Medicinal Chemistry - Volume 8, Issue 5, 2012

The reaction of K2PtCl4 with anticancer-alkylating agent mechlorethamine hydrochloride (CH3NH(C2H4Cl)2 x HCl = HN2xHCl), in the molar ratio 1 : 2, affords the complex [H2N2]2[PtCl4]. In vitro antimicrobial and lipoxygenase inhibitory activities of the complex and its precursor were evaluated. Antimicrobial activity of the HN2xHCl and [H2N2]2[PtCl4] complex was investigated against 29 species of microorganisms. Testing is perf Read More

A series of compounds including N-aryl substituents of phthalimide and 4-nitrophthalimide were synthesized and evaluated for their anticonvulsant properties. The in vivo screening data suggest that all the analogs have the ability to protect against pentylenetetrazole-induced seizures. These compounds exerted their maximal effects 30 min after administration. The most potent compound in both, tonic and clonic seizure was Read More

Tolbutamide (N-[(butylamino)carbonyl]-4-methylbenzenesulfonamide, CAS 64-77-7, I) is the first generation of potassium channel blocker and sulfonylurea oral hypoglycemic drug that imparts marked blood glucose lowering effect in type 2 diabetes or non-insulin dependent diabetes mellitus (NIDDM) patients. In this study, I and its two new analogs with substituting butylamine side by 3-diethylamino-1-propylamine (3) Read More

We have studied inhibition of Plasmodium falciparum lactate dehydrogenase (pfLDH) by dihydroxynaphthoic acid (DHNA) analogues derivatives of hemigossypol-sesquiterpene found in cottonseed known to exhibit antimalarial activity. Molecular models of pfLDH-DHNA complexes were prepared from high-resolution crystal structures containing DHNA and azole inhibitors and binding affinities of the inhibitors were computed by mo Read More

A simple and practical synthetic approach for tasigna was described here in six steps with high yield (40%). All of the intermediates and final target compound were isolated cleanly in high yield without a need for chromatographic purification. Significantly, the facile synthetic route proposed in this work has the characteristics of mild synthetic conditions, inexpensive reagents, high yield and simple operation.