In-vitro drug–drug interaction studies of diltiazem with floroquinolones

Diltiazem is an established cardiovascular drug mainly used for the management of hypertension specifically for the angina pectoris. Fluoroquinolones are widely prescribed against the treatment of severe infections. In vitro relations of diltiazem with fluoroquinolones (ciprofloxacin, levofloxacin, norfloxacin, and ofloxacin) were examined using spectrophotometric and separation techniques, i.e., RP-HPLC. Diltiazem’s availabilities were observed to be predisposed highly in the presence of fluoroquinolones. To investigate the mechanism of interaction in a variety of dissolution environments, i.e., simulating body environments with regard to pH on these interactions has been studied. Moreover, complex of diltiazem–fluoroquinolones were prepared and elucidated through IR spectroscopy and confirmed by computational molecular modeling.     

Palladium(II) and platinum(II) derivatives of benzothiazoline ligands: Synthesis, characterization, antimicrobial and antispermatogenic activity

A series of Pd(II) and Pt(II) complexes with two N(∩)S donor ligands, 5-chloro-3-(indolin-2-one)benzothiazoline and 6-nitro-3-(indolin-2-one)benzothiazoline, have been synthesized by the reaction of metal chlorides (PdCl2 and PtCl2) with ligands in 1:2 molar ratios. All the synthesized compounds were characterized by elemental analyses, melting point determinations and a combination of electronic, IR, 1H NMR and 13C NMR spectroscopic techniques for structure elucidation. In order to evaluate the effect of metal ions upon chelation, both the ligands and their complexes have been screened for their antimicrobial activity against the various pathogenic bacterial and fungal strains. The metal complexes have shown to be more antimicrobial against the microbial species as compared to free ligands. One of the ligands, 5-chloro-3-(indolin-2-one)benzothiazoline and its corresponding palladium and platinum complexes have been tested for their antifertility activity in male albino rats. The marked reduction in sperm motility and density resulted in infertility by 62-90%. Significant alterations were found in biochemical parameters of reproductive organs in treated animals as compared to control group. It is concluded that all these effects may finally impair the fertility of male rats.     

Isolation of onosmins A and B, lipoxygenase inhibitors from Onosma hispida

Onosmins A (1) and B (2), lipoxygenase inhibitors, have been isolated from Onosma hispida. Their structures were established as 2-[(4-methylbenzyl)amino]benzoic acid (1) and methyl 2-[(4-methylbenzyl)amino]benzoate (2) through spectroscopic studies, including 2D-NMR. The known compounds apigenin (3), 6,4'-dimethoxy-3,5,7-trihydroxyflavone (4), 6,7-dimethoxy-3,5,4'-trihydroxyflavone (5) and apigenin 7-O-beta-D-glucoside (6) are also reported for the first time from this species. Compounds (1) and (2) inhibited lipoxygenase (LOX, EC 1.13.11.12) enzyme in a concentration-dependent fashion with IC50 values of 24.0 and 36.2 microM, respectively. Lineweaver-Burk as well as Dixon plots and their secondary replots indicated that the nature of inhibition was purely a non-competitive type, with K(i) values 22.0 microM and 31.1, respectively.     

Tyrosinase-inhibitory long-chain esters from Amberboa ramosa

Long-chain esters 1 and 2 have been isolated from the chloroform-soluble fraction of Amberboa ramosa and their structures assigned to be methyl 2beta(2S)-hydroxyl-7(E)-tritriacontenoate (1) and methyl 2beta(2S)-O-beta-D-galactopyranosyl-7(E)-tetratriacontenoate (2). In addition, tricontane (3) and apigenin (4) are also reported for the first time from this species. The structures were assigned on the basis of 1D and 2D NMR techniques. Compounds 1 and 2 showed strong to moderate inhibitory activity against tyrosinase.     

Spectral and biocidal studies of palladium(II) and platinum(II) complexes with monobasic bidentate Schiff bases

The monobasic bidentate Schiff base complexes of palladium(II) and platinum(II) derived from 1H-indol-2,3-dione thiosemicarbazone (L¹H) and 1H-indol-2,3-dione semicarbazone (L²H) have been characterized on the basis of elemental analysis, molecular weight determinations, i.r., ¹H n.m.r. and u.v. spectral studies. Based on these studies a square planar environment around the metal atoms has been proposed. Antimicrobial effects of both the ligands and their complexes on different species of pathogenic fungi and bacteria have been recorded and these are found to possess significant fungicidal and bactericidal properties.     

New Epoxydammarane Triterpenes from Salvia santolinifolia

Three new 20,24‐epoxydammarane triterpenes, santolins A–C ( 1 – 3 ), were isolated from the AcOEt‐soluble fraction of the MeOH extract of Salvia santolinifolia (whole plant). Their structures were assigned based on ¹H‐NMR, ¹³C‐NMR (DEPT), and 2D‐NMR analyses, in combination with HR‐MS experiments and comparison with literature data of related compounds.     

Divalent manganese and palladium complexes of the phenylmethyl ester of hydrazinecarbodithioic acid

Mn^II and PdII complexes of o-FC₆H₄C(H)NNC(SH)SCH₂Ph (L1H) and o-FC₆H₄C(Me)NNC(SH)SCH₂Ph (L²H) have been synthesized and characterized by physicochemical and spectroscopic means. The complexes are of the types [MnCl(L)H₂O], [Mn(L)₂], [Pd(L)₂]Cl₂ and [Pd(L)₂]. Spectral data suggest that the ligands coordinate in a monobasic bidentate fashion through the S and N atoms. L₂H and its complexes were found to exhibit antimicrobial properties.