共查询到20条相似文献,搜索用时 15 毫秒
1.
Anilkumar R. Kore Muthian ShanmugasundaramIrudaya Charles 《Tetrahedron letters》2012,53(27):3518-3520
An efficient synthesis of new cap analogs containing aminoallyl linkers such as m7G[5′]pppp[5′]U-aminoallyl and m27,3′OG[5′]pppp[5′]U-aminoallyl is reported. The final cap analog has been isolated with high purity (>99.8%) after ion-exchange column purification. 相似文献
2.
A series of l-oxacephem analogs were synthesized and their antibacterial properties against five strains of Gram-positive and Gram-negative bacteria were evaluated in vitro while ceftazidine was selected as control. Some of the tested compounds, compound 2c in narticular,showed more active aeainst three selected strains than the standard. 相似文献
3.
《中国化学快报》2016,(3)
The presence of hydroxyl groups at the C4 and C7 positions in coumarin backbone has been proposed as a potential modification site for providing excellent bioactivity according to previous studies. A series of novel coumarin derivatives were rationally designed and synthesized by use of a complex catalytic system for a targeted modification at the above sites. These derivatives were assayed for nematicidal activity. As predicted, the derivatization enhanced the activity of the coumarins against five nematodes.Compounds 7b, 9a, 10 c and 11 c showed significant strong nematicidal broad spectrum activity against all tested nematodes. Compound 10 c was the most effective with the lowest LC50 values against Meloidogyne incognita(5.1 mmol/L), Ditylenchus destructor(3.7 mmol/L), Bursaphelenchus mucronatus(6.4 mmol/L), Bursaphelenchus B. xylophilus(2.5 mmol/L) and Aphelenchoides besseyi(3.1 mmol/L),respectively. A brief investigation on the structure–activity relationships(SAR) revealed that the targeted modification by a C7 hydroxyl was optimum compared with that of a C4 hydroxyl and that the coupling chain length was crucial for the nematicidal activity. 相似文献
4.
New oxophenylarcyriaflavins were synthesized in a few efficient steps. The key steps involved at first a palladium cross-coupling between the 3-bromo-4-(1H-indol-3-yl)1-methylpyrrole-2,5-dione and the 2-formylphenylboronic acid or a methyl 2-trialkylstannylbenzoate, followed by an intramolecular acylation in a C-2 indolic position. All the sequence was carried out without any indolic protective group. 相似文献
5.
Shoja Sajede Mahmoodi Nosrat Ollah Ghafouri Hossein Rassa Mehdi Sharafshah Alireza Panahi Kokhdan Esmaeel 《Research on Chemical Intermediates》2020,46(7):3327-3339
Research on Chemical Intermediates - The structure of urea has received special attention due to its biological activity. A new and efficient one-pot three-component reaction for the synthesis of... 相似文献
6.
Fourteen phosphodiester-type β-nicotinamide adenine dinucleotide (NAD+) analogs were prepared starting from nicotinamide. The phosphodiester linkage was effectively assembled in 69-93% yields via condensation reaction between 2′,3′-di-O-acetyl nicotinamide mononucleotide and alcohols in the presence of 2,4,6-triisopropylbenzenesulfonyl chloride. The analog β-nicotinamide ribose-5-(2-phenylethyl) phosphate showed beneficial effects on cell growth of model microorganisms. 相似文献
7.
Anna Miyazaki Yoshifumi Tachibana Eibai Lee Gyongyi Bokonyi Yuko Tsuda Yoshio Okada 《Tetrahedron letters》2004,45(33):6323-6327
It was reported that the somatostatin analog TT-232, d-Phe-c(Cys-Tyr-d-Trp-Lys-Cys)-Thr-NH2, exhibited a highly potent antitumor activity in vitro and in vivo. Using pyrazinone analogs and aliphatic amino acids instead of the disulfide bond, we prepared novel type somatostatin analogs including the sequence essential for antitumor activities, Tyr-d-Trp-Lys. These analogs exhibited antiproliferative effect on A431 tumor cells. 相似文献
8.
The synthesis and self-association of protected oxymethylene-bridged UA analogues are described. 相似文献
9.
José G. Aguirre-De Paz Davir González-Calderón Aydeé Fuentes-Benítes Carlos González-Romero 《Tetrahedron letters》2018,59(18):1760-1762
The exploration of azide-enolate cycloaddition in the synthesis of novel Rufinamide analogs is reported for the first time. A very simple procedure involving the use of β-ketonitriles as dipolarophiles afforded 5-aril/heteroayl Rufinamide derivatives in two steps. 相似文献
10.
