Synthesis,Characterization, and Screening for Antiamoebic Activity of Palladium(II), Platinum(II), and Ruthenium(II) Complexes with NS‐Donor Ligands

Reaction of [PdCl₂(DMSO)₂], [PtCl₂(DMSO)₂], and [RuCl₂(η⁴‐C₈H₁₂)(MeCN)₂] with S‐acetyl N^β‐acetyldithiocarbazate (=2‐acetylhydrazinecarbodithioic acid anhydrosulfide with ethanethioic acid; aadt; 1 ), S‐methyl N^β‐[(5‐nitrothiophene‐2‐yl)methylene]dithiocarbazate (=S‐methyl 2‐[(5‐nitrothiophene‐2‐yl)methylene]hydrazinecarbodithioate; mntdt; 2 ), and S‐benzyl N^β‐[(5‐nitrothiophene‐2‐yl)methylene]dithiocarbazate (=S‐benzyl 2‐[(5‐nitrothiophene‐2‐yl)methylene]hydrazinecarbodithioate; bntdt; 3 ) led to new complexes [PdCl₂(L)], [PtCl₂(L)], and [RuCl₂(η⁴‐C₈H₁₂)(L)] (L=ligands 1 – 3 ). All these compounds were characterized by elemental analysis, IR, ¹H‐ and ¹³C‐NMR and UV/VIS spectra and thermogravimetric analysis. Ligand 1 coordinates through the thioxo S‐atom and the carbazate N(β) atom, whereas in ligands 2 and 3 the thioxo S‐atom and the azomethine N‐atom are coordinated to the metal ion. Screening of antiamoebic activity of these compounds was performed in vitro against the HK‐9 strain of E. histolytica. All the complexes were more active than their respective ligands; compound 3a showed the most promising activity.     

Synthesis of Pyrazole Derivatives Possessing Anticancer Activity: Current Status

Pyrazole is a versatile lead compound to design potent bioactive molecules for drug discovery and development, particularly in cancer therapy. The aim of this review is to present the most recent deeds in the field of synthetic route made for functionalized pyrazole derivatives active against cell proliferation disease. The review article covers the synthesis of 1H-pyrazole, synthesis of N-substituted pyrazoles, synthesis of pyrazolopyrazoles, and synthesis of pyrazoles fused with a naturally occurring moiety. Some of these reported compounds have passed the preclinical or initial-phase clinical trials for their anticancer activity.     

Cyclodextrin based novel drug delivery systems

The versatile pharmaceutical material cyclodextrin’s (CDs) are classified into hydrophilic, hydrophobic, and ionic derivatives. By the early 1950s the basic physicochemical characteristics of cyclodextrins had been discovered, since than their use is a practical and economical way to improve the physicochemical and pharmaceutical properties such as solubility, stability, and bioavailability of administered drug molecules. These CDs can serve as multi-functional drug carriers, through the formation of inclusion complex or the form of CD/drug conjugate and, thereby potentially serving as novel drug carriers. This contribution outlines applications and comparative benefits of use of cyclodextrins (CDs) and their derivatives in the design of novel delivery systems like liposomes, microspheres, microcapsules, nanoparticles, cyclodextrin grafted cellulosic fabric, hydrogels, nanosponges, beads, nanogels/nanoassemblies and cyclodextrin-containing polymers. The article also focuses on the ability of CDs to enhance the drug absorption across biological barriers, the ability to control the rate and time profiles of drug release, drug safety, drug stability, and the ability to deliver a drug to targeted site. The article highlight’s on needs, limitations and advantages of CD based delivery systems. CDs, because of their continuing ability to find several novel applications in drug delivery, are expected to solve many problems associated with the delivery of different novel drugs through different delivery routes.     

Nanocrystalline copper(II) oxide catalyzed aza-Michael reaction and insertion of α-diazo compounds into N-H bonds of amines

Nanocrystalline copper(II) oxide efficiently catalyzed the conjugate addition of aliphatic amines to α,β-unsaturated compounds to produce β-amino compounds with excellent yields under mild reaction conditions. Similarly, Glycine esters are obtained in good yields by the insertion of α-diazoacetate into N-H bonds of amines. The catalyst is used for three cycles with minimal loss of activity.     

Understanding changes in DTI metrics in patients with different stages of neurocysticercosis

Diffusion tensor imaging (DTI) was performed on 25 patients with neurocysticercosis (NCC). The aim of this study was to investigate the changes in DTI measures during the evolutionary course of NCC lesions from vesicular to calcified stage in the brain. DTI measures were quantified from the NCC lesions of all patients. On the basis of conventional imaging findings, NCC lesions were classified into vesicular, vesicular colloidal, granular nodular and calcified stages. Significant inverse correlation was observed between the evolutionary stage of NCC lesion and mean diffusivity (MD; r=−0.748, P<0.001) and spherical anisotropy (CS; r=−0.585, P<.001) values. Significant direct correlations were observed between evolutionary stages of NCC lesion and mean fractional anisotropy (FA; r=0.575, P<0.001), linear anisotropy (CL; r=0.478, p<0.001) and planar anisotropy (CP; r=0.561, p<0.001) values. Successive decrease in MD values calculated from NCC lesions was observed, moving from vesicular to granular nodular stage. On FA, CL and CP maps, a significant increase in signal intensity value was observed in calcified as compared to other stages. We conclude that DTI measures may indicate the evolutionary changes in NCC from vesicular to calcified stage.