共查询到20条相似文献,搜索用时 15 毫秒
1.
Synthesis and anti-HIV-1 activity of the conjugates of gossypol with oligopeptides and D-glucosamine
Jian Yang Ju-Rong Li Jing-Xiang Yang Long-Long Li Wen-Jie Ouyang Shu-Wen Wu Fang Zhang 《中国化学快报》2014,25(7):1052-1056
A series of novel gossypol derivatives were synthesized and screened for their in vitro anti-HIV- 1I activity. The results showed that replacing the aldehyde groups of gossypol with certain oligopeptides and Dglucosamine not only reduced the cytotoxicity of gossypol derivatives but also enhanced their antiviral activity against HIV-1. Interestingly, D-glucosamine derivative of gossypol that lacked the COONa group also exhibited the same potent anti-HIV-1 activity as oligopeptide derivatives with the COONa group. These compounds blocked the entry of HIV-1ⅢB into target cell. which was similar to T20. Furthermore, the molecular docking analysis rationalized their anti-HIV-1 activity. The results also implied that certain oligopeptides and D-glucosamine were important moities to prepare gossypol derivatives as HIV- 1 entry inhibitors besides certain amino acids. 相似文献
2.
3.
Revathi A. Gupta Arun Kumar Gupta Love Kumar Soni Satish G. Kaskhedikar 《Chemical Papers》2009,63(6):723-730
Enduring pandemic nature of tuberculosis urges to explore novel antimycobacterial agents with different mechanism of actions.
Plant containing 1,4-naphthoquinone derivatives showed promising antitubercular activity with novel mode of action and their
synthetic/semi-synthetic derivatives devoid of toxicity. Structural requirements of naphthalene-1,4-dione derivatives towards
antitubercular activity and cytotoxicity were explored using a mathematical model in order to understand their physicochemical
parameters. A quantitative structure activity relationship study furnished some important structural insights for antitubercular
activity, i.e. average connectivity index, information content index of neighborhood symmetry, aromatic ratio, and path/walk
3 Randic shape index. Similarly it also provides drivers for the cytotoxicity of compounds. These drivers will be helpful
in further development of safer and potent 1,4-naphthoquinone derivatives. 相似文献
4.
Shoji Kobayashi Yoshiki Hamada Takeshi Yasumoto Yuuki Hashino Araki Masuyama Kaoru Nagai 《Tetrahedron letters》2018,59(18):1733-1736
We report the syntheses and neuroprotective activities of hericenes and their derivatives against endoplasmic reticulum (ER) stress-dependent cell death. Four natural products, including hericenes A?C and hericenol A, and five synthetic derivatives were synthesized and their protective activities were evaluated. In designing the synthetic derivatives, we focused on the binding position of the fatty chain. Hericenes B and C showed moderate protective activity against thapsigargin-induced ER stress-dependent cell death. In contrast, their regioisomers (with respect to the position of the fatty chain) exhibited higher protective activity against tunicamycin-induced ER stress. This study clearly shows that the number and the binding position of the fatty chain are critical for protective activity against ER stress-dependent cell death. 相似文献
5.
A series of 75 imidazo[1,2-a]pyrimidine derivatives were synthesized. The "in vitro" antibacterial activity of these compounds and their corresponding alpha-bromoketones against a variety of gram (+), gram (-) bacteria and Mycobacterium species is reported. Some of the prepared derivatives exhibited potent antimicrobial activity. 相似文献
6.
A series of 3-substituted guaiazulene derivatives has been synthesized and their antioxidant properties were evaluated by monitoring their capacity for scavenging the stable free-radical DPPH. 3-Vinylguaiazulene was the most potent, possessing antioxidant activity superior than alpha-tocopherol. These derivatives were also moderate inhibitors of the proliferation of human promyelocytic leukemia cells. 相似文献
7.
Chen-Yu Ling Yun-Liang Tao Wen-Jing Chu Hui Wang Hai-Dong Wang Yu-She Yang 《中国化学快报》2016,27(2):235-240
A series of novel pleuromutilin derivatives with 4H-pyran-4-one and pyridin-4-one substitution in the C-14 side chain have been designed and synthesized. In vitro antibacterial activity evaluation showed that most of the derivatives exhibited potent antibacterial activity against drug resistant Gram-positive strains. Compounds 12a, 12d, and 28 are the most active derivatives in this series, displaying activity comparable to that of retapamulin and BC-3781. As the metabolic stability of this series is not satisfactory, further modifications are going on to improve their pharmacokinetic profile. 相似文献
8.
