The influence of ischemia–reperfusion (I/R) action on pancreatic blood flow (PBF) and the development of acute pancreatitis (AP) in laboratory rats is evaluated in vivo by using the laser speckle ...contrast imaging (LSCI). Additionally, the optical properties in norm and under condition of AP in rats were assessed using a modified integrating sphere spectrometer and inverse Monte Carlo (IMC) software. The results of the experimental study of microcirculation of the pancreas in 82 rats in the ischemic model are presented. The data obtained confirm the fact that local ischemia and changes in the blood flow velocity of the main vessels cause and provoke acute pancreatitis.
Fused 2-amino-3-cyano-4
H
-pyrans were synthesized by the tandem Knoevenagel—Michael reaction. A previously unknown version of the ring opening of 2-amino-3-cyano-4
H
-pyrans giving substituted ...2,6-dicyanoaniline was discovered. The structure of the latter compound was established by X-ray diffraction.
The multicomponent condensation of cyclopentylidene- or cyclohexylidenemalononitrile, cyanoacetic acid amides or thioamides, and alkylating agents affords 4-spirocyclopentane- and ...4-spirocyclohexanenicotinic acid nitriles and amides. The structures of several reaction products were determined by X-ray diffraction.
New nicotinamide derivatives have been synthesized by reactions of enamino ketones, aryl(hetaryl)methylidenecyanothioacetamides, alkylating agents, formamide, and cycloalkanones. The structure of ...some of the synthesized compounds has been determined by X-ray analysis.
New Synthesis of Tetrahydroisoquinolines Dyachenko, I. V.; Dyachenko, V. D.; Dorovatovskii, P. V. ...
Russian journal of organic chemistry,
05/2022, Volume:
58, Issue:
5
Journal Article
Peer reviewed
The reaction of cyclohexylidenecyanothioacetamide with
N
,
N
-dimethylformamide dimethyl acetal was studied. This transformation, depending on the reaction conditions, leads to different results: ...when the starting reagents are refluxed without a solvent, 3-(methylsulfanyl)-5,6,7,8-tetrahydroisoquinoline-4-carbonitrile is formed, and refluxing in benzene leads to 2-cyano-3-(dimethylamino)prop-2-enethioamide. The structure of these products was studied by XRD analysts.
Nicotinamide and nicotinonitrile derivatives containing a C
5
–C
7
-cycloalkane ring fused to the C
4
–C
5
bond were synthesized via Knoevenagel condensation, nucleophilic vinylic substitution (S
N
...Vin), and alkylation. The structure of (1-amino-5-phenyl-5,6,7,8-tetrahydrothieno2,3-
c
isoquinolin-2-yl)(phenyl)methanone was determined by X-ray analysis.
Multicomponent condensation of alkylating reagents with carbonyl compounds functionalized by CH-acids is initiated by the Knoevenagel reaction and leads to the formation of substituted pyridines, ...thienopyridines, pyridothienopyridines, and pyrimidothienopyridopyrimidines. The structure of the key products was studied by the X-ray diffraction method.
Оligoarginines were recently discovered (Lebedev et al., 2019 Nov) as a novel class of nicotinic acetylcholine receptors (nAChRs) inhibitors, octaoligoarginine R8 showing a relatively high affinity ...(44 nM) for the α9/α10 nAChR. Since the inhibition of α9/α10 nAChR by α-conotoxin RgIA and its analogs is a possible way to drugs against neuropathic pain, here in a mice model we compared R8 with α-conotoxin RgIA in the effects on the chemotherapy-induced peripheral neuropathy (CIPN), namely on the long-term oxaliplatin induced neuropathy. Tests of cold allodynia, hot plate, Von Frey and grip strength analysis revealed for R8 and α-conotoxin RgIA similar positive effects, expressed most prominently after two weeks of administration. Histological analysis of the dorsal root ganglia sections showed for R8 and RgIA a similar partial correction of changes in the nuclear morphology of neurons. Since α9/α10 nAChR might be not the only drug target for R8, we analyzed the R8 action on rat TRPV1 and TRPA1, well-known nociceptive receptors. Against rTRPV1 at 25 μM there was no inhibition, while for rTRPA1 IC50 was about 20 μM. Thus, involvement of rTRPA1 cannot be excluded, but in view of the R8 much higher affinity for α9/α10 nAChR the latter seems to be the main target and the easily synthesized R8 can be considered as a potential candidate for a drug design.
•Oligoarginine R8 and α-conotoxin RgIA exert therapeutic effects on CIPN after oxaliplatin cessation.•R8 and RgIA demonstrated similar anti-pain activity.•R8 corrected some changes in the nuclear morphology of DRG neurons.•R8 and R16, known to inhibit α 9/α 10 nAChRs in nM range, block rTRPA1 in the micromolar range.
The tandem Knoevenagel—Michael—intramolecular ammonolysis—alkylation reaction was used to synthesize functionalized tetrahydropyridones. The molecular and crystal structures of four pyridone ...derivatives were studied by X-ray diffraction.
New cycloalka
b
pyridine and chromene derivatives were synthesized by multicomponent condensations. The structure of some of the synthesized compounds was determined by X-ray analysis.
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