Potential neurotropic and antiinflammatory agents: 2-Chloro-10,11-dihydrodibenzo[b,f]thiepin-10-yl sulfides

1989 ◽  
Vol 54 (5) ◽  
pp. 1403-1421 ◽  
Author(s):  
Vladimír Valenta ◽  
Marie Vlková ◽  
Miroslav Protiva
Keyword(s):  
Sodium Salt ◽  
Primary Amine ◽  
Antimicrobial Activities ◽  
The Other ◽  
Ethyl Chloroformate ◽  
Acid Chlorides ◽  
Ethyl Chloroacetate ◽  
Antiinflammatory Agents

2-Chloro-10,11-dihydrodibenzo[b,f]thiepin-10-thiol (VII) was synthesized from 2,10-dichloro-10,11-dihydrodibenzo[b,f]thiepin (IV) and was alkylated with a series of aminoalkyl chlorides which led to amino sulfides IX, XII, XIII, and XVI-XX. The primary amine IXa was transformed by treatment with ethyl chloroformate to the carbamate Xa which was reduced to the methylamino compound XIa. The carbamate XX was similarly reduced to compound XXI. Alkylation of VII with 2-bromoethanol gave the alcohol XIVa which was transformed to the crude tosylate XVa. Its reactions with the corresponding piperazines gave compounds XXII to XXIV. The alcohol XXII was esterified to the decanoate XXV. Reactions of the sodium salt of VII with ethyl chloroacetate, ethyl 2-chloropropionate and ethyl 4-chlorobutyrate gave the corresponding esters which were saponified to acids XXVIb-XXVIIIb. Their amides XXVId to XXVIIId and XXVIe were prepared either via the acid chlorides or via the esters. Out of the compounds prepared only XIa showed a clear profile of a potential antidepressant. The other compounds showed indications of thymoleptic, antiinflammatory and antimicrobial activities.

Amphiphilic cationic copolymers with ciprofloxacin: preparation and antimicrobial activities

2016 ◽  
Vol 40 (2) ◽  
pp. 1354-1364 ◽  
Author(s):  
Man He ◽  
Yuming Zhou ◽  
Huining Xiao ◽  
Peng Lu
Keyword(s):  
Primary Amine ◽  
Cellulose Fibers ◽  
Antimicrobial Activities ◽  
Amine Salt ◽  
Amphiphilic Copolymers ◽  
Cationic Copolymers

Amphiphilic copolymers with ciprofloxacin and primary amine salt copolymers applied to cellulose fibers showed excellent antimicrobial activities.

Induction of antimicrobial peptides from Rana dybowskii under Rana grylio virus stress, and bioactivity analysis

2012 ◽  
Vol 58 (7) ◽  
pp. 848-855 ◽  
Author(s):  
Shu-Jing Yang ◽  
Xiang-Hong Xiao ◽  
Yi-Gang Xu ◽  
Dan-Dan Li ◽  
Long-Hui Chai ◽  
...  
Keyword(s):  
Antimicrobial Peptides ◽  
Antimicrobial Activities ◽  
The Other ◽  
Degenerate Primers ◽  
Cdna Sequences ◽  
Gram Positive Bacteria ◽  
Pathogen Invasion ◽  
Peptide Precursors ◽  
Rana Dybowskii

The skin glands of Ranidae are a rich source of antimicrobial peptides. In this study, the genomic RNA of Rana dybowskii was extracted from its skin while under Rana grylio virus stress. Five new cDNA sequences encoding 5 mature peptides, Ranatuerin-2YJ (GLMDIFKVAVNKLLAAGMNKPRCKAAHC), Dybowskin-YJb (IIPLPLGYFAKKP), Dybowskin-YJa (IIPLPLGYFAKKKKKKDPVPLDQ), Temperin-YJa (VLPLLETCSMTCWENNQTFGK), and Temperin-YJb (VLPLVGNLLNDLLGK), were obtained by reverse transcription polymerase chain reaction with a pair of degenerate primers designed according to the conserved terminal sequences of cDNA encoding antimicrobial peptide precursors of genus Rana. The antimicrobial activities of the peptides were analyzed, and the results demonstrated that all these peptides showed a significant anti-Rana grylio virus activity, and the virus was gradually cleared with the increase in gene expression. Among the 5 peptides obtained in this work, Ranatuerin-2YJ also showed a broad-spectrum anti-Gram-positive bacteria and anti-Gram-negative bacteria activity with a minimal inhibitory concentration of 22.5 µg/mL and 7.64% hemolysis activity, both of which were significantly lower (p < 0.05) than that of the other peptides. Moreover, Ranatuerin-2YJ was widely distributed in the skin, liver, spleen, and blood of R. dybowskii, while the other 4 peptides could only be cloned from the skin, indicating that the Ranatuerin-2YJ in vivo plays an important role in the protection against pathogen invasion.

