One‐Pot Synthesis and Antimicrobial Activity of Novel α‐Aminophosphonates Using TMG

Kumar, B. Siva; Reddy, Y. Haranadha; Chinthaparthi, Radha Rani; Reddy, G. Chnadra Sekhar

doi:10.1155/2011/906320

Cited by 1 publication

(1 citation statement)

References 17 publications

(18 reference statements)

Supporting

Mentioning

Contrasting

Order By: Relevance

“…α-aminophosphonates are a typeof bioisostere analogues of natural α-amino acids, which largely determines their physiological activity. Various aminophosphonates exhibit antitumour, antibiotic, antifungal, herbicidal and fungicidal activity and have growth-stimulating activity [1,10,29,34,44,53]. Thus, they are crucial for medical chemistry.…”

Section: Introductionmentioning

confidence: 99%

Synthesis and Experimental Study of the Local Anesthetic Activity of New Modified Piperazine Derivatives

KHAIITOVA¹

2023

FARMACIA

View full text Add to dashboard Cite

N-substituted piperazines, an important class of compounds with different pharmacological activities were taken as the basic starting object for the synthesis and study of α-aminophosphonates. The objective of the study was the synthesis, analysis of biological effects (toxicity and local anaesthetic activity) of some new piperazine derivatives, and the evaluation of their potential pharmacological effects. The new piperazine derivatives were coded as LAS-276, LAS-277, LAS-278, where LAS is a local anaesthetic substance. The compounds were synthesized under the conditions of the Kabachnik-Fields reaction. Their acute toxicity in mice, the local anaesthetic activity in a regional and infiltration anaesthesia models were studied, and their estimated pharmacological activity was analysed using the online PASS (Prediction of Activity Spectra for Substances) program. In a series of experiments the administration of high doses of the studied compounds has not caused death of laboratory animals. The study of local anaesthetic activity in the infiltration anaesthesia model showed varying degrees of activity. The compounds showed moderate activity on the regional anaesthesia model. The PASS analysis revealed a very high probability of thrombolytic, anticoagulant, antisclerotic effects and stimulation of endothelin receptors. The implemented studies revealed the low toxicity, moderate local anaesthetic activity of the studied piperazine compounds. There is also a high probability of their thrombolytic activity, which requires further research. RezumatPiperazinele N-substituite sunt o clasă importantă de compuși cu activitate farmacologică ce stau la baza sintezei și studiul αaminofosfonaților. Obiectivele studiului au fost sinteza, analiza efectelor biologice (toxicitate și activitate anestezică locală) și evaluarea efectelor farmacologice ale noilor derivați de piperazină. Compușii au fost sintetizați în condițiile reacției Kabachnik-Fields. Apoi s-a studiat toxicitatea lor după administrarea în doză unică la șoareci, activitatea anestezică locală într-o anestezie regională și modele de infiltrație. Activitatea lor farmacologică a fost evaluată folosind programul online PASS (Predicția Spectrelor de Activitate pentru Substanțe). Într-o serie de experimente, administrarea de doze mari din compușii studiați nu a provocat moartea animalelor de laborator. Studiul activității anestezice locale în modelul de anestezie prin infiltrare a arătat grade variate de activitate. Compușii au prezentat activitate moderată în modelul de anestezie regională. Analiza PASS a relevat o probabilitate foarte mare de efecte trombolitice, anticoagulante, antisclerotice și de stimulare a receptorilor de endotelină. Studiile implementate au evidențiat toxicitatea scăzută, precum și activitatea anestezică locală moderată a compușilor piperazinici studiați. Există, de asemenea, o probabilitate mare a activității lor trombolitice, ceea ce necesită cercetări suplimentare.

show abstract

Section: Introductionmentioning

confidence: 99%

Synthesis and Experimental Study of the Local Anesthetic Activity of New Modified Piperazine Derivatives

KHAIITOVA¹

2023

FARMACIA

View full text Add to dashboard Cite

show abstract

One‐Pot Synthesis and Antimicrobial Activity of Novel α‐Aminophosphonates Using TMG

Cited by 1 publication

References 17 publications

Synthesis and Experimental Study of the Local Anesthetic Activity of New Modified Piperazine Derivatives

Synthesis and Experimental Study of the Local Anesthetic Activity of New Modified Piperazine Derivatives

Contact Info

Product

Resources

About