E. A. Alekseeva K. S. Andronati A. V. Mazepa A. I. Gren’ T. V. Pavlovskaya I. A. Kravchenko V. I. Bozhanov 《Russian Journal of General Chemistry》2006,76(9):1464-1467
A series of p-tert-butylcalix[4]arene derivatives containing 1,4(1,5)-benzodiazepinone fragments as substituents were prepared. The biological activity of the compounds, namely, their antispasmodic activity in mice, was evaluated by antagonism with a spasmodic agent, Corazol, upon transdermal administration. According to the data obtained, benzodiazepine derivatives of calixarenes show higher antispasmodic activity compared to 3-hydroxyphenazepam, taking into account their considerably higher molecular weight. 相似文献
9.
AbstractObtucarbamate A was purified from Disporum cantoniense with good antitussive property. In present work, a series of obtucarbamate A derivatives were designed and synthesized from obtucarbamate A by microwave method, and their antitussive activity were evaluated. The results showed that the toluene diisocyanate was obtained with a yield of 95.1% using a simple method, 1-methyl-2-pyrrolidinone as solvent, temperature of 190?°C, microwave irradiation at 60?W power for 30?min. All compounds have good antitussive activity, and small steric hindrance unsaturated groups of ester chains and amino groups favor activity. It is the first reported of obtucarbamate A derivatives used as antitussive, and the results provide a basis for the application of obtucarbamate derivatives as new antitussive. 相似文献
10.
A series of novel furan-2-yl(phenyl)methanone derivatives were synthesized, and their structures were established on the basis of 1H-NMR, 13C-NMR and mass spectral data. All the prepared compounds were screened for their in vitro protein tyrosine kinase inhibitory activity and several new derivatives exhibited promising activity, which, in some cases, was identical to, or even better than that of genistein, a positive reference compound. The preliminary structure-activity relationships of these compounds were investigated and are discussed. 相似文献
11.
Synthesis and preliminary cytotoxic evaluation of substituted indoles as potential anticancer agents
Chang Qing Shi Zhang Qin Liu Wen Qing Lin Yuan Wei Chen 《中国化学快报》2007,18(8):899-901
A variety of indole derivatives were designed,synthesized and preliminarily evaluated for their in vitro cytotoxic activity in the A431 and H460 cell lines.All the compounds examined conferred unusual potency in a tumor cell cytotoxicity assay.The findings showed the indole derivatives would be a promising candidate for the development of new anticancer agents. 相似文献
12.
E. Noula V. F. Samanidou A. N. Assimopoulou V. P. Papageorgiou I. N. Papadoyannis 《Analytical and bioanalytical chemistry》2010,397(6):2221-2232
Isohexenylnaphthazarins (IHN), commonly known as alkannins and shikonins (A/S), are potent pharmaceutical substances with
a wide spectrum of wound healing, antimicrobial, anti-inflammatory, and antitumor activity. Purification of A/S is crucial
for their use in pharmaceuticals and for biological experimentation. Dimeric and oligomeric A/S derivatives co-exist with
the active monomeric ones in most of the samples produced either by (semi)-synthesis or biotechnologically or isolated from
natural products. Oligomeric A/S derivatives have not been studied for biological activity hitherto and a method to isolate
them is essential. 相似文献
13.
Pier Luigi Ferrarini Claudio Mori Muwaffag Badawneh Clementina Manera Adriano Martinelli Federico Romagnoli Giuseppe Saccomanni Mauro Miceli 《Journal of heterocyclic chemistry》1997,34(5):1501-1510
Several 1,8-naphthyridine derivatives have been diazotizated to obtain the corresponding hydroxy derivatives or mixture of hydroxy and hydroxy nitro derivatives. The respective amounts of hydroxy and hydroxy nitro derivatives depends on the nature of the substituents, on their position on the naphthyridine nucleus, on the amount of sodium nitrite and on the reaction temperature. A study of the electronic density of some molecules suggests a possible explanation of the effects induced by the nature of the substituents and of their position. Some of the compounds were tested for their ability to inhibit human platelet aggregation in vitro induced by arachidonic acid. Only compound 26 showed interesting antiplatelet activity. 相似文献
14.
Naturally occurring isohexenylnaphthazarins (IHN), such as Alkannin, Shikonin (A/S) and their derivatives, are potent pharmaceutical substances with a wide spectrum of biological activity. In the present study, inclusion complexes of alkannin and shikonin commercial samples and IHN derivatives in the form of an oily extract of Alkanna tinctoria roots were formed with beta-cyclodextrin (CD) and beta-HPCD. These complexes were investigated to evaluate the effect of complexation on their aqueous solubility, decoloration, and also the percentage of polymeric A/S and IHN derivatives enclosed in the CDs cavity, since these decrease the active monomeric IHN. Both beta-CD and beta-HPCD increased the aqueous solubility of A/S and IHN derivatives and thus inclusion complexes can be used as drug delivery systems for A/S in both internal (capsules, tablets) and external hydrophilic pharmaceutical and cosmetic preparations (creams, gels, sprays) with enhanced bioavailability. The inclusion complexes formed had a pale purple colour, contributing to the partial decoloration of the A/S and thus of the fi nal pharmaceutical preparations. Finally, CDs selectively included more monomeric and less polymeric IHN, compared with the initial each time sample that is encapsulated; thus inclusion complexes may present enhanced biological activity. 相似文献
15.