Synthesis of Novel Macrocyclic Peptido-calix[4]arenes and Peptidopyridines as Precursors for Potential Molecular Metallacages, Chemosensors and Biologically Active Candidates

2006 ◽  
Vol 61 (11) ◽  
pp. 1335-1345 ◽  
Author(s):  
Abd El-Galil El-Sayed Amr ◽  
Mohamed Abo-Ghalia ◽  
Mohamed M. Abdalah
Keyword(s):  
Dipicolinic Acid ◽  
Antimicrobial Activities ◽  
Biologically Active ◽  
Hybrid Structures ◽  
Ethyl Chloroformate ◽  
Acylating Agent ◽  
Acid Acid ◽  
Structure Assignment ◽  
New Compounds ◽  
Upper Rim

Novel macrocyclic dipicolinic acid acylated peptides based on upper rim bridged peptidocalix[ 4]arenes, peptido-pyridines or hybrid structures of both, were synthesized as potential molecular metallacages and chemosensors. While conventional azide or mixed anhydride (ethyl chloroformate) peptide couplings served well for assembling the L-tyrosine or L-ornithine peptide backbones, the acid chloride of pyridine-2,6-dicarboxylic acid (dipicolinic acid) acid served as the complementary acylating agent. The structure assignment of the new compounds was based on chemical and spectroscopic evidences. Some of these compounds exhibit antimicrobial activities.

scholarly journals Flowering Response of Bougainvillea Cultivars to Dikegulac

HortScience ◽  
1994 ◽  
Vol 29 (4) ◽  
pp. 282-284 ◽  
Author(s):  
J.G. Norcini ◽  
J.H. Aldrich ◽  
J.M. McDowell
Keyword(s):  
Sodium Salt ◽  
Growth Habit ◽  
Foliar Spray ◽  
Late Summer ◽  
Early Summer ◽  
Late Spring ◽  
The Other ◽  
Spray Application ◽  
Flowering Response ◽  
Bougainvillea Glabra

Foliar spray application of dikegulac at 1600 mg·liter-1 during production of Bougainvillea glabra Choicy `Mauna Kea White', and Bougainvillea `Raspberry Ice', `Royal Purple', `Summer Snow', and `Temple Fire' in 4.5-liter hanging baskets (25.4 cm in diameter) was investigated in relation to flowering. The effect of foliar-applied dikegulac at 0, 400, 800, 1200, and 1600 mg·liter-1 on bracteole size of `Mauna Kea White' was also determined. Liners of `Temple Fire' pruned at transplanting (0 weeks) and sprayed with dikegulac at, 0 and 4 weeks had increased flowering and a slightly more compact, pendulous growth habit than plants that had only been pruned at 0 and 4 weeks. Dikegulac had little to no effect on flowering of the other cultivars. Under late-spring to early summer conditions (generally increasing temperatures), bracteole size of `Mauna Kea White' was reduced ≈25 % by 400 mg dikegulac/liter compared to nontreated plants; 800 to 1600 mg dikegulac/liter reduced bracteole size ≈37%. Under late-summer to mid-fall conditions when the weather was cooler and wetter, dikegulac had little to no effect on bracteole size; however, bracteoles of nontreated plants were ≈25% smaller than those of plants grown under the warmer and drier conditions of late spring to early summer. Chemical name used: sodium salt of 2,3:4,6-bis -O- (1-methylethylidene) -α-l-xylo- 2-hexulofuranosonic acid (dikegulac).

scholarly journals Green propolis as an adjuvant against nontuberculous mycobacteria

Rodriguésia ◽  
2021 ◽  
Vol 72 ◽  
Author(s):  
Suzane Olachea Allend ◽  
Lisiane Volcão ◽  
Carolina da Silva Canielles ◽  
Israel Barbosa ◽  
Dara Biatobock ◽  
...  
Keyword(s):  
Antimicrobial Activity ◽  
Nontuberculous Mycobacteria ◽  
Ethanol Extract ◽  
Antimycobacterial Activity ◽  
Antimicrobial Activities ◽  
Resistance Mechanisms ◽  
The Other ◽  
New Drugs ◽  
Mycobacterium Chelonae

