Antiviral activity of tetrahydro-2(1H)-pyrimidinones and related compounds

24 derivatives of tetrahydro-2(1H)-pyrimidinone and related compounds were tested in vitro for antiviral activity against representatives of six viral taxonomic groups. The screening was carried out by a two-stage procedure including the agar-diffusion plaque-inhibition test and the one-step growth cycle setup. A distinct activity of three mono- and bis-morpholinomethyl derivatives of tetrahydro-2(1H)-pyrimidinone (THP), 1,3-bis(piperidinomethyl)-THP, the 1-morpholinomethyl derivative of tetrahydro-2(1H)-pyrimidinethione (THPT) and the related N,N'-bis(morpholinomethyl)-urea against the fowl plague virus was established. In the one-step growth cycle setup these compounds inhibited 87.5-99.6% of the infectious virus yield. Two of the compounds, namely 1-morpholinomethyl derivatives of THP and THPT manifested a strong inhibitory effect on the reproduction of Semliki Forest virus as well, exceeding 99.9% in the one-step growth cycle test. A borderline effect was observed in some derivatives against vaccinia virus and Newcastle disease virus. The structure-activity relationship of this group of compounds is discussed.     

Antiviral activity of Bolivian plant extracts.

Ethanolic and aqueous extracts of seven plant species used in the traditional medicine of Bolivia have been tested for their antiviral activity against herpes simplex type I (HSV-1), vesicular stomatitis virus (VSV), and poliovirus type 1. The aqueous extracts of most of the species investigated showed antiviral activity. Two of these plants-namely, Satureja boliviana and Baccharis genistelloides-were active against two different viruses-HSV-1 and VSV.     

Biological activity and structure of antitumor compounds from Plantago media L

Tyrosine kinase inhibition and tumor growth inhibition activity of verbascoside and homoplantaginin are described. Both molecules proved to be equally significant inhibitors of isolated EGF-R tyrosine kinases, nevertheless their in vitro antiproliferative activity was variable in cellular assays. Their different inhibitory efficacies could be interpreted on the basis of conformational analysis and lipophilicity evaluation.     

Antiviral activity of amino derivatives of tricyclic compounds

Translated from Khimiko-farmatsevticheskii Zhurnal, No. 8, pp. 963–966, August, 1989.     

Evaluation of in vitro activity of aurones and related compounds against Cryptosporidium parvum.

The efficacy of a series of aurones, auronols and 4-methoxy-alpha-pyrones has been screened for the ability to inhibit the intracellular growth of the parasitic protist Cryptosporidium parvum using an in vitro enzyme linked immunosorbent assay (ELISA). All aurones of this series were active at 25 to 100 microM. 10 of 19 aurones inhibited the intracellular growth of C. parvum by > 90 % with moderate to no toxicity. The most active of these was 3',4',6-trihydroxy-2-[phenylmethylene]-3(2H)-benzofuranone.     

Inhibitory activity of Plantago major L. on angiotensin I-converting enzyme

Eight compounds were isolated from methanol extract of Plantago major L. leaves and investigated for their ability to inhibit angiotensin I-converting enzyme activity. Among them, compound 1 showed the most potent inhibition with rate of 28.06 ± 0.21% at a concentration of 100 μM. Compounds 2 and 8 exhibited weak activities. These results suggest that compound 1 might contribute to the ability of P. major to inhibit the activity of angiotensin I- converting enzyme.     

Antiviral activity of glycyrrhizin against varicella-zoster virus in vitro

One of the plant extracts, glycyrrhizin (GL) was investigated for its antiviral action on varicella-zoster virus (VZV) in vitro. When human embryonic fibroblast (HEF) cells were treated with GL after inoculation of virus (post-treatment), the average 50%-inhibitory dose (ID50) for five VZV strains was 0.71 mM, and the selectivity index (ratio of ID50 for host-cell DNA synthesis to ID50 for VZV replication) was 30. GL was also effective against VZV replication when HEF cells were treated 24 h before the inoculation (pretreatment). Furthermore, at a concentration of 2.4 mM GL inactivated more than 99% of virus particles within 30 min at 37 degrees C. In combination with other anti-herpes drugs (acyclovir, adenine arabinoside, bromovinyldeoxyuridine, and phosphonoformate) or human native beta-interferon, GL had an additive or slightly synergistic effect on VZV replication. The mechanism of anti-VZV action is still unclear. We postulate that GL inhibits the penetration, uncoating or release of virus particles.     

