Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
9769299 | European Journal of Medicinal Chemistry | 2005 | 10 Pages |
Abstract
New triorganotin(IV) derivatives of dipeptides with general formulae R3Sn(HL), where R = Me and/or n-Bu and/or Ph and HL is the monoanion of glycylglycine (H2L-1), glycylvaline (H2L-2), glycylleucine (H2L-3), glycyltryptophane (H2L-4) and glycyltyrosine (H2L-5) have been synthesized and characterized on the basis of infrared, multinuclear NMR and 119Sn Mössbauer spectroscopic studies. All the newly synthesized compounds were examined for their in vivo anti-inflammatory activity (using the carrageenan-induced paw edema bioassay in rats), acute toxicity (LD50) and cardiovascular activity. These compounds were also screened for their in vitro antimicrobial activity against Staphylococcus aureus Mau (29/58) and (78/71), Bacillus subtilis (18/64), Escherichia coli (326/71), Candida albicans (Pn-10), Microsporum gypseum and Euglena gracillis. The results revealed that triphenyltin(IV) derivatives exhibited anti-inflammatory activity comparable to that of phenylbutazone with high safety margin (LD50 > 500 mg kg-1). Further Ph3Sn(Gly-Val) displays a potent cardiovascular activity. Moreover, most of the compounds displayed appreciable antibacterial activities when compared with ampicillin and norfloxacin. Compounds Ph3Sn(Gly-Gly) and Ph3Sn(Gly-Val) are the most distinctive derivatives identified in the present study because of their promising in vivo anti-inflammatory activity and in vitro antibacterial activity against gram-positive and -negative bacteria.
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Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Mala Nath, Sandeep Pokharia, George Eng, Xueqing Song, Ashok Kumar,