A series of 2-methylthio-1,4-dihydropyrimidine derivatives (II) were synthesized in good yields by alkylation of 1,2,3,4-tetrahydropyrimidines (I) with methyl iodide in the presence of pyridine. Their structures were confirmed by elemental analysis, IR and 1H NMR spectra. The compounds were tested for analgesic activity by acetic acid induced writhing method. Compounds IIh, IIe, IIk and IIl sho...

a series of 2-methylthio-1,4-dihydropyrimidine derivatives (ii) were synthesized in good yields by alkylation of 1,2,3,4-tetrahydropyrimidines (i) with methyl iodide in the presence of pyridine. their structures were confirmed by elemental analysis, ir and 1h nmr spectra. the compounds were tested for analgesic activity by acetic acid induced writhing method. compounds iih, iie, iik and iil sho...

Hepatocellular carcinoma (HCC) is a highly complex cancer, resistant to commonly used treatments and new therapeutic agents are urgently needed. A total of thirty-two thieno[3,2-b]pyridine derivatives of two series: methyl 3-amino-6-(hetero)arylthieno[3,2-b]pyridine-2-carboxylates (1a-1t) and methyl 3-amino-6-[(hetero)arylethynyl]thieno[3,2-b]pyridine-2-carboxylates (2a-2n), previously prepared...

4-Aminopyridine (4-AP), a potassium channel blocker, is capable of restoring conduction in the injured spinal cord. However, the maximal tolerated level of 4-AP in humans is 100 times lower than the optimal dose in in vitro animal studies due to its substantially negative side effects. As an initial step toward the goal of identifying alternative potassium channel blockers with a similar abilit...

The ever-growing demand for fluorogenic dyes usable in the rapid construction of analyte-responsive fluorescent probes, has recently contributed to a revival interest chemistry diketopyrrolopyrrole (DPP) pigments. In this context, we have explored potential symmetrical and unsymmetrical DPP derivatives bearing two or one 4-pyridyl substituents acting as optically tunable group(s). unique behavi...

We describe a general catalytic methodology for the enantioselective dearomative alkylation of pyridine derivatives with Grignard reagents, allowing direct access to nearly enantiopure chiral dihydro-4-pyridones yields up 98%. The involves dearomatization in situ-formed N-acylpyridinium salts, employing alkyl organomagnesium reagents as nucleophiles and copper (I) complex catalyst. Computationa...

We have previously reported that a single injection of nicotinamide into mice leads to over a lo-fold increase in liver diphosphopyridine nucleotide (DPN) (1). The maximal increase in DPN concentration occurred from 8 to 12 hours after administration of the nicotinamide; this increase is followed by a pronounced decrease, and after 24 hours the DPN level is essentially the same as that of the u...

We have prepared a set of heterocyclic benzimidazole derivatives bearing amidino substituents at C-5 of benzimidazole ring, by introducing various heterocyclic nuclei (pyridine, N-methyl-pyrrole or imidazole) at C-2, and evaluated their antitumor and antiviral activities. The most pronounced antiproliferative activity was shown with compounds 6 and 9, having imidazolinylamidino-substituent. Int...

Dichloroboryldisilylamines [SiClm(CH3)3−m]N[Si(CH3)3](BCl2) (m = 1 – 3) as well as chloromethylboryl-bis-(chlorodimethylsilyl)amine [SiCl(CH3)2]2N[BCl(CH3)] form 1 : 1 adducts with pyridine (1 – 4). Those with m = 2 and 3 have been converted into functionalized diazadiboretidine derivatives which are still coordinated by pyridine: [(SiClm(CH3)3−m)NBCl · Py]2 (5: m = 2, 6: m = 3). Single-crystal...