Effects of rigor temperature and electrical stimulation on venison quality.

The effects of rigor temperature and electrical stimulation on venison quality were assessed using venison longissimus dorsi muscle. In the first trial, effect of rigor temperature (0, 15, 25, 30, 35 and 42°C) and time post-mortem (at rigor, 3, 7 and 14 days) on drip and cooking losses, % expressible water (water holding capacity, WHC), sarcomere length, protein solubility, meat tenderness and colour were investigated. In the second trial, the effects of rigor temperature (15 and 35°C), electric stimulation (stimulated or not stimulated) and time (at rigor, 3 and 6 weeks post-mortem) on tenderness and colour were further investigated.

Post-mortem metmyoglobin reduction in fresh venison.

The accumulation of metmyoglobin (MetMb) at the surface of meat during storage contributes significantly to its discolouration. Under appropriate conditions it may be possible to utilise residual meat MetMb reducing activity to maintain fresh colour. Venison meat colour stability is poorer compared with other species.

Evaluation of apoptosis-induction by newly synthesized phthalazine derivatives in breast cancer cell lines.

Newly synthesized phthalazine derivatives including copper and platinum complexes were evaluated for cytotoxicity in human breast cancer cell lines. The cells were incubated with the compounds (100 microM) for 72 h and cytotoxicity, apoptosis and DNA content were measured by flow cytometery. Our results suggest that the parent (H1-2), copper (C1-2)- and platinum (P1-2)-derivatized compounds were relatively more active in inducing apoptosis and cell killing in both human breast cancer cell lines, MDA-MB-231 cells being the more sensitive.

Synthesis and biological evaluation of some hydroxypyrazole derivatives as anti-inflammatory-antimicrobial agents.

Some hydroxypyrazole derivatives 2-7 were synthesized by cyclocondensation of the keto-ester 1 with hydrazines hydrate or substituted hydrazines followed by reduction and acylation with acetic anhydride or trifluoroacetic anhydride. The newly synthesized compounds were evaluated for their anti-inflammatory, antimicrobial activities. In addition, the ulcerogenic and acute toxicity profiles were determined.

Synthesis of 3-benzyl-2-substituted quinoxalines as novel monoamine oxidase A inhibitors.

A new series of 3-benzyl-2-substituted quinoxalines have been synthesized by means of microwave enhancement of nucleophilic substitution reaction involving the corresponding 2-chloroquinoxaline analogs and substituted amines or hydrazine. The synthesized compounds were evaluated for their monoamine oxidase A and B inhibitory activity by determination of their IC(50). All the newly synthesized compounds showed more selective inhibitory activity toward MAO-A than MAO-B.

Metmyoglobin reducing activity.

Meat colour is a major factor that influences the purchase decision by consumers. Many intrinsic and extrinsic factors contribute to the final colour of meat. The role of the MetMb reducing system in maintaining meat colour has been controversial and a considerable amount of work has been published since [Giddings, G.

Effect of pyrazoloquinoline derivatives on the growth of Leishmania donovani promastigotes.

A screening study was conducted to examine the effect of a series of synthesized pyrazoloquinoline derivatives on the growth of Leishmania donovani promastigotes. Sixteen compounds were tested, ten of which showed an inhibitory effect on the growth of promastigotes. Compound 1 demonstrated potent antileishmanial activity, followed by compounds 3 and 7.

Effect of calcium chloride, zinc chloride, and water infusion on metmyoglobin reducing activity and fresh lamb color.

Calcium chloride (CaCl2), zinc chloride (ZnCl2), or water infusions were used to investigate the biochemical factors that affect fresh lamb color, and to examine the role of metmyoglobin-reducing activity in regulating this important quality attribute. Immediately after exsanguination, lamb carcasses (n = 6 per treatment) were infused (10% of BW) with 0.3 M CaCl2, 0.

Novel milrinone analogs of pyridine-3-carbonitrile derivatives as promising cardiotonic agents.

In an attempt to design new inotropic drugs for congestive heart failure (CHF) with less proarrhythmic potential, three series of compounds analogous to milrinone were prepared, namely, 4-aryl-6-(4-pyridyl)-2-oxo-1,2-dihydropyridine-3-carbonitriles 2a-g, 4-aryl-6-(4-pyridyl)-2-thioxo-1,2-dihydropyridine-3-carbonitriles 3a-g and 2-amino-4-aryl-6-(4-pyridyl)-pyridine-3-carbonitriles 4a-g. The first series was prepared by reacting 4-acetyl pyridine with the appropriate aldehyde, ethyl cyanoacetate and ammonium acetate in ethanol. Reaction of 2a-g with phosphorus pentasulfide afforded the second series 3a-g.

Novel pyrazole derivatives as potential promising anti-inflammatory antimicrobial agents.

