The regioselective functionalization of terminal alkenes and alkynes is of utmost importance for the synthesis of a wide variety of organic products. Based on the original observation by Vladimir Markovnikov-the pioneer of this field of research-in the 19th century, the possible regioisomeric products are classified as Markovnikov or anti-Markovnikov products. Contrary to traditional belief, it is nowadays possible to control the regiochemistry of various additions of nucleophiles to alkenes and alkynes by applying different transition-metal catalysts. Recent developments in this area of selective functionalization of alkenes and alkynes are reviewed.

Catalytic Markovnikov and anti-Markovnikov functionalization of alkenes and alkynes: recent developments and trends.

Reaktionen zur selektiven Veredelung von Alkenen zahlen zu den wichtigsten Methoden in der Organischen Synthese. Durch die Entwicklung von Ubergangsmetallkatalysatoren in den letzten Jahrzehnten konnen heute alle Arten von Selektivitat bei einer Vielzahl von Transformationen effizient gesteuert werden. Auch 100 Jahre nach dem Tod von Vladimir Markownikow – dem Pionier auf diesem Gebiet – ist die regioselektive Funktionalisierung von Alkenen und Alkinen immer noch ein wichtiges Forschungsziel: Besonders die Anti-Markownikow-Addition von Sauerstoff- und Stickstoff-Nucleophilen an aliphatische Alkene und Alkine verfugt uber groses industrielles Potenzial. In diesem Aufsatz werden neuere Entwicklungen auf diesem Gebiet beschrieben. Eine Auswahl aktueller Beispiele zeigt, wie die Regioselektivitat durch die Wahl des Katalysators gesteuert werden kann.

Katalytische Markownikow‐ und Anti‐Markownikow‐Funktionalisierung von Alkenen und Alkinen

Corrosion inhibitors for iron in hydrochloride acid solution by newly synthesised pyridazine derivatives

Thermodynamic characterisation of steel corrosion and inhibitor adsorption of pyridazine compounds in 0.5 M H2SO4

Diabetes mellitus occurrence has been associated to the modification of the physiologicallevels of glucose and is often accompanied by several long-term complications, namely neuropathy,nephropathy, retinopathy, cataract, and cardiovascular Aldose reductase (AR) is an enzyme of aldoketoreductase super-family that catalyzes the conversion of glucose to sorbitol in the polyol pathwayof glucose metabolism In this context, aldose reductase inhibitors (ARIs) have received much attention worldwideDecreased sorbitol flux through polyol pathway by ARIs could be an emerging target for the management of majorcomplications of diabetes The present review article describes a brief overview of the role of aldose reductase in thediabetic complications, advances achieved on ARIs and their potential use in the treatment and management of the majordiabetic complications such as cataract, retinopathy, neuropathy, nephropathy and cardiovascular The ARIs developedvary structurally, and representative structural classes of ARIs include i) carboxylic acid derivatives (such as Epalrestat,Alrestatin, Zopalrestat, Zenarestat, Ponalrestat, Lidorestat, and Tolrestat), ii) spirohydantoins and related cyclic amides(such as Sorbinil, Minalrestat, and Fidarestat), and iii) phenolic derivatives (related to Benzopyran-4-one and Chalcone)Among these inhibitors, Epalrestat is the only commercially available inhibitor till date In addition, some other ARIssuch as Sorbinil and Ranirestat had been advanced into late stage of clinical trials and found to be safe for human use Therole of various natural ARIs in management of diabetic complications will be discussed Adapting ARIs could preventsepsis complications, prevent angiogenesis, ameliorate mild or asymptomatic diabetic cardiovascular autonomicneuropathy and appear to be a promising strategy for the treatment of endotoxemia and other ROS-induced inflammatorydiseases The role of ARIs in non-diabetic diseases will also be discussed

Updates on Aldose Reductase Inhibitors for Management of Diabetic Complications and Non-diabetic Diseases.