Abstract Natural products have been touted as important tools because of their vast potential for the development of compounds with antimicrobial activity and the possible inhibitory activity and/or adjuvant resistance mechanisms. Propolis has been empirically used for many years for the treatment of diseases, mainly due to its antioxidant, anti inflammatory and antimicrobial activities. This study aimed to evaluate the in vitro antimycobacterial activity of the ethanol extract of propolis alone and in combination with rifampicin (RIF), amikacin (AMI) and ciprofloxacin (CIP). The ethanol extract of propolis showed antibacterial activity against Mycobacterium chelonae and M. kansasii and was capable of increasing AMI, RIF and CIP activity in combination. On the other hand, compared to M. absecessus, M. fortuitum and M. avium, the extract was not active at 200 µg/mL and did not show pronounced adjuvant capacity when evaluated in association with the drugs. Based on these results, it can be concluded that the ethanol extract of propolis could be an alternative in the development of new drugs and can be used complementary with the current mycobacteriosis treatment.

scholarly journals Fusarium Cyclodepsipeptide Mycotoxins: Chemistry, Biosynthesis, and Occurrence

Toxins ◽  
2020 ◽  
Vol 12 (12) ◽  
pp. 765
Author(s):  
Monika Urbaniak ◽  
Agnieszka Waśkiewicz ◽  
Łukasz Stępień
Keyword(s):  
Drug Discovery ◽  
Secondary Metabolism ◽  
Fusarium Species ◽  
Animal Health ◽  
Antimicrobial Activities ◽  
The Other ◽  
Cancer Drugs ◽  
Anti Cancer ◽  
The World ◽  
Vegetables And Fruits

Most of the fungi from the Fusarium genus are pathogenic to cereals, vegetables, and fruits and the products of their secondary metabolism mycotoxins may accumulate in foods and feeds. Non-ribosomal cyclodepsipeptides are one of the main mycotoxin groups and include beauvericins (BEAs), enniatins (ENNs), and beauvenniatins (BEAEs). When ingested, even small amounts of these metabolites significantly affect human and animal health. On the other hand, in view of their antimicrobial activities and cytotoxicity, they may be used as components in drug discovery and processing and are considered as suitable candidates for anti-cancer drugs. Therefore, it is crucial to expand the existing knowledge about cyclodepsipeptides and to search for new analogues of these compounds. The present manuscript aimed to highlight the extensive variability of cyclodepsipeptides by describing chemistry, biosynthesis, and occurrence of BEAs, ENNs, and BEAEs in foods and feeds. Moreover, the co-occurrence of Fusarium species was compared to the amounts of toxins in crops, vegetables, and fruits from different regions of the world.

Bioactivity of Lignans from Taxus baccata

2004 ◽  
Vol 59 (7-8) ◽  
pp. 494-498 ◽  
Author(s):  
Nurgun Erdemoglu ◽  
Bilge Sener ◽  
M. Iqbal Choudhary
Keyword(s):  
Antibacterial Activity ◽  
Cell Line ◽  
Ethanol Extract ◽  
Antimicrobial Activities ◽  
Chloroform Extract ◽  
The Other ◽  
Bovine Aortic Endothelial Cell ◽  
Taxus Baccata ◽  
Reference Drug ◽  
Cell Line Panel

AbstractThree lignan derivatives, (-)-taxiresinol (1), (-)-3′-demethylisolariciresinol-9′-hydroxyisopropylether (2) and (-)-3-demethylisolariciresinol (3), previously isolated from the heartwood of Taxus baccata L. (Taxaceae) were investigated for cytotoxicity against the Oncology Cell Line Panel (breast, colon, ovary, prostate, lung and a normal adult bovine aortic endothelial cell line) as well as for antimicrobial activities. Besides, a chloroform-soluble portion of the ethanol extract from the heartwood of T. baccata was also tested for antimicrobial activities. Compounds 1 - 3 did not demonstrate much cytotoxic potency according to the reference drug etoposide. With the exception of compound 2, the other two lignans (1 and 3) and the chloroform extract were shown to possess antifungal activity, whereas only the chloroform extract exhibited antibacterial activity against Pseudomonas aeruginosa

The action of local hormones

1950 ◽  
Vol 137 (888) ◽  
pp. 292-300 ◽  
Keyword(s):  
Primary Amine ◽  
General Circulation ◽  
Sympathetic Nerves ◽  
Blood Stream ◽  
The Other ◽  
Adrenergic Nerves ◽  
Important Advance ◽  
Unknown Substance ◽  
Stimulation Of

In order to account for the resemblance between the actions of sympathetic nerves and those of adrenaline, Elliott (1904) suggested that sympathetic nerves might act by liberating adrenaline. Discussing this theory Barger & Dale (1910) came to the conclusion that the actions of sympathetic nerves did not resemble those of adrenaline so closely as they did those of the corresponding primary amine now known as noradrenaline. Loewi’s demonstration that some sympathetic nerves do actually liberate a substance like adrenaline was published in 1921. Cannon & Rosenblueth (1937) obtained evidence that stimulation of the sympathetic nerves in a cat led to the liberation into the blood stream of a variable mixture of two substances. They supposed that one of those substances had purely excitor effects and the other purely inhibitor effects, and they called them sympathin E and sympathin I. The discovery that two substances were involved was an important advance, but it now seems likely that the two substances are adrenaline and noradrenaline, and since neither of these has purely excitor or purely inhibitor effects the terms sympathin E and Sympathin I should be forgotten. The word sympathin is a convenient label for the substances specifically liberated by adrenergic nerves and may perhaps survive with this meaning. The reason for the slow advance of knowledge about these substances is that the quantities available for study are small. The evidence is still almost entirely pharmacological, since no other methods are sensitive enough. The distinction between adrenaline and noradrenaline has depended on the use of parallel quantitative tests using tissues with different values for the ratio of the activities of these two drugs. If the unknown substance is adrenaline it should match the same amount of adrenaline by any test. It was by using this criterion and studying the effect on distant organs of substances liberated into the general circulation that Cannon & Rosenblueth showed that adrenaline was not the only substance liberated. Their results were such as might be produced by the liberation of a mixture of adrenaline and noradrenaline, but they did not adopt this explanation which was first published by Bacq (1933).

scholarly journals EFFECTS OF INDOMETHACIN AND THE OTHER ANTIINFLAMMATORY AGENTS ON ACTIVATION OF DORSAL HORN CELL IN THE SPINAL CORD INDUCED BY INTRA-ARTERIAL INJECTION OF BRADYKININ

1976 ◽  
Vol 26 (3) ◽  
pp. 309-314 ◽  
Author(s):  
Masamichi SATOH ◽  
Takayuki DOI ◽  
Kazuo KAWASAKI ◽  
Akinori AKAIKE ◽  
Hiroshi TAKAGI
Keyword(s):  
Spinal Cord ◽  
Dorsal Horn ◽  
The Other ◽  
Antiinflammatory Agents

Comparative Merits of Two Topical Corticosteroid-Antimicrobial Drugs

1981 ◽  
Vol 9 (6) ◽  
pp. 453-458 ◽  
Author(s):  
J Barba-Rubio ◽  
G Calle-Vélez ◽  
L Dommguez-Soto ◽  
F Londoño
Keyword(s):  
Topical Corticosteroid ◽  
Antimicrobial Activities ◽  
The Other ◽  
Betamethasone Valerate ◽  
Parallel Study ◽  
Antimicrobial Drugs ◽  
Clinical Assessments ◽  
Local Irritation ◽  
Cutaneous Candidiasis ◽  
Therapeutic Responses

The anti-inflammatory and antimicrobial activities of two topical creams, one containing halcinonide, neomycin and nystatin (HNN), and the other betamethasone valerate, gentamicin, iodochlorhydroxyquin and tolnaftate (BGI), were compared in a randomized, parallel study of 154 patients (eighty-seven secondarily infected ecematous dermatoses; sixty-seven cutaneous candidiasis). Repeated clinical assessments showed that the two creams produced equivalent therapeutic responses both in patients with infected eczematous lesions and candidiasis. HNN and BGI creams eradicated the bacterial pathogens isolated prior to treatment in 80% and 76%, respectively, of the patients with eczematous dermatoses. The organism most frequently isolated in these patients was S. aureus. Local irritation prompting discontinuance of therapy occurred in just one patient receiving HNN, and two patients receiving BGI.

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