Sinteza i preliminarna ispitivanja antikonvulzivnog djelovanja derivata benzotiazol-2-il tiadiazola

Various N-(5-chloro-6-substituted-benzothiazol-2-yl)-N\u27-(substituted phenyl)-[1,3,4]thiadiazole-2,5-diamines (5a-t) were designed and synthesized starting from substituted acetophenones. Structures of all the compounds were confirmed on the basis of spectral and elemental analyses. All the newly synthesized compounds were screened for their anticonvulsant activity and were compared with the standard drug phenytoin sodium. Interestingly, all the compounds showed protections against seizures in the range 50-100 % indicative of the promising nature of the compounds against the seizure spread. Compounds 5b and 5c showed complete protection against MES induced seizures.U radu je opisano dizajniranje i sinteza različitih N-(5-klor-6-supstituiranih-benzotiazol-2-il)-N\u27-(supstituiranih fenil)-[1,3,4]tiadiazol-2,5-diamina (5a-t) polazeći od odgovarajućih acetofenona. Strukture spojeva određene su na temelju spektroskopskih podataka i elementarne analize. Ispitano je antikonvulzivno djelovanje svih novosintetiziranih spojeva i uspoređeno s djelovanjem natrijeve soli fenitoina. Spojevi 5b i 5c pružaju potpunu zaštitu od konvulzija uzrokovanih MES-om, a svi spojevi štite od konvulzija u rasponu od 50 do 100 %

QSAR Optimization of Benzofuran and Benzothiophene Sulfono Biphenyl as Potent PTPase-1B Inhibitors

ABSTRACT: Insulin resistance is associated with a defect in protein tyrosine phosphorylation in the insulin signal transduction cascade. Protein tyrosine phosphatase (PTPase) enzyme dephosphorylates the active form of insulin receptor and thus attenuates its tyrosine kinase activity, therefore the need of potent PTPase inhibitor is there with that intention the Quantitative structure-activity relationship QSAR was performed. QSAR has been established on a series of compounds of novel sulfono biphenyl analogs using SYSTAT (Version 7.0) software, for their PTPase-1B inhibitor activity, in order to understand the essential structural requirement for binding with the receptor. Among several 2D QSAR models, one for a series was selected on the basis of high correlation coefficient, least standard deviation, & high value of significance for maximum no. of subject was considered. The interpreted data signify the essentiality of Benzofuran ring in the designing of the new PTPase-1B inhibitors and any substitution on the biphenyl and sulfonyl phenyl is going to decrease its activity. Key words: QSAR, PTPase-1B inhibitor, Sulfono biphenyl analog

Benzothiazole incorporated thiazolidin-4-ones and azetidin-2-ones derivatives: Synthesis and in vitro antimicrobial evaluation

In this study, a series of novel thiazolidin-4-ones (5a–g) and azetidin-2-ones (6a–g) were synthesized from N-(6-chlorobenzo[d]thiazol-2-yl)hydrazine carboxamide derivatives of the benzothiazole class. Antimicrobial properties of the title compound derivatives were investigated against one Gram (+) bacteria (Staphylococcus aureus), three Gram (−) bacteria (Escherichia coli, Pseudomonas aeruginosa, Klebsiella pneumoniae) and five fungi (Candida albicans, Aspergillus niger, Aspergillus flavus, Monascus purpureus and Penicillium citrinum) using serial plate dilution method. The investigation of antibacterial and antifungal screening data revealed that all the tested compounds showed moderate to good inhibition at 12.5–200 μg/mL in DMSO. It has been observed that azetidin-2-ones derivatives are found to be more active than thiazolidin-4-ones derivatives against all pathogenic bacterial and fungal strains