction in glucose levels.     

取代喜树碱20S-羟基酯衍生物的合成和抗肿瘤活性

为了改善取代喜树碱的溶解性、抗肿瘤活性和毒副作用,设计合成了十二个新的取代喜树碱20-位羟基酯衍生物。初步的体外抗肿瘤实验结果表明,取代喜树碱的酯衍生物与其母体化合物具有相近的细胞毒,这个结果可能和该类酯在溶液中自活化作用有关。而体内抑制肿瘤试验显示这些新酯衍生物的体内抗肿瘤活性弱于拓扑替康。