Letters in Drug Design & Discovery - Volume 9, Issue 6, 2012

Intensive insulin therapy to control blood glucose level increases survival among critically ill patients in intensive care unit and hospital. Hyperglycemia is potentially harmful because it acts as a procoagulant, induces insulin resistance, causes apoptosis, impairs neutrophil function, increases the infection rate and is associated with the risk of morbidity and mortality. Hyperglycemia and insulin resistance are virtually Read More

In this paper some semicarbazide and 1,2,4-triazolin-5-one derivatives are evaluated in vitro for their anticancer activity towards human tumour cell line: ovary (TOV 112D), lung (A 549), breast (T47D) and uterus (Hela). Compounds 2-4 have been found to show the most effective in vitro activity against ovary cancer cell line. For compound 4 the growth inhibition (80% and 70%) is observed in two concentrations (100 μg/m Read More

Fifteen berberine–bile acid analogues were synthesized. Anticancer activities of these analogues compared with berberine (BBR) were evaluated in vitro; among the analogues, A4, B4, and B5 had higher cytotoxicity than that of BBR. Most of the analogues showed higher antimicrobial activity against Staphylococcus aureus ATCC 25923 and Staphylococcus albus ATCC 8799 than that of BBR, but Bacillus subtilis AS 1.398 and Esc Read More

Three-dimensional quantitative structure-activity relationship (3-D QSAR) was performed using comparative molecular field analysis (CoMFA) and comparative molecular similarity indices analysis (CoMSIA) techniques in order to understand the carbonic anhydrase inhibition activity. A large number of 25 structurally and functionally diverse series of aromatic heterocyclic sulfonamides carbonic anhydrase (CA, EC 4.2.1.1) inhi Read More

The current treatment of organophosphorus compounds induced intoxication consists of combined administration of anticholinergic drug, oxime reactivator and anticonvulsant. Oxime reactivators are causal treatment of organophosphorus intoxication and they are able to cleave OP moiety from the molecule of inhibited acetylcholinesterase. Unfortunately, none of the currently used oximes is sufficiently effective against all Read More

A set of 28 compounds with inhaled general anesthetics properties and with the literature values of their biological activity was used to search for relationships between structural parameters obtained from PCM (Polarizable Continuum Model) method. Ab initio calculations have been done for molecules in vacuo and also placed in the aquatic environment and the environment of an organic solvent (ethanol). Finally the data exa Read More

We report the synthesis, evaluation and rationalisation of the inhibitory activity of a series of 3,5-dibromo derivatives of 4-hydroxyphenyl ketone as probes of the active site of the type 3 of 17β-hydroxysteroid dehydrogenase (17β-HSD3). The results support the important role of hydrogen bonding interaction in the inhibition of 17β-HSD3.

A series of twelve novel azetedinones 4a-l have been synthesized by cyclocondensation of various Schiff bases of amino thiadiazole with chloroacetyl chloride in the presence of triethylamine. Various novel Schiff bases 3a-l were synthesized by condensation of 2-amino-5-aryl-5H-thiazolo[4,3-b]-l,3,4-thiadiazole with various aryl aldehydes. The synthesized compounds were characterized by FTIR, 1H-NMR, 13C-NMR Read More

3-Amino-5-methyl-2,4-dicarbonitrile biphenyl derivatives 1-14 have been synthesized and all compounds were screened for their antibacterial effects against fourteen Gram-positive and sixteen Gram-negative bacterial strains and showed varying degree of activities. Compounds 1, 2, 4, 5, 6, 8, 13, and 14 were found to be significantly active against various Gram-positive bacteria, however, compounds 1, 3, 4, 6, 9, 12, and Read More

A series of 2-amino-(5 or 7-substituted-2-oxoindolin-3-ylidene) benzoxazole-5-carbohydrazide derivatives were synthesized by treating 2-aminobenzoxazole-5-carbohydrazide with different substituted isatins. All the synthesized derivatives (VI a-l) were screened for their in vitro anticancer (against HeLa, IMR-32 & MCF-7 cancer cell lines), antioxidant (against DPPH radicals) and antimicrobial activities. The results Read More

Several new, N2-substituted derivatives of 1,2,4-triazole-3-thione were synthesised in order to analyse the impact of substituent in the N-4 position on antibacterial activity. Structure of the compounds in question was confirmed on the basis of 1H NMR and IR spectra as well as by means of the elementary analysis (C, H, N). Microbiological studies were conducted on Gram-positive and Gram-negative bacteria strains. One of the Read More

1-Methylhydantion is a compound, which was isolated from Oviductus Ranae for the first time. In our study, we found that it showed good antitussive and anti-inflammatory activity. It is also the first report which illustrates the antitussive activity of hydantion derivative. A series of hydantion derivatives were synthesized and evaluated for their anti-inflammatory and antitussive activity in vivo. The pharmacological t Read More