Synthesis and biological activity of certain amino-derivatives of 5α-steroids

Certain 17β-aminoderivatives of 5α-steroids based on tigogenin were synthesized and their antitumor activity was studied. The structures of the synthesized compounds were confirmed by NMR and IR spectroscopy and mass spectrometry. __________ Translated from Khimiya Prirodnykh Soedinenii, No. 3, pp. 263–265, May–June, 2006.     

Synthesis and biological activity of certain derivatives of anesthesine (Benzocaine)

Certain derivatives of ethyl p-aminobenzoate were synthesized with the purpose of creating biologically active oligomeric condensation products.     

苯并异噻唑啉酮类化合物的合成与活性研究

通过烷基醇与固体三光气(BTC)反应后加入1,2-苯并异噻唑啉-2(3H)-酮(BIT)继续反应的“一锅法”制备了8种未见文献报道的2-(苯并异噻唑啉-3-酮-2-基)甲酸酯类化合物.化合物结构经IR、1HNMR和元素分析确认,并且对枯草芽孢杆菌、金黄色葡萄球菌、嗜水单细胞菌和大肠杆菌进行了初步抑菌活性实验,实验结果表...     

Morpholines. Synthesis and biological activity

The review analyzes methods of synthesis of 1,4-oxazines (morpholines) starting from vicinal amino alcohols and their derivatives, oxiranes, and aziridines. Examples of using morpholines in medicinal and organic chemistry as catalysts, auxiliaries, biologically active substances, and building blocks for their preparation are considered. The data published until February 2013 have been covered.     

Synthesis and biological activity of mycalolide analogs

Mycalolide analog 4, consisting only of the side chain of mycalolide B (2), a trisoxazole macrolide of marine origin, was stereoselectively synthesized using Roush crotylboration, an Evans aldol reaction, and a Paterson aldol reaction as key steps. The analog 4 was found to have strong actin-depolymerizing activity.     

Synthesis and biological activity of yuccagenin bisrhamnoside

The two hydroxyls of yuccagenin can be glycosylated by Koenigs-Knorr condensation with acetobromorhammose in dichloroethane in the presence of mercuric cyanide. The bisrhamnoside of yuccagenin markedly lowers the cholesterol and triglyceride content in blood serum of healthy animals and animals with experimental hyperlipidemia.Translated from Khimiya Prirodnykh Soedinenii, No. 3, pp. 242–243, May–June, 2000.     

Synthesis and biological activity of bactobolin glucosides

Bactobolin glucosides, 5-O-(alpha-D-glucopyranosyl)-, 5-O-(beta-D-glucopyranosyl)- and 6-O-(beta-D-glucopyranosyl)-bactobolin were prepared by glycosidation of bactobolin (1) with the glucopyranosyl trichloroacetoimidate. These compounds were evaluated antimicrobial activity and cytotoxicity.     

Synthesis and biological activity of apratoxin derivatives

This review covers the total asymmetric synthesis and biological evaluation of derivatives of the marine natural products known as the apratoxins.     

Monoterpenoids dithiophosphates. Synthesis and biological activity

O,O-Dialkyldithiophosphoric acids adds at the double bond of the racemic camphene and (+)- limonene in the presence of Lewis acids in accordance with the Markownikoff rule with the formation of Sterpenyl esters of dithiophosphoric acids. The reaction with camphene is accompanied by the rearrangement of camphane structure to that of bornane. Addition of dithiophosphoric acid to (+)-limonene proceeds with the participation of the exocyclic double bond. Toxic and genotoxic properties of the monoterpenoid dithiophosphates were studied.     

Synthesis and cytotoxic activity of certain new arylazothiazole containing compounds

2‐Amino‐5‐arylazo‐4‐(2‐chlorophenyl)thiazoles ( 2a‐e ) were prepared by the coupling of aryldiazonium chlorides with 2‐amino‐4‐(2‐chlorophenyl) thiazole ( 1 ). The thioureas 3a‐e were obtained by condensing the arylazothiazoles 2a‐c with the appropriate isothiocyanates. Reaction of 2d with aromatic aldehydes afforded the chalcone analogues 4a‐c . The pyridone derivatives 5a,b were synthesized by reacting the ketone 2d with different aromatic aldehydes, ethyl cyanoacetate and ammonium acetate. On the other hand, 5b was also prepared by cyclizing 4c with ethyl cyanoacetate and ammonium acetate. Furthermore, 6‐chloroimidazo[2,l‐b]‐thiazole 7 was obtained from the acid derivative 6b by treatment with POC1₃. While, the imidazo[2,l‐b]‐thiazolones 9a‐d were produced by the cyclization of the chloroacetyl derivatives 8a‐d with DMAP/pyri‐dine. Representative examples of the prepared compounds were tested for in vitro antitumor activity against two human tumor cell lines. Some compounds showed activity against brain tumor cell lines.     

双1,3,4-噻二唑基取代脲的合成及其生物活性研究

用2-氨基-5-巯基-1,3,4-噻二唑与1,3-二溴丙烷和一系列叠氮化合物反应,合成了7种未见文献报道的双1,3,4-噻二唑基取代脲类化合物,并用元素分析、红外光谱、质谱和核磁共振氢谱对化合物进行了表征,生物活性实验证明,该类化合物10mg/L表现出较好的生长素活性和细胞分裂素活性。其中化合物a、b的细胞分裂素活性最好,其活性达到39%。     

Synthesis, characterization and biological activity of polyketones

Polyketone resins have been prepared by the Friedel-Crafts polymerization of dithiophenylidenecyclopentanone (Ⅰ), dithiophenylidenecyclohexanone (Ⅱ) and dithiophenylideneacetone (Ⅲ) with adipoyl, sebacoyl and terephthaloyl dichlorides using boron trifluoride as catalyst and carbon disulphide as solvent. Polymers were characterized with IR, 1 H-NMR, and the results showed the presence of carbonyl of ketonic groups in the main chain. The polyketones have inherent viscosities of 0.40-0.70 dL/g. All the polymers are semicrystalline and most of them are partially soluble in most common organic solvents but freely soluble in aprotic solvents. The temperatures of 50% weight loss are as high as 185℃ to 280℃ in air, indicating that these aromatic polyketones have excellent thermal stability. All the polyketones were tested for their antimicrobial activity against bacteria and fungi.     

Synthesis and biological activity of some triarylantimony dipyrazolecarboxylates

A series of triarylantimony dipyrazolecarboxylates was synthesized by the reaction of pyrazolecarboxylic acid with triarylantimony dibromides in the presence of potassium hydroxide. The structures of the title compounds were confirmed by elemental analysis, ¹H NMR, IR, and mass spectra. Some of these compounds were found to possess antibacterial activity. © 2002 Wiley Periodicals, Inc. Heteroatom Chem 13:299–301, 2002; Published online in Wiley Interscience (www.interscience.wiley.com). DOI 10.1002/hc.10033