Zhen-Xing Li He-Shu Fang Wu-Bin Shao Pei-Yi Wang Zhi-Bing Wu 《Phosphorus, sulfur, and silicon and the related elements》2017,192(12):1279-1285
A series of novel nucleobase derivatives and their analogues possessing diethoxyphosphoryl scaffolds were synthesized through four-step reactions and screened for their antiviral activity toward tobacco mosaic virus (TMV). Preliminary bioassays suggested that some of these simple structures displayed appreciable anti-TMV activity in vivo. Among them, compound (diethoxyphosphoryl)methyl 4-[2-(1H-benzo[d][1,2,3]triazol-1-yl)acetamido]-benzoate (a-3) exerted the strongest chemotherapeutic and protective effects against TMV with the rates of 52.8 and 72.2% at the dosage of 500 µg/mL, respectively, which were comparable with those of the commercial agricultural antiviral agent ningnanmycin (54.2 and 70.2%). Molecular docking with TMV helicases revealed that compound a-3 had strong interactions with receptor amino acid residues. Given the facile synthetic route and significant chemotherapeutic and protective potentials, compound a-3 could be further studied and exploited as a promising antiviral candidate. 相似文献
11.
A new class of sugar-oxasteroid-quinone hybrid molecules has been designed and synthesized involving an efficient enyne metathesis/Diels-Alder reaction strategy. 相似文献
12.
Victor A. Egorov Fanuza A. Gimalova Gullira M. Khalikova Mansur S. Miftakhov 《Tetrahedron》2012,68(35):7122-7128
Novel highly functionalized chlorocyclopentenones derivatives with N-, O-, and C-substituents were synthesized. 相似文献
13.
Bhaskar C. Das Sakkarapalayam M. Mahalingam Pranoy Mohapatra 《Tetrahedron letters》2009,50(42):5860-5863
Guanidine-containing new retinoids 1–4 were synthesized through the addition of guanidine to the activated carboxylic acids (retinoids) promoted by carbonyldiimidazole (CDI). A set of structurally and functionally diverse guanidine derivatives of retinoids were obtained in high yields (78–82%). We are in the process of studying the biological effect of these molecules on retinoic acid signaling pathways. 相似文献
14.
Ren-Min Wu Na Qi Yu-Wen Jia Zhu Guan Liang-Ren Zhang Li-He Zhang Zhen-Jun Yang 《中国化学快报》2014,25(12):1583-1585
A facile and efficient protocol for the synthesis of sulfur substituted-cyclopyrophosphate of cIDPRE(P_S~1-cIDPRE) was developed.The key step was the cyclization process which was completed by the sulfur substituted cyclization precursor 1b via the one-pot phosphoramidite strategy. 相似文献
15.
16.
Sakayu Shimizu Kiyoshi Yamane Yoshiki Tani Hideaki Yamada 《Applied biochemistry and biotechnology》1983,8(3):237-247
A new and simple enzymatic method for the synthesis of flavin adenine dinucleotide (FAD) from flavin mononucleotide by the
transadenylylation reaction using microbial cells is described.
Among various microorganisms tested,Artherobacter globiformis IFO 12138 and two soil bacteria were selected as useful enzyme sources. Under suitable reaction conditions, the amount of
FAD synthesized was 2.25 μmol/mL with cells ofA. globiformis.
The transadenylylation reaction could be coupled with the ATP supplying system through a glycolysis process with yeast. 相似文献
17.
18.
Nan-Yang Chen Li-Ping Ren Min-Ming Zou Zhi-Ping Xu Xu-Sheng Shao Xiao-Yong Xu Zhong Li 《中国化学快报》2014,25(2):197-200
Spiro heterocycles frequently occur in bioactive molecules. In the pursuit of neonicotinoids with spiro hererocycles, three types of novel neonicotinoids with spirobenzofuranone, spirooxindole or spiroacenaphythylenone framework were designed and synthesized. Insecticidal evaluation showed that some of spirobenzofuranone containing neonicotinoids exhibited moderate activity against cowpea aphid, armyworm or brown planthopper. 相似文献
19.
A variety of novel 2-alkylthiopyrimidines were synthesized through simple condensation of arylidenemalononitriles with different 2-alkylthiouronium halide derivatives catalyzed by anhydrous potassium carbonate (K2CO3). The reactions have been carried out under mild conditions in i-PrOH, and the products were obtained in moderate to good yields with a simple work-up method. Subsequently, some examples of these compounds have been converted into Tacrine analogs by applying the Friedländer reaction. 相似文献
20.
Biheterocyclic compounds in recent years have gained a significant importance in medicinal chemistry. In this paper the synthesis of novel pyrazol-3ylthiazoles through Vilsmeier–Haack reaction using 2-amino thiazoles as precursors is described. Synthesis of twelve new derivatives was accomplished with moderate yield (70–76%). Structures of all the newly synthesized compounds were characterized by spectral (1H NMR, 13C NMR, IR, LC–MS) and elemental analyses. 相似文献