a series of cyclic analogues of bioactive thiosemicarbazide derivatives have been synthesized as potential antimycobacterial agents. the 4-amino-1,2,4-triazole-5-thione analogues (ia-f) were prepared by heating a mixture of thiocarbohydrzide and appropriate carboxylic acids. reaction of thiocarbohydrazide with γ-ketoesters in the presence of sodium methoxide furnished triazolopyridazine derivat...

current researches have showed that n3, n5-diaryl-2, 6-dimethyl -1, 4-dihydropyrine-3, 5- dicarboxamide analogues demonstrate notable anti-tubercular activity. in this study, hantzsch condensation was used to design and synthesize new analogues of dihydropyridine (dhp). different diary carboxamides were inserted at positions 3 and 5 of the dhp ring. 4(5)-chloro-2-ethyl-5(4)-imidazolyl moiety wa...

We examine classes of quantum algebras emerging from involutive, non-degenerate set-theoretic solutions the Yang-Baxter equation and their q-analogues. After providing some universal results on quasi-bialgebras admissible Drinfeld twists we show that produced q-analogues are in fact quasi-triangular quasi-bialgebras. Specific illustrative examples compatible with our generic findings worked out...

Two types of prodrugs, benzyl analogues of isophosphoramide mustard (iPAM), activated by cytochrome P450, and acylthioethyl analogues, activated by esterases, were designed. In contrast to iPAM that hydrolyse rapidly, the examined compounds are stable in phosphate-buffered saline and Tris buffer. Benzyl analogues of iPAM are poor substrates for cytochrome P450, are not cytotoxic and posses no a...

Curcumin analogues were evaluated for COX-2 inhibitory as anti-inflammatory activities. The designed analogues significantly enhance COX-2 selectivity. The three compounds could dock into the active site of COX-2 successfully. The binding energies of -8.2, - 7.6 and -7.5 kcal/mol were obtained for three analogues of curcumin respectively. Molecular docking study revealed the binding orientation...

[ru(terpy)(bpy)(l)]pf6 complexes, where terpy is 2,2΄:6′,2″– terpyridine, bpy is 2,2΄ - bipyridine and l is monoanions of  4 - bromophenylcyanamide (4 - brpcyd), 4-methoxyphenylcyanamide (4 - meopcyd), 2, 4 - dibromophenylcyanamide (2,4 - br2pcyd), 2,4-dimethylphenylcyanamide (2,4 - me2pcyd), 2 - methylphenylcyanamide  (2 - mepcyd), phenylcyanamide  (pcyd) and naphtylcyanamide  (ncyd)  have bee...

this paper describes 3d-qsar analysis and biological evaluation of 1,5-benzodiazepine analogues. benzodiazepine nucleus with its simple structure gives a good opportunity for further modification regarding an increase of its antimicrobial activity. we synthesized a series of benzodiazepine analogues from condensation of various chalcones and halo substituted o-phenelynene diamines. all compound...

H. Piperidine Analogues of Phenyltropanes 967 III. Cocaine Analogues 969 A. Stereoisomers of Cocaine 970 B. Phenyl Ring Substituted Cocaines 970 C. 2â-Substituted Cocaines 973 1. 2â-Substituted Cocaines 973 2. 2â-Substituted 4′-Iodococaines 977 D. N-Modified Cocaines 978 E. 3â-Carbamoyl Analogues of Cocaine 981 F. 3â-Alkylphenyltropanes 982 G. 6/7-Substituted Cocaine and Pseudococaine 982 H. 6-...

This review will describe the recent advances in the synthesis of C-nucleosides with inhibitory activity of inosine monophosphate dehydrogenase (IMPDH), a key enzyme in the biosynthesis of guanine nucleotides. The review will cover synthetic approaches of structural analogues showing modifications in the furanose ring as well as in the heterocyclic base. Heterocyclic sugar nucleoside analogues ...