Antiviral activity of N-benzoylphenylisoserinates of Lactarius sesquiterpenoid alcohols in vitro

Cytotoxic, antiviral, antibacterial and antifungal properties of a new, originally synthesised group of compounds: the N-benzoylphenylisoserinates of sesquiterpenoid alcohols - derivatives of taxol and various sesquiterpenes of Lactarius origin were evaluated in vitro. Among 16 compounds tested, 6 decreased HSV-1 titres. Selectivity indices ranged from 13.9 to 31.7. No activity against RNA viruses (parainfluenza 3, Coxsackie B3, vesicular stomatitis virus, and encephalomyocarditis virus), bacteria: Escherichia coli, Proteus mirabilis, Staphylococcus aureus, Enterococcus faecium and Bacteroides fragilis and fungal strain of Candida albicans was detected.     

Antiviral and antiproliferative activity in vitro of some new benzimidazole derivatives

The antiviral and antiproliferative activity of new compounds having n-benzenesulphony 1-2 (2 or 3-pyridylethyl) benzimidazole as a base structure were studied in vitro. Their antitumour activity against human chronic myeloid leukaemia cells was evaluated and compared with that of equimolar doses of daunorubicin. Only compound 7a, with the presence of both the pyridyl moiety bound at the ethylenic bridge in C-2 of benzimidazole and the nitro-group in the benzene ring, displays a selective antiproliferative effect against certain leukaemia cells and a good antiviral activity especially towards the Coxsackie B5 virus. However, it should be noted that, in the case of hydroxybenzyl-benzimidazole, resistance also builds up to compound 7a, the Coxsackie B5 virus developing resistance to it after about ten runs. Cytotoxicity tests show that many of these substances are well tolerated by the VERO cells. The mechanism of action is still unclear.     

金银花及其复方的体外抑菌活性与体内抗炎作用

目的观察金银花及其复方仙方活命饮水提液对金黄色葡萄球菌、大肠埃希菌、枯草芽孢杆菌、白色念珠菌和黑曲霉的体外抑菌活性,探讨两者对小鼠抗炎作用及对炎性细胞的影响,并考察两者对小鼠免疫器官的影响。方法采用琼脂扩散法测定金银花及其复方仙方活命饮的水煎提取液对5种菌的抑菌能力。用试管二倍稀释法与平板涂布法结合确定药液对5种菌的最小抑菌浓度(MIC)。以二甲苯诱发的小鼠耳肿胀炎症作为急性炎症动物模型,进行抗炎作用研究。结果金黄色葡萄球菌、大肠埃希菌、枯草芽孢杆菌、白色念珠菌对金银花水提液与仙方活命饮水提液均敏感;黑曲霉对金银花水提液敏感,对仙方活命饮水提液不敏感。金银花水提液与仙方活命饮水提液,均能抑制二甲苯所致小鼠耳肿胀反应,提高小鼠脾脏指数,降低血清中白细胞介素-6与肿瘤坏死因子-α的含量。结论金银花及其复方仙方活命饮有抑菌、抗炎作用,且复方的功效强于单味药。     

Antibacterial activity of dipropofol and related compounds

Phenolic compounds, in general, exhibit antioxidant and antibacterial activities. We studied antimicrobial activity of the phenolic antioxidants, propofol (2,6-diisopropylphenol), tocopherol, eugenol, butylated hydroxyanisole (BHA), and several of their dimer compounds. Dipropofol (dimer of 2,6-diisopropylphenol) showed strong antibacterial activity against gram-positive strains including methicillin resistant Staphylococcus aureus (MRSA) and vancomycin resistant Enterococci (VRE), while propofol and other monomeric and dimeric phenols having methyl or tert-butyl groups showed no remarkable activity. The results indicated that the dimeric structure of 2,6-diisopropylphenol moiety may play an important role in the antibacterial activity.