Synthesis and Antithyroid Activity of Pyridine, Pyrimidine and Pyrazine Derivatives of Thiazole-2-thiol and 2-Thiazoline-2-thiol.

Lagorce, Jean F.; Comby, Frédéric; Rousseau, Annick; Buxeraud, Jacques; Raby, C

doi:10.1248/cpb.41.1258

Cited by 19 publications

(12 citation statements)

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“…While halogen bonding involving the halogenated thyroid enzymes is often the focus of studies in this area, the role of I 2 is also of interest [17,18]. Closely related to this are investigations into the interaction of various antithyroid drugs with I 2 [19].…”

Section: Significance Of Halogen Bonding With Dihalogensmentioning

confidence: 99%

Halogen Bonding with Dihalogens and Interhalogens

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Section: Significance Of Halogen Bonding With Dihalogensmentioning

confidence: 99%

Halogen Bonding with Dihalogens and Interhalogens

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“…Hence, MMI and PTU are the only basic drugs, which have their own limitations and side effects (Bandyopadhyay et al, 2002). Scarcity of medicines for the treatment of hyperthyroidism motivated the workers to look for alternate drugs (Lagorce et al, 1993). During such efforts certain synthetic compounds like 2,3-dihydroxypyridine (Abou-Shaaban et al, 1995), and 1-cyclohexyl-3-(3-quinolyl)-2-thiourea (Laurence et al, 1998), are found to exhibit antithyroid activity.…”

Section: Introductionmentioning

confidence: 99%

Assessment of antithyroid activity of 2,8-disulfanyl-1,9-dihydro-6H-purin-6-one in vitro and in vivo

et al. 2011

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2,8-Disulfanyl-1,9-dihydro-6H-purin-6-one has been examined in vitro and in vivo, for its potential antithyroid effects. It exhibited stable higher order complexation with iodine in vitro, which is a sign of its possible antithyroid activity. The blood assays of rats were carried out using radioimmunoassay technique to determine free triiodothyronine and thyroxin levels and with ELISA method for thyroid stimulating hormone concentration; which showed a decrease in the former two hormone levels and increase in the latter, for the animals treated with 2,8-disulfanyl-1,9-dihydro-6H-purin-6-one as compared to the control groups. Similarly, thyroid histology of the treated animals depicted hyperactive gland conditions with little colloid material and cylindrical shape of follicular epithelium as compared to the normal cuboidal epithelium with sufficient stores of colloid material in the control animals, which confirms the antithyroid activity of the 2,8-disulfanyl-1,9-dihydro-6H-purin-6-one. The results were also compared with the animals treated with methimazole (1-methyl-1H-imidazole-2-thiol), the well known antithyroid drug and it was found that 2,8-disulfanyl-1,9-dihydro-6H-purin-6-one is more potent than methimazole as far as hormonal variations are concerned.

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“…Consequently, antithyroid activity of a number of synthetic and natural compounds was studied. 3 Synthetic antithyroid agents may either act by making stable complexes with iodine or by interfering with thyroid peroxidase (TPO) enzyme. In the first mechanism they make stable electron donoracceptor complexes with molecular iodine produced by the oxidation of iodides, diverting the oxidized iodides away from thyroglobulin and ceasing the biosynthesis of thyroid hormones (T 3 and T 4 ).…”

Section: Introductionmentioning

confidence: 99%

Antithyroid activity of 6-chloropurine

Fatima¹,

Munawar²,

Khan³

et al. 2010

J. Braz. Chem. Soc.

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A atividade antitireóidea do 6-cloropurina, in vitro, foi determinada espectrofotometricamente por estudos de formação de seu complexo com iodo. O complexo mostrou estequiometria de 1:1. A constante de formação do complexo encontrada foi 7,652 × 10 3 L mol -1, o que indicou um bom potencial de 6-cloropurina, como agente antitireóideo. Posteriores verificações mostraram mudanças nos níveis hormonais tireóideos em coelhos machos, in vivo, após administração da dose via intraperitoneal (i.p.) durante 14 dias e medindo os níveis de triiodotironina (T 3 ) e tetraiodotironina (T 4 ) livres, na circulação sanguínea, usando-se a técnica de radioimunoensaio. As análises de sangue mostraram decréscimo nos níveis de T 3 e T 4 livres em animais tratados, quando comparados com os controles. Desta maneira, confirmou-se uma boa atividade antitireóidea do 6-cloropurina.Antithyroid activity of 6-chloropurine was determined, in vitro, by studying its complex formation with iodine spectrophotometrically. The complex exhibited a 1:1 stoichiometry. Formation constant (K c ) of the complex was found to be 7.652 × 10 3 L mol -1, which indicated good antithyroid potential of 6-chloropurine. For further verification, changes in the thyroid hormone levels of the male rabbits were observed, in vivo, after administering the dose through intra peritoneal (i.p.) injections for 14 days and measuring free triiodothyronine (T 3 ) and tetraiodothyronine (T 4 ) levels in the blood serum using radioimmunoassay technique. The blood assays showed decrease in free T 3 and T 4 levels in the treated animals as compared to the control ones thus confirming fairly good antithyroid activity of 6-choloropurine.

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Synthesis and Antithyroid Activity of Pyridine, Pyrimidine and Pyrazine Derivatives of Thiazole-2-thiol and 2-Thiazoline-2-thiol.

Cited by 19 publications

References 0 publications

Halogen Bonding with Dihalogens and Interhalogens

Halogen Bonding with Dihalogens and Interhalogens

Assessment of antithyroid activity of 2,8-disulfanyl-1,9-dihydro-6H-purin-6-one in vitro and in vivo

Antithyroid activity of 6-chloropurine

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