Four series of 1H-pyrazole derivatives have been synthesized. The first series was synthesized starting by condensing the hydrazine derivatives 1a-d with 4-(1-ethoxycarbonyl-2-oxopropyl)azobenzoic acid 2a in ethanol or glacial acetic acid to generate the corresponding pyrazoline derivatives 3a-d. Likewise, heating 1a-d with 4-(1-acetyl-2-oxopropyl)azobenzoic acid 2b gave rise to the pyrazole derivatives 4a-d.

Evaluation of some pyrazoloquinolines as inhibitors of herpes simplex virus type 1 replication.

Three structurally related aminopyrazoloquinoline derivatives were evaluated for their antiviral activity against Herpes Simplex virus type 1. These compounds were examined for their in vitro antiviral activity by two different bioassays, namely; crystal violet staining and tetrazolium dye (MTS) measurement. The antiviral role of these compounds was confirmed by enumerating the infectious particles with plaque assay.

Up- and down-regulation of longissimus tenderness parallels changes in the myofibril-bound calpain 3 protein.

The objective of this study was to utilize Ca(2+) and Zn(2+) treatments of meat to critically explore the possible role of calpain 3 in meat tenderisation. Calpains 1 and 2 were also examined for comparative purpose. Control animals plus animals infused with CaCl(2), ZnCl(2) or H(2)O were used (six lambs per treatment) to determine the temporal changes in muscle calpain 3 protein in the Longissimus thoracis et lumborum (LTL) during post-mortem storage.

Synthesis of aldehydo-sugar derivatives of pyrazoloquinoline as inhibitors of herpes simplex virus type 1 replication.

Synthesis of a novel series of structurally related pyrazoloquinoline nucleosides is described. All the newly synthesized compounds were examined for their in vitro antiviral activity against herpes simplex type-1 as shown by two different bioassays, namely; crystal violet staining or the MTS tetrazolium dye measurement. The acute toxicity (LD50) values of the biologically active compounds were determined.

Synthesis, characterization and cytotoxicity evaluation of some new platinum(II) complexes of tetrazolo[1,5-a]quinolines.

Several new platinum(II) complexes of the general formulae cis-[PtCl(2)(DMSO)L], where L is a Schiff base or hydrazone derived from tetrazolo[1,5-a]quinoline-4-carboxaldehyde as carrier ligands, have been synthesized and characterized physicochemically and spectroscopically. These platinum complexes which are structurally analogues to what so called cisplatin [cis-[PtCl2(NH3)2]; the first generation anticancer agent] were evaluated for their cytotoxicity on HL-60 (human promyelocytic leukemia) cells. Two of the platinum complexes were almost similar in their activity to cisplatin, while the remaining three complexes have demonstrated higher efficacy than that of cisplatin.

Synthesis of some thiazolyl and thiadiazolyl derivatives of 4(3H)-quinazolinone as anti-inflammatory-antimicrobial agents.

This paper describes the synthesis of four series of 4(3H)-quinazolinone derivatives. The first series was prepared by cyclization of the intermediate 3-aryl-2-substituted thiocarbamoylhydrazonomethyl-4(3H)-quinazolinones 2a,b with ethyl bromoacetate to afford the corresponding thiazolidinonyl derivatives 3a,b. The second series were prepared by the cyclization of the intermediate 2a,b with phenacyl bromide or 4-substituted phenacyl bromide giving rise to thiazolinyl derivatives 4a-f.

Tetrazolo[1,5-a]quinoline as a potential promising new scaffold for the synthesis of novel anti-inflammatory and antibacterial agents.

Three series of tetrazolo[1,5-a]quinoline derivatives have been synthesized. The first series was synthesized starting by the condensation of tetrazolo[1,5-a]quinoline-4-carboxaldehyde 2 with substituted thiosemicarbazides, followed by cyclization of the resulting thiosemicarbazones 3 with malonic acid in the presence of acetyl chloride to give pyrimidyl derivatives 4a-c. The second series was prepared by the condensation of the latter compounds 4a-c with the selected aromatic aldehydes to afford the arylidene derivatives 5a-f.

Design, synthesis and biological evaluation of some pyrazole derivatives as anti-inflammatory-antimicrobial agents.

The synthesis of novel series of structurally related 1H-pyrazolyl derivatives is described. All the newly synthesized compounds were tested for their in vivo anti-inflammatory activity by two different bioassays namely; cotton pellet-induced granuloma and sponge implantation model of inflammation in rats. In addition, COX-1 and COX-2 inhibitory activities, ulcerogenic effects and acute toxicity were determined.

The relationship between meat tenderization, myofibril fragmentation and autolysis of calpain 3 during post-mortem aging.