A series of 4,6-diaryl pyridazinones, chemically related to trazodone, ws synthesized and evaluated for analgesic activity. With ED50 values ranging from 8.4 to 46.7 mg kg(-1) i.p. in the phenylbenzoquinone-induced writhing test (PBQ test), most compounds were several times more potent than acetaminophen (ED50 = 231.3 mg kg(-1) i.p.) and noramidopyrine (ED50 = 68.5 mg kg(-1) i.p.). A multiple linear regression analysis demonstrated a correlation between antinociceptive activity and lipophilicity, as well as electronic and steric factors. The most active pyridazinones 2c and 2j exhibited minimal sedative and neurotoxic effects at the dose of 25 mg kg(-1) i.p. They were devoid of activity in the hot plate test and their analgesic activity was not significantly reversed by naloxone in the PBQ test. The antinociceptive response induced by morphine (0.15 mg kg(-1) s.c.) in the PBQ test was greatly potentiated by 2c and 2j administered at the low doses of 1 and 2.5 mg kg(-1) i.p., respectively. On the other hand, their analgesic effects were enhanced synergistically by 5-hydroxytryptophan combined with carbidopa. All these data imply that a significant part of the antinociceptive effect induced by 2c and 2j may involve both opioid and serotonergic pathways. In addition, these two pyridazinones did not exhibit any antidepressant properties in the forced swimming test, nor did they potentiate yohimbine-induced toxicity.

Synthesis and Trazodone-like Analgesic Activity of 4-Phenyl-6-aryl-2-[3-(4-arylpiperazin-1-yl)propyl]pyridazin-3-ones

Synthesis of pyridazine acetic acid derivatives possessing aldose reductase inhibitory activity and antioxidant properties

N -Acetic acid derivatives of 4-carboxy-6-arylpyridazin-3-ones were synthesized for the dual purpose of inhibiting aldose reductase and exhibiting antioxidant properties. All the prepared compounds showed a significant in vitro aldose reductase inhibitory effect (10 −5 M ≤ IC 50 ≤ 10 −4 M). The spatial configuration of the most active derivative 4f (4- i -PrC 6 H 4 at C 6 , IC 50 = 0 95 × 10 −5 M) was compared with pharmacophore requirements of the aldose reductase inhibitor site using a molecular modeling system. The antioxidant action of 4a–f was also studied in vitro . Compound 4c (4-ClC 6 H 4 at C 6 , IC 50 = 1.56 × 10 −3 M) was the most effective at scavenging the superoxide anion whereas compound 4a (C 6 H 5 at C 6 , IC 50 = 1.28 × 10 −3 M) was the most active at inhibiting lipid peroxidation. In addition, biological activities (log 1/IC 50 ) for most of the data sets could be correlated directly to lipophilic, electronic and steric parameters.

Synthesis of Pyridazine Acetic Acid Derivatives Possessing Aldose Reductase Inhibitory Activity and Antioxidant Properties.

A series of 3-arylpiperazinyl-5-benzyl-pyridazines was synthesized and evaluated for analgesic activity. The structures of these new pyridazine derivatives were confirmed by IR, 'H-NMR spectra and by elementary analysis. With ED 50 values ranging from 6.0 to 71.5 mg/kg i.p. most of the compounds were several times more potent than acetaminophen (ED 50 = 228.6 mg/kg i.p.) and noramidopyrine (ED 50 = 68.8 mg/kg i.p.) in the phenylbenzoquinone-induced writhing test (PBQ-test). Quantitative structure-activity relationships were accomplished by a Hansch analysis. The most active pyridazines 2h-j exhibited sedative properties from the dose of 25 mg/kg i.p. Their lack of activity in the hot plate test was in favour of peripherally acting agents. In the PBQ test, analgesic activity of 2h-j was not antagonized by naloxone. However, their antinociceptive effect added up to those of 5-hydroxytryptophan when given in association with carbidopa. These results demonstrated that analgesic properties of pyridazine derivatives might involve a serotonergic pathway without interaction with opioidergic systems.

Synthesis of peripherally acting analgesic 3-arylpiperazinyl-5-benzyl-pyridazines

Synthesis and Trazodone‐Like Analgesic Activity of 4‐Phenyl‐6‐aryl‐2‐( 3‐(4‐arylpiperazin‐1‐yl)propyl)pyridazin‐3‐ones.

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