In order to determine the optimum size of heterocycle of lead compound 1 (6-methyl-3-phenethyl-3,4-dihydro-1H-quinoline-2-thione; IC(50)=0.8 microM) for inhibition of melanogenesis, we have synthesized and evaluated some benzimdazole-2(3H)-thiones 5a-e. The preliminary bioassay has shown that the benzimdazole-2(3H)-thione motif of 5 is essential structural unit for their inhibitory activity. Am...

In the title N-Mannich bases, 3-(adamantan-1-yl)-4-(4-fluoro-phen-yl)-1-[(4-phenyl-piperazin-1-yl)meth-yl]-4,5-di-hydro-1H-1,2,4-triazole-5-thione (C29H34FN5S) (I), and 3-(adamantan-1-yl)-4-(4-fluoro-phen-yl)-1-{[4-(2-meth-oxyphen-yl)piperazin-1-yl]-meth-yl}-4,5-di-hydro-1H-1,2,4-triazole-5-thione (C30H36FN5OS) (II), fluoro-phenyl, adamantane and piperazine moieties are linked to a planar triaz...

Tuberculosis (TB) ranks second, next to AIDS making it most formidable disease if the present age. One of the crucial enzymes involved in cell wall synthesis of Mycobacterium tuberculosis, InhA (enoyl acyl carrier protein reductase) has been authenticated as an effective target for anti-mycobacterial drug development. In the current work, we have developed novel derivatives of 1,2,4-triazole-5-...

For the first time, 5-formyl-1-(pyridin-3-yl)-1H-1,2,3-triazole-4-carboxylate was synthesized via a two-step scheme. The molecular structure of compound determined by single-crystal X-ray diffraction analysis. Hirshfeld surface analysis used to study various intermolecular interactions. crystalline is marked presence three types ?-interactions (n??*, lp···?, and ?···?) between -C(H)=O group tri...

Metal complexes with the anion of 1-R-tetrazolethiones have been prepared by reactions of chlorido complexes with 1-R-tetrazole-5-thionate [1, 2]. The preparation of metal complexes with these heterocycles by [2+3] cycloaddition of azido complexes with organic isothiocyanates has been intensively studied [3 – 6], recently by Kim [5], Mohr [6] and their coworkers. S-coordination of these heteroc...

Crystals of the title compound, C(12)H(14)N(4)S, were obtained from a condensation reaction of 4-amino-3-ethyl-1H-1,2,4-triazole-5(4H)-thione and 2-methyl-benzaldehyde. In the mol-ecular structure, there is a short N=C double bond [1.255 (2) Å], and the benzene and triazole rings are located on opposite sites of this double bond. The two rings are approximately parallel to each other, the dihed...

In the title compound, C(18)H(15)ClN(6)O(3), the 1,2,3-triazole ring forms dihedral angles of 15.64 (5) and 57.50 (5)° with the two benzene rings. The dihedral angle between the two benzene rings is 72.26 (5)°. In the crystal, mol-ecules are linked via C-H⋯O hydrogen bonds into chains propagating along the b axis. A short O⋯C contact of 2.9972 (13) Å is observed.

In the title compound, C(34)H(34)BrN(5)S, the two phenyl rings of the diphenyl-amino-methyl group are inclined at an angle of 73.86 (8)° and they form dihedral angles of 74.04 (8) and 48.74 (8)° with the triazole ring. Intra-molecular C-H⋯S hydrogen bonds generate S(6) and S(5) ring motifs. The crystal structure is stabilized by weak C-H⋯π inter-actions.