The objective was to study the potential role of calpain 3 in postmortem myofibril breakdown and meat tenderization. We determined the temporal changes in calpain 3 protein in the ovine m. longissimus thoracis et lumborum (LTL, n=4) during post-mortem storage.

Does the newly discovered calpain 10 play a role in meat tenderization during post-mortem storage?

The objective was to study calpain 10 during meat tenderization. Western assays were developed and changes in calpain 10, tenderization level and desmin were determined in Longissimui (LTL) during post-mortem storage. A comparison between some characteristics of calpains 1, 2 and 10 indicated differences in the pI and sub-cellular distribution.

Synthesis and biological evaluation of some new substituted naphthoquinones.

Two novel series of 1,4-naphthoquinone derivatives have been synthesized namely; N-ethoxycarbonyl-2-ethoxycarbonyloxy-3- alkyl-1,4-naphthoquinon-1-substituted phenylhydrazones 3a-f and 2-chlorocetyloxy-3-alkyl-1,4-naphthoquinone-1-substituted phenylhydrazones 4a-d. The antimicrobial activity as well as anticancer activity of these compounds have been evaluated. The acute toxicity of the active compounds was determined.

Particulate metmyoglobin reducing activity and its relationship with meat color.

There is controversy about the effect of storage time on metmyoglobin (MetMb) reducing activity in the sarcoplasmic fraction of meat and the role of this reducing activity in maintaining the color of red meat. The presence of metmyoglobin reducing activity in the myofibrillar fraction of muscle extracts was investigated as a possible reason for this controversy. NADH-dependent MetMb reducing activity was found in the particulate fraction of meat following sedimentation of a meat homogenate at 35 000g.

Design and synthesis of some substituted 1H-pyrazolyl-oxazolidines or 1H-pyrazolyl-thiazolidines as anti-inflammatory-antimicrobial agents.

Four series of 1 H-pyrazole derivatives have been synthesized. The first series was synthesized starting with the reaction of 3-(5-bromo-2-thienyl)-1-phenyl-1 H-pyrazole-4-carboxaldehyde 1 with L-serine, L-cysteine, or L-penicillamine, followed by N-protection using (Boc)(2)O to provide compounds 2. The latter compounds could be N-deprotected by 4N HCl/dioxane to afford the second series 3 or reacted with NH(4)OH in the presence of DCC/HOBt to give the corresponding amides 4 followed by N-deprotection giving rise to compounds 5.

Design and synthesis of some substituted 1H-pyrazolyl-thiazolo[4,5-d]pyrimidines as anti-inflammatory-antimicrobial Agents.

The synthesis of two novel series of structurally related 1H-pyrazolyl derivatives of thiazolo[4,5-d]pyrimidines is described. All the newly synthesised compounds were examined for their in vivo anti-inflammatory activity in two different bioassays namely; cotton pellet-induced granuloma and carrageenan-induced paw edema in rats. The in vitro inhibitory activity of the most active compounds towards human COX-1 and COX-2 enzymes was also estimated.

Synthesis of some new bis-thiazoles as possible anticancer agents.

Several new 5-(2,3-dihydrothiazol-2-yledinyl)rhodanines 3a-c and 5-(4-oxothiazolidinon-2-ylidenyl)rhodanine 4 were synthesized through the reaction of 5-thiocarbamoyl rhodanines 2 with phenacyl bromides or chloroacetic acid, respectively. The synthesis of the arylidene derivatives 5a-c were also described. The 5-(4-amino-5-cyano-2,3-dihydrothiazol-2-yledinyl)rhodanines 10a, b were obtained through reaction of rhodanines 1a, b with thiazolium salt 9.

Thioglycolic acid and pyrazole derivatives of 4(3H)-quinazolinone: synthesis and antimicrobial evaluation.

New derivatives of 4(3H)-quinazolinone were synthesized and evaluated for their antibacterial and antifungal activity. The derivatives are: 3-Aryl-2-[3-aryl-1-(carboxymethylthio)-3-oxopropyl)]-4(3H)-quinazolinones 2a-f; 3-Aryl-2-(3-aryl-1H-pyrazol-5-yl)-4(3H)-quinazolinones 3a-f; 3-Aryl-2-(1,3-diaryl-1H-pyrazol-5-yl)-4(3H)-quinazolinones 4a-f; 3-Aryl-2-(3-aryl-1-thiocarbamoyl-1H-pyrazol-5-yl)-4(3H)-quinazolinones 5a-f; 3-Aryl-2-[3-aryl-1-(carboxymethylthio)-3-hydroxyiminopropyl)]-4(3H)- quinazolinones 6a-f; and 3-Aryl-2-[3-aryl-1-(carboxymethy- lthio)-3-thiocarbamoyliminopropyl)]-4(3H)-quinazolinones 7a-f. Some of the tested compounds showed activity comparable to that of the standard references used.