唾液酸类化合物的合成研究进展

综述了近年来在唾液酸及其衍生物、类似物的设计、合成，以及它们作为唾液 酸酶抑制剂等相关的生物学应用方面的研究进展。     

A concise methodology for the synthesis of (−)-Δ-tetrahydrocannabinol and (−)-Δ-tetrahydrocannabivarin metabolites and their regiospecifically deuterated analogs

The availability of tetrahydrocannabinols (Δ⁹-THC), tetrahydrocannabivarins (Δ⁹-THCV), and their metabolites in both their undeuterated and deuterated forms is critical for the analysis of biological and toxicological samples. We report here a concise methodology for the syntheses of (−)-Δ⁹-THC and (−)-Δ⁹-THCV metabolites in significantly improved overall yields using commercially available starting materials. Our approach allowed us to obtain the key intermediates (6aR,10aR)-9-nor-9-oxo-hexahydrocannabinols in four steps from (+)-(1R)-nopinone. This was followed by an optimized Shapiro reaction to give the (−)-11-nor-9-carboxy-metabolites, which were converted to their respective (−)-11-hydroxy analogs. The synthetic sequence involves a minimum number of steps, avoids undesirable oxidative conditions, and incorporates the costly deuterated resorcinols near the end of the synthetic sequence. This methodology enabled us to synthesize eight regiospecifically deuterated (−)-Δ⁹-THC and (−)-Δ⁹-THCV metabolites in a preparative scale and high optical purity without deuterium scrambling or loss.     

Efficient guanylation of N,N-difunctionalized polyamines at the secondary amino functions

Treatment of N^α,N^ω-ditritylated linear and aromatic polyamines and of polyamine conjugates of the alkaloid kukoamine A (KukA) type with N,N′-bis(tert-butoxycarbonyl)thiourea in the presence of Mukaiyama’s reagent produced high yields of derivatives guanylated at the secondary amino functions.     

Synthesis and antibacterial activity of 4“-O-carbamoyl analogs of clarithromycin

<正>A series of novel 4"-O-carbamoyl analogs of clarithromycin were synthesized and evaluated for their in vitro antibacterial activity. All of the desired compounds showed excellent activity against erythromycin-susceptible S.pneumoniae.Particularly,4-fluorobenzyl carbamate 7a demonstrated potent activity against erythromycin-resistant S.pneumoniae encoded by the mef gene,and remarkably improved activity against erythromycin-resistant S.pneumoniae encoded by the erm gene,and the erm and mef genes.     

Synthesis of Salmon Calcitonin Analogs Using Fmoc-based Chemistry on MBHA Resins

Calcitoninisacyclic32aminoacidpeptidehormonethathashypocalcemicactivity.Althoughtherearemanydifferencesinindividualaminoacidsincalcitoninsofdifferentspecies,theyallhaveadisulfidebridgebetWeencysteineresiduesatpositionsland7,andtheC-terminusisalwaysprolinearnide.TheN-terminaldisulfidebridgeisessentialforthebiologicalactivityofhumancalcitonin,butitisnotrequiredforthatofeelandsalmoncaIcitonin.Alth0ughStudieshavedemonstratedtherequirementforalm0sttheentirepeptidestructuret0keepthehighhyp0calcemi…     

Synthesis and Anti-HIV Activity of Trisubstituted （3＇R, 4＇R）-3＇,4＇-Di-O-（S）-camphanoyl-（＋）-c/s-khenactone （DCK） Analogs

To further explore the potential of DCK analogs as anti-HIV drug candidates, ten new tri-substituted （3＇R,4＇R）-3＇,4＇-di-O-（S）-camphanoyl-（＋）-cis-khellactone （DCK） derivatives （4-13） were designed, synthesized, and evaluated against HIV replication in MT4 cells and H9 lympho- cytes.     

Novel ecdysteroid analogs with oxygen-containing heterocycles in the steroid skeleton

The reaction of ecdysteroids (20-hydroxyecdysone and its acetonides) with lithium in liquid ammonia gave novel analogs with an oxetane 9α,14α-oxacycle in the steroid skeleton. In aqueous alcohol solution the 9,14-oxa analogs rearrange to the more stable 9α,13α-oxa analogs through a 1,2-migration of the 18-Me group from the C-13 to the C-14 atom. Dedicated to Academician B. A. Trofimov in his 70^th jubilee. Translated from Khimiya Geterotsiklicheskikh Soedinenii, No. 9, pp. 1339–1355, September, 2008.     

Synthesis of phosphinic analogs of sulfur-containing amino acids

Phosphinic analogs of the key compounds of the metabolism of methionine were synthesized. The compounds obtained were selectively oxidized either at the phosphinic group or at the sulfur-containing fragment. Translated fromIzvestiya Akademii Nauk. Seriya Khimicheskaya, No. 7, pp. 1360–1363, July, 1999.     

桃抗病基因同源序列的克隆与分析

根据已克隆的STK类抗病基因的保守区设计简并引物对4个不同桃的基因组DNA进行PCR扩增,将获得的扩增片段的回收产物,应用pGEM-T easy裁体试剂盒进行了目的基因片段的克隆.随机挑取若干单克隆经PCR鉴定确认后,进行测序,共获得11个各不相同的片段序列.氨基酸序列分析中,有6个片段能推导出完整的氨基酸序列.除了两侧都基本具有STK类抗病基因产物的保守结构域.