《Journal of heterocyclic chemistry》2018,55(9):2123-2129
Two new series of pyrazoles and bipyrazoles were synthesized, and their structures were elucidated according to all data results from spectral and elemental analyses. The pathway of the formation of the new bipyrazole derivatives was discussed. Further, all the synthesized derivatives were screened for their antitumor activity on human lung (A‐549) and hepatocellular cancer (HepG‐2) cell lines. The results of antitumor screening have exhibited that several derivatives are more potent than the reference drug. 相似文献
16.
Antioxidative and 5-lipoxygenase inhibiting activities of novel bis(4-hydroxy-2,3,5-trimethylphenoxy)alkyl derivatives 总被引:2,自引:0,他引:2
Hirano T Kawasaki N Miyataka H Nishiki M Satoh T 《Chemical & pharmaceutical bulletin》2001,49(2):225-229
Novel bis(4-hydroxy-2,3,5-trimethylphenoxy)alkyl derivatives were synthesized and evaluations were made of their inhibiting action on Fe3+-ADP induced lipid peroxidation in rat liver microsome and reducing action on alpha,alpha-diphenyl-beta-picrilhydrazyl (DPPH), a stable radical, in addition to their inhibiting action on 5-lipoxygenase (5-LO), an enzyme that synthesizes leukotrienes. We performed a structure-activity correlation study on these derivatives. A strong Fe3+-ADP induced lipid peroxidation preventing activity was observed for the derivatives with an odd number of methylene groups including 1,3-bis(4-hydroxy-2,3,5-trimethylphenoxy)propane (3b) and 3a. No change in the DPPH reducing activity was found with change in the number of methylene groups. 5-LO inhibiting activity among the derivatives was the highest for 1,6-bis(4-hydroxy-2,3,5-trimethylphenoxy)hexane (3e). MM2 calculations were performed to find a stable steric structure for the derivatives, and 1,5-bis(4-hydroxy-2,3,5-trimethylphenoxy)pentane (3d) showed a strong activity in both antioxidative action and 5-LO inhibiting action. 相似文献
17.
Ramesh V. Rao G. Purna Chander Ramachandran D. Chakravarthy A. Kalyan 《Russian Journal of General Chemistry》2019,89(7):1491-1495
A series of new amide derivatives of imidazopyridine is synthesized and structures of the products are confirmed by 1H and 13C NMR, and mass spectral data. The synthesized derivatives are screened for their anticancer activity against four human cancer cell lines: lung cancer (A549), breast cancer (MCF-7), melanoma cancer (A375), and colon cancer (HT-29). Six synthesized compounds exhibit more potent activity than the control drug.
相似文献18.
A series of 1,3,4‐oxadiazole and 1,2,4‐triazole derivatives of 4‐hydroxyphenyl acetic acid have been synthesized and evaluated for their anti‐inflammatory activity by carrageenan induced rat paw edema method. The compounds, which showed good anti‐inflammatory activity, were screened for their ulcerogenic and lipid peroxidation activities. 相似文献
19.
Thirteen novel NO-releasing derivatives of betulinic acid (BA) bearing two types of NO-donors (nitrates and furoxans) were synthesized and evaluated for their antitumor activity. The results showed that furoxan-based derivatives exhibited higher antitumor activity than nitrate-based derivatives, with compounds 11a and 11b displaying promising potency against B16 cell lines and HepG2 cell lines (IC50 < 1 μmol/L). Wesupposed that NO-releasing amount of these derivatives which can be detected by Griess method may contribute more to their antitumor activity. As a result, furoxan-based derivatives released larger amount of NO than that of nitrate-based derivatives, which partially explained the higher anti-tumor activity of the former. 相似文献
20.
Hiroyuki Nakazumi Tamio Ueyama And Teijiro Kitao 《Journal of heterocyclic chemistry》1984,21(1):193-196
A number of 2-phenyl-4H-benzo[b]thiopyran-4-ones (thioflavones) and related compounds have been prepared to test their antibacterial activity. The flavone derivatives were also prepared to compare with their antibacterial activity. It was found that hydroxythioflavones were easily prepared by demethylation of methoxythioflavones with aluminium chloride. In the test of antimicrobial activity, methoxy- or hydroxythioflavones were found to be inactive. It is suggested that the sulfone or sulfoxide of thioflavone is required for antimicrobial activities against yeast funguses and molds. These thioflavone derivatives exhibit low acute toxicity. 相似文献