Zygophyllum coccineum, an edible halophytic plant, is part of the traditional medicine chest in Mediterranean region for symptomatic relief diabetes, hypertension, wound healing, burns, infections, and rheumatoid arthritis pain. The current study aimed to characterize Z. coccineum phytoconstituents, evaluations anti-microbial-biofilm, anti-cancers bioactivities plant’s mother liquor, i.e., aqueous-ethanolic extract, its subsequent fractions. silico receptors interaction feasibility major...

After anaerobic incubation of arctiin (1) from the seeds Arctium lappa with a human fecal suspension, six metabolites were formed, and their structures identified as (-)-arctigenin (2), (2R,3R)-2-(3',4'-dihydroxybenzyl)-3-(3",4"-dimethoxybenzyl)butyrolactone (3), (2R,3R)-2-(3'-hydroxybenzyl)-3-(3",4"-dimethoxybenzyl)butyrolactone (4), (2R,3R)-2-(3'-hydroxybenzyl)-3-(3"-hydroxy-4"-methoxybenzyl)butyrolactone (5), (2R,3R)-2-(3'-hydroxybenzyl)-3-(3",4"-dihydroxybenzyl)butyrolactone (6),...

Lead structure discovery mainly focuses on the identification of noncovalently binding ligands. Covalent linkage, however, is an essential mechanism for a multitude successfully marketed drugs, although discovered by serendipity in most cases. We present concept design fragments covalently to proteases. linkage enables fragment unrelated affinity shallow protein sites and at same time allows differentiated targeted hit verification location through mass spectrometry. describe systematic...

The ostrich oil of Struthio camelus (Ratite) found uses in folk medicine as an anti-inflammatory eczema and contact dermatitis. effect a γ-lactone (5-hexyl-3H-furan-2-one) isolated from its formulated nano-emulsion formalin-induced paw edema was investigated this study. Ostrich saponified using standard procedure; the aqueous residue fractionated, purified, characterized through interpretation IR, NMR, MS analyses. methylcellulose (MC) for oral solubilized form. nanoparticles...

Abstract 8-Quinolinol reacts with cinnamonitrile derivatives in presence of a basic catalyst to afford pyrano[3,2-h]quinolines (3a–f). The reaction 3a reagents such as acetic anhydride/pyridine, formamide, formic acid/formamide, and carbon disulfide gave the fused heterotetracyclic systems pyrimido[4′,5′: 6,5]pyrano[3,2-h]quinolines.

Seventeen thiopaeonimetabolin-I adducts were obtained as mixtures of diastereoisomers after incubation paeoniflorin with Lactobacillius brevis in the presence various thiols. The anticonvulsant activity was investigated mice using maximal subcutaneous pentylenetetrazol seizure test and sodium valproate (1.5 mmol/kg) a positive control. Thirteen showed dose-dependent prolongation latencies clonic tonic convulsions. Maximal protection against convulsions effectively demonstrated by...

In a one pot procedure, 18 compounds of 7-(substituted phenyl)-2-substituted-6,7-dihydro-4H-[1,2,4]triazolo[1,5-a] pyrimidin-5-one derivatives (16-33) have been synthesized. 3(5)-Amino-5(3)-substituted-1,2,4-triazole (7-12) were used as synthomes which cyclo-condensed by fusion with substituted methyl cinnamate esters (13-15) to afford the target (16-33). an effort develop new non-nucleoside antiviral agents, 16-33 evaluated for their anti-HIV-1 and anti-HSV-1 activities. Complete inhibition...

Abstract 1‐Isopropyl‐4‐piperidone (1) reacts with sulphur and active methylene nitriles to give thienopyridines (2a‐c). Compounds 2a, b react CS 2 in pyridine produce pyridothienopyrimidines (3a, b) which upon methylation MeI S‐methylated derivatives (4a, b). Dibenzylidene compound (5) hydrazine hydrate, phenyl hydrazine, thiourea malononitrile or cyanoacetamide compounds 6–9 respectively. Piperidylidene (10) benzaldehyde derivative 11 undergoes an addition reaction 12 is also obtained by...

Abstract 3,5-Dibenzylidene-1-isopropy1-4-piperidinone (1) reacts with cyanothioacetamide to give 1,6-naphthyridine-2(1H) thione derivative 2. Reaction of 2 halo ketones or esters followed by ring closure gives thieno[2,3-b][1,6]naphthyridine derivatives 5a—i, which are used as versatile intermediates in the synthesis related heterocyclic systems pyrimidothienonaphthyridines 10, 11, 14, and 15, oxazinothienonaphthyridine (13) triazinothienonaphthyridine (9).

