Specific binding of [3H]LY186126, an analogue of indolidan (LY195115), to cardiac membranes enriched in sarcoplasmic reticulum vesicles.

Kauffman, Raymond F.; Utterback, Barbara G.; Robertson, David W.

doi:10.1161/01.res.64.5.1037

Cited by 16 publications

(7 citation statements)

References 8 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…IR (KBr) cm The compounds (7)(8)(9)(10)(11)(12)(13) were identified on the basis of the difference in the melting points and R f values with respect to their reactants. These compounds were not subjected for their spectral analysis as their ACE inhibitory activity results .i.e.…”

Section: -Benzoyl-4-(4-bromobenzylidene)-6-phenyl-45-dihydropyridazmentioning

confidence: 99%

“…There are many cardioactive pyridazinone derivatives, which are either in clinical use or have been tested in clinical trials, for example, imazodan 7,8 , CI-930 8,9 , pimobendan 8,10 , indolidan 8,11 , levosimendan 8,12 , SK&F-93741 8,13 , Y-590 8,14 , Meribendan 15 , NSP-804 16 , NSP-805 16 , bemoradan 17,18 , senazodan 19 , amipizone 8,18 , prinoxodan 20 , SKF 95654 21 , siguazodan 22 and KF 15232 22 . Some of these pyridazinone derivatives were found not suitable for further development because of their side effects and low potency.…”

Section: Introductionmentioning

confidence: 99%

See 1 more Smart Citation

Synthesis and Antihypertensive Activity of Some Novel Pyridazinones

Imran¹,

Nayeem²

2016

Orient. J. Chem

View full text Add to dashboard Cite

Four pyridazinones (2-5) were synthesized by the reaction of 3-benzoylpropionic acid with the corresponding hydrazines. These pyridazinones were further derivatized with appropriate aromatic aldehydes in the presence of piperidine to obtain the desired compounds (6-13). The chemical structures of the synthesized pyridazinones were elucidated on the basis of their spectral analysis (IR, 1 H-NMR, and 13 C-NMR). Molecular docking studies were carried out to identify the most active antihypertensive pyridazinone compound by using the crystal structure of human Angiotensin Converting Enzyme (ACE), the enzyme implicated in the pathogenesis of hypertension. The compound (6) was identified as the most active inhibitor of the Angiotensin Converting Enzyme (ACE). This compound was further assessed for its ACE inhibitory activity using Dojindo ACE Kit-WST test kit. The enzymatic ACE inhibitory activity revealed that the compound (6) had IC 50 value of 5.78 µg/ mL, wherein the standard drug Lisinopril had IC 50 value of 0.85 µg/mL. It has been concluded that incorporation of free amino groups and free carboxylic acid groups in the structure of the synthesized pyridazinone (6-13) may provide more active and potent ACE inhibitors.

show abstract

Section: -Benzoyl-4-(4-bromobenzylidene)-6-phenyl-45-dihydropyridazmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Synthesis and Antihypertensive Activity of Some Novel Pyridazinones

Imran¹,

Nayeem²

2016

Orient. J. Chem

View full text Add to dashboard Cite

show abstract

“…Initial binding studies with [3H]-LY 186 126 were camed out using canine cardiac membranes (22). [3H]-LY 186 126 bound with high affinity (Kd = 4 nM) to an apparent single class of sites associated with highly purified preparations of sarcoplasmic reticulum vesicles ( Fig.…”

Section: Binding Studiesmentioning

confidence: 99%

Indolidan: A Potent, Long‐Acting Cardiotonic and Inhibitor of Type IV Cyclic AMP Phosphodiesterase

Kauffman¹,

Robertson²,

Franklin³

et al. 1990

Cardiovascular Drug Reviews

View full text Add to dashboard Cite

“…These drugs are either in use clinically or under the clinical trials. They contain imazodan [27,28], CI-930 [29]; indolidan; pimobendan, levosimendan [30][31][32], SK&F-93741, Y-590, meribendan [33][34][35], NSP-805;…”

Section: Introductionmentioning

confidence: 99%

A Review on Pyridazinone Ring Containing Various Cardioactive Agents

Asif

2019

J. Chem. Rev.

View full text Add to dashboard Cite

In this work, some pyridazinones were studied for their cardioactive activity. These compounds showed significant cardio-active action with respect to the regular used drugs. However, it was found that the existence of the pyridazine ring is a crucial necessity in the structure of these pyridazinonecompounds to show the improved cardioactive activities. It was also understood that the substitution of the different group on the pyridazinone ring with other related bioisosteres or isosteres along with the existence of pyridazine ring may provide better cardioactive compounds. Pyridazinoneis, a component of various cardio-active agents, which are in uses clinically or in clinical trials. These contain pimobendan, indolidan, levosimendan, imazodan, CI-930, meribendan, bemoradan, senazodan, siguazodan, amipizone, prinoxodan, Y-590, SK&F-93741, SKF 95654, NSP-805, NSP-804 and KF 15232. This study briefly reviews the pyridazinone ring for the progress of new cardio-active drugs.

show abstract

Specific binding of [3H]LY186126, an analogue of indolidan (LY195115), to cardiac membranes enriched in sarcoplasmic reticulum vesicles.

Cited by 16 publications

References 8 publications

Synthesis and Antihypertensive Activity of Some Novel Pyridazinones

Synthesis and Antihypertensive Activity of Some Novel Pyridazinones

Indolidan: A Potent, Long‐Acting Cardiotonic and Inhibitor of Type IV Cyclic AMP Phosphodiesterase

A Review on Pyridazinone Ring Containing Various Cardioactive Agents

Contact Info

Product

Resources

About