In an effort to discover potent, orally bioavailable compounds for the treatment of atrial fibrillation (AF) and ventricular tachycardia (VT), we developed a class of gap-junction modifiers typified by GAP-134 (1, R(1)=OH, R(2)=NH(2)), a compound currently under clinical evaluation. Selected compounds with the desired in-vitro profile demonstrated positive in vivo results in the mouse CaCl(2) a...

0263-2241/$ see front matter 2013 The Authors. Published by Elsevier Ltd. All rights reserved. http://dx.doi.org/10.1016/j.measurement.2013.08.007 q This is an open-access article distributed under the terms of the Creative Commons Attribution-NonCommercial-No Derivative Works License, which permits non-commercial use, distribution, and reproduction in any medium, provided the original author a...

A number of benzothiazole-2-ylsulfanyl derivatives 2(1,3-Benzothiazol-2-ylsulfanyl)alkanoylhydrazide (IA – IG) and 5-[1-(1,3-Benzothiazol-2-ylsulfanyl)alkyl]-1,3,4-thiadiazole-2(3H) thione (IIA-IIG) have been synthesised from (1,3Benzothiazol-2-ylsulfanyl)acetic acid. These compounds were synthesied and characterized from their F.T.I.R, and H-NMR spectral studies. The compound (IIA to IIG) were...

The complete mol-ecule of the title compound, C(16)H(12)Cl(2)N(2)S(3), is generated by crystallographic twofold symmetry, with the S atom of the thiadiazole ring lying on the rotation axis. The dihedral angle between the mean planes of the 1,3,4-thia-diazole and benzene rings is 87.19 (7)°. In the crystal, mol-ecules are linked by C-H⋯N inter-actions and short S⋯S contacts [3.3389 (9) Å] occur.

New 1,3,4-thiadiazole, 5a-e, and 1,2,4-triazolecompounds 6a-c, containing a D,L-methionine moiety were synthesized by intramolecular cyclization of 1,4-disubstituted thiosemicarbazides 4a-e in acid and alkaline media, respectively. The potential antimicrobial effects of the synthesized compounds were investigated using the Staphylococcus aureus ATCC 25923, Bacillus antracis ATCC 8705, Bacillus ...

A series of five membered heterocyclics was synthesized by the reaction between isoniazid and various substituted isothiocyanates and was tested for their anticonvulsant activity by determining their ability to provide protection against convulsions induced by electroconvulsometer. Among the synthesized compounds, (IIf) 2-(4-chlorophenyl)amino-5-(4-pyridyl)-1,3,4-thiadiazole and (IIIf) 2-(4-chl...

In the presence of 1 mol% of a copper(II) catalyst and air, a readily available N-acetyl-N-thioacylguanidine undergoes a one-pot benzylic oxidation–oxidative heterocyclization sequence to give the 3-amino5-acyl-1,2,4-thiadiazole core of polycarpathiamines A (2) and B (3) and thus facilitating the first synthesis of both natural products. This methodology offers a straightforward alternative to ...

Cancer is a big global problem and is one of the top and main causes of mortality in developed countries. Many of the current treatments and anticancer therapeutics have problems with severe side effects and on the other hand, the drug resistance is also another obstacle in the cancer chemotherapy. Hence, there is a strong demand for the discovery and development of effective new antineopla...