Seventeen thiopaeonimetabolin-I adducts were obtained as mixtures of diastereoisomers after incubation paeoniflorin with Lactobacillus brevis in the presence various thiols. Four compounds, 8-(n-hexylthio)- (8), 8-cyclopentylthio-, 8-(p-tolyl)thio- and 8-benzoylthio- (18) paeonimetabolins, showed 100% protection against pentylenetetrazole-induced convulsions at doses 0.125, 0.25, or 0.50 mmol/kg, relative to valproic acid (100% 1.5 mmol/kg). For 8 18, principle anticonvulsant activity...

A linear quantitative structure-activity relationship (QSAR) study that encodes various aspects of physicochemical, topological and electronic descriptors has been developed for a series 1,3,4-thiadiazole-2-thione derivatives (1a-r 2a-c). The carbonic anhydrase IX inhibitory activity the candidates under 2a-c) were correlated to selected parameters using stepwise regression analyses achieve best QSAR model. Promising results obtained with employed tetra-parametric model indicating...

Anaerobic incubation of phorbol (1) from Croton tiglium with human intestinal bacteria afforded five metabolites: isophorbol (2), deoxyphorbol (3), 4β,9α,20-trihydroxy-13,15-seco-1,6,15-tigliatriene-3,13-dione (4), 4β,9α,20-trihydroxy-15,16,17-trinor-1,6-tigliadiene-3,13-dione (5) and 4β,9α,20-trihydroxy-14(13→12)-abeo-12αH-1,6-tigliadiene-3,13-dione (6). All these metabolites (2—6) were identified characterized by spectroscopic means, including two-dimensional (2D)-NMR. Nine defined strains...

Paeoniflorin (1) and its derivatives having in common a cage-like pinane skeleton with hemiketal-acetal system, were evaluated for their effects on memory impairment induced by scopolamine mice using step-down type passive avoidance task. In the test session, 1 intraperitoneally (i.p.) administered at doses of 0.002, 0.01, 0.02 0.2 mmol/kg, 30 min later (15 before experiment), (1 mg/kg, i.p.) was given. These compounds showed dose-dependent attenuation dose range 0.002-0.02 mmol/kg also...

Forty-eight derivatives of phorbol (9) and isophorbol (14) were evaluated for their inhibition human immunodeficiency virus (HIV)-1 induced cytopathic effects (CPE) on MT-4 cells, as well activation protein kinase C (PKC), indices anti-HIV-1 tumor promoting activities, respectively. Of these compounds, the most potent CPE was observed in 12-O-tetradecanoylphorbol 13-acetate (8) 12-O-acetylphorbol 13-decanoate (6). The former also showed strongest PKC activity, while latter no activity at 10...

Griseofulvin 1 is an important antifungal agent that has recently received attention due to its antiproliferative activity in mammalian cancer cells. Study of SAR some griseofulvin analogues led the identification 2′-benzyloxy 3 , a more potent analogue which retards tumor growth through inhibition centrosomal clustering. However, similar compound exhibited poor aqueous solubility. In order improve water solubility, six new 5 – 10 were synthesized and tested for their The semicarbazone 9...

Anaerobic incubation of prednisone 1 with human intestinal bacteria (HIB) afforded nine metabolites: 5beta-androst-1-ene-3,11,17-trione 3, 3alpha-hydroxy-5alpha-androstane-11,17-dione 4, 3beta,17alpha,20-trihydroxy-5alpha-pregnan-11-one 5, 3alpha,17alpha-dihydroxy-5alpha-pregnane-11,20-dione 6, 3alpha,17alpha-dihydroxy-5beta-pregnane-11,20-dione 7, 3beta,17beta-dihydroxy-5alpha-androstan-11-one 8beta, 3beta,17alpha-dihydroxy-5alpha-androstan-11-one 8alpha,...

Abstract The reaction of 5-acetyl-8-quinolinol (1) and corresponding chalcone derivatives 2a–f with hydroxylamine hydrochloride in boiling pyridine gave the oximes 3 4a–f respectively almost quantitative yields. Further interaction 4a–e phenyl isocyanate and/or thiocyanate carbamate thiocarbamate (5a,b) (6a–e, 7a–e) were achieved. Metal chelates 1, 3, 4e,f bivalent metal cations like Fe(II), Cu(II), Zn(II) have been synthesized characterized by elemental IR-spectral analysis. compounds...