Synthesis and biological studies of triazolo-/thiadiazolo-benzoxazines.

Diethyl bromomalonate (2) with an equimolar amount of 2-aminophenol (1) in the presence of sodium fluoride undergoes a cyclization reaction to form 2H,4H-2-ethoxycarbonyl-3,4-dihydro-3-oxo-1,4-benzoxazine (3). Furthermore, compound 3 undergoes a condensation reaction with hydrazine hydrate in the presence of methanol to yield 2H,4H-2-hydrazinocarbonyl-3,4-dihydro-3-oxo-1,4-benzoxazine (4), which on further reaction with aryl isothiocyanates gave 2H,4H-2-[ (4'-substituted)-phenylthiosemicarbazino]-carbonyl-3,4-dihydro-3-oxo-1,4-benzoxazine (5). Compound 5 on treatment with NaOH, cone.

Microwave-assisted Heterocyclic Dicarboxylic Acids as Potential Antifungal and Antibacterial Drugs.

A series of new dicarboxylic acid derivatives of 1,3,4-thiadiazines, 1,4-benzopiperizines, 1,4-thiazines, 1,3-thiazoles, 1,3-oxazoles and 1,3-imidazoles have been synthesized in 80-87% yield by the environmentally benign microwave induced technique involving the cyclocondensation of 2,3-dibromosuccinic acid with 2-aminothiophenol, o-phenylene diamine, 1,2,4-triazole, amidinothiocarbamide, amidinocarbamide and guanidine hydrochloride. The structures of all newly synthesized compounds have been established on the basis of analytical and spectral data. Evaluation of antibacterial and antifungal activity showed that almost all compounds exhibited better results than reference drugs thus they could be promising candidates for novel drugs.

Synthesis and biological studies of bis (thiadiazole/triazole) by sonication.

5,5-Dimethylcyclohexane-1,3-dione was treated with semicarbazide to yield its acid hydrazide, which on further reaction under ultrasound condition with aryl isothiocyanates gave 1,3-bis-imino-[1-(carboxy)-4-substituted phenylthiosemicarbazide]-5,5-dimethylcyclohexane. This compound in acidic medium gave 1,3-bis-imino-[5-(substituted) phenylamino-1,3,4-thiadiazol-2-yl-]-5,5-dimethylcyclohexane, whereas in basic medium 1,3-bis-imino-[4-(substituted) phenyl-5-mercapto-1,2,4-triazol-3-yl-]-5,5-dimethylcyclohexane was obtained. The synthesized compounds were investigated for their antibacterial activities.

Behavioural effects of parafascicular thalamic lesions in an animal model of parkinsonism.

We recently reported that the centromedian-parafascicular thalamic complex (CM-Pf) degenerates in Parkinson's disease and progressive supranuclear palsy. The contribution of such thalamic pathology to disease symptoms has not yet been established. The present study therefore investigated the behavioural impact of lesioning the corresponding thalamic region (termed Pf) on a range of behaviours present in rodents.

A study of autonomic functions in leprosy.

The two groups of leprosy patients were compared with normal for the evaluation of the functional status of the autonomic nervous system, with the aid of several established procedures. Our findings reveal that in the leprosy patients the adrenergic system is hypo-functional as compared to the cholinergic. Further, in maculoanaesthetic group, there appears to be a physiological Dale's vasomoter reversal when adrenaline was used.