Farmakološko djelovanje izatina i njegovih derivata

Isatin is an endogenous compound identified in humans that possesses wide range of biological activities. Isatin has anxiogenic, sedative, anticonvulsant activity and acts as a potent antagonist on atrial natriuretic peptide receptors in vitro. A series of p-substituted isatin semicarbazones have shown anticonvulsant activity in MES, scPTZ and scSTY tests. Various isatin N-Mannich bases of isatin-3-thiosemicarbazones have shown antiviral and tuberculostatic activity. Methisazone is an effective compound against variola and vaccinia viruses. The N-dimethyl and morpholino derivative of 5-methyl isatin and trimethoprim exhibited an EC50 of more than 4.3 and 17.7 microgram mL-1 and 17.7 microgram mL-1, respectively. Isatin (3-o-nitrophenyl)hydrazone has shown activity against Walker carcinoma-256. Various substituted indolinones showed antitubercular activity against M. tuberculosis H37Rv with MIC ranging from 10-20 microgram mL-1. Isatin derivatives of Mannich bases had fibrinolytic, muscle relaxant, antiallergic, immunosuppressant, and antithrombotic activity. Isatin showed cardioinhibitory effect on frog heart, and hypotensive, respiratory depression and antidiuretic effects.Izatin je endogeni spoj prisutan u organizmu čovjeka koji posjeduje niz farmakoloških učinaka. Izatin djeluje kao antioksidans, sedativ i antikonvulziv. In vitro je snažni antagonist na receptorima za natrijeve ione u atriju. Serija p-supstituiranih semikarbazona izatina pokazala je antikonvulzivno djelovanje u MES, scPTZ i scSTY testovima, a N-Mannichove baze izatina i izatin-3-tiosemikarbazona virustatsko i tuberkulostatsko djelovanje. Metisazon je učinkovit protiv infekcija variola i vakcinia virusima. EC50 N-dimetil i morfolino derivata 5-metilizatina i trimetoprima veći je od 4,3, odnosno 17,7 g mL-1. Izatin (3-o-nitrofenilhidrazon) inhibira rast tumorskih stanica Walker-256, a supstituirani indolinoni su aktivni protiv M. tuberculosis H37Rv (MIC vrijednosti 1020 g mL-1. Mannichove baze izatina djeluju kao fibrinolitici, miorelaksansi, antihistaminici, imunosupresivi i antitrombotici. Izatin ima kardioinhibitorni učinak na srce žabe, a djeluje i kao hipotenziv, depresor respiracije i antidiuretik

Farmakološko djelovanje izatina i njegovih derivata

Isatin is an endogenous compound identified in humans that possesses wide range of biological activities. Isatin has anxiogenic, sedative, anticonvulsant activity and acts as a potent antagonist on atrial natriuretic peptide receptors in vitro. A series of p-substituted isatin semicarbazones have shown anticonvulsant activity in MES, scPTZ and scSTY tests. Various isatin N-Mannich bases of isatin-3-thiosemicarbazones have shown antiviral and tuberculostatic activity. Methisazone is an effective compound against variola and vaccinia viruses. The N-dimethyl and morpholino derivative of 5-methyl isatin and trimethoprim exhibited an EC50 of more than 4.3 and 17.7 microgram mL-1 and 17.7 microgram mL-1, respectively. Isatin (3-o-nitrophenyl)hydrazone has shown activity against Walker carcinoma-256. Various substituted indolinones showed antitubercular activity against M. tuberculosis H37Rv with MIC ranging from 10-20 microgram mL-1. Isatin derivatives of Mannich bases had fibrinolytic, muscle relaxant, antiallergic, immunosuppressant, and antithrombotic activity. Isatin showed cardioinhibitory effect on frog heart, and hypotensive, respiratory depression and antidiuretic effects.Izatin je endogeni spoj prisutan u organizmu čovjeka koji posjeduje niz farmakoloških učinaka. Izatin djeluje kao antioksidans, sedativ i antikonvulziv. In vitro je snažni antagonist na receptorima za natrijeve ione u atriju. Serija p-supstituiranih semikarbazona izatina pokazala je antikonvulzivno djelovanje u MES, scPTZ i scSTY testovima, a N-Mannichove baze izatina i izatin-3-tiosemikarbazona virustatsko i tuberkulostatsko djelovanje. Metisazon je učinkovit protiv infekcija variola i vakcinia virusima. EC50 N-dimetil i morfolino derivata 5-metilizatina i trimetoprima veći je od 4,3, odnosno 17,7 g mL-1. Izatin (3-o-nitrofenilhidrazon) inhibira rast tumorskih stanica Walker-256, a supstituirani indolinoni su aktivni protiv M. tuberculosis H37Rv (MIC vrijednosti 1020 g mL-1. Mannichove baze izatina djeluju kao fibrinolitici, miorelaksansi, antihistaminici, imunosupresivi i antitrombotici. Izatin ima kardioinhibitorni učinak na srce žabe, a djeluje i kao hipotenziv, depresor respiracije i antidiuretik

Anticonvulsant and Sedative-Hypnotic Activities of N-Acetyl / Methyl Isatin Derivatives

A series of N-methyl/acetyl 