Synthesis of drug metal complexes and their influence on human platelet aggregation

During the past few decades the emergence of inorganic medicinal chemistry has been developed novel therapeutic agents. Researcher's perseverance in this branch of chemistry has led them to explore further valuable chemical spaces by synthesizing metal complexes already known pharmacological agents for their potential use. However, it is in its early stage, this methodology has demonstrated metal complexes with better bioactivities than the parent ligand molecules. In this study, transition metal complexes of pyrazinamide [PZ], isoniazid [INH], fluconazole [FCZ], metformin [dimethylbiguanide, DMBG] and losartan potassium [LS-K] were selected to evaluate for their possible anti-platelets aggregation in the light of reports on divalent and trivalent cations like calcium, copper, manganese, magnesium, and cadmium may influence the process of thrombocytic activity and aggregation. The required evaluation was carried out on human plasma through an APACT 4004 platelet aggregation analyzer. Arachidonic acid [ADP] was used to gauge any alteration in platelet shape and aggregation process. The parent drugs showed some antiplatelets aggregation, however, their metal complexes demonstrated better efficacy

Spectroscopic and cytotoxic studies of losartan complexes

Use of drug-metal complexes for the treatment of several human diseases has resulted in significant progress in the field of medicinal inorganic chemistry. The current study describes the synthesis and characterization of Cu [II] and Ni [II] complexes of Losartan, an antihypertensive drug. These complexes were evaluated for their cytotoxic activity against four human cancer cell lines; SNB-19, HCT-15, COLO-205 and KB-3-1. Spectroscopic characterization revealed that during complex formation, the metal was bound through the nitrogen atoms of the tetrazole moiety of the losartan molecule. The molecular formulas of copper [[Cu [LS][2] Cl[2]].6H[2]O] and nickel [[Ni [LS][2]Cl[2]]. H[2]O] complexes were found to be in agreement with the analytical data obtained through elemental analysis. For both the complexes, metal to ligand ratios of 1:2 were calculated. As revealed by FTIR, UV-Visible, and 1H-NMR studies, both the complexes displayed octahedral geometries. Scanning electron microscopy [SEM] revealed marked changes in the morphology of the complexes, compared to the pure drug. From XRD studies, characteristic crystalline peaks of pure losartan were observed whereas no prominent peaks were observed for its complexes. Complexes were found to be inactive in the cytotoxic activity test performed using SNB-19, HCT-15, COLO-205 and KB-3-1 cell lines

Phytochemical investigations on chemical constituents of Achillea tenuifolia lam

Achillea tenuifolia Lam [Asteraceae] afforded a methanolic extract from which after fractionation in solvents with different polarities two known flavones 3', 5- dihydroxy- 4', 6, 7- trimethoxy flavone [eupatorine, compound 3], 5- hydroxy- 3', 4', 6, 7- tetramethoxyflavone [compound 4], besides stearic acid [compound 1 ], lupeol [compound 2], daucosterol [beta- sitosterol 3-O- beta- D- glucopyranoside, compound 5], 2, 4- dihydroxy methyl benzoate [compound 6] were isolated for the first time. The structure of isolated compounds was elucidated by means of different spectroscopic methods such as UV, IR, Mass and [1]H- NMR [1D and 2D] and [13]C-NMR. For further confirming of structures of isolated compounds, comparison of the spectral data of them with those reported in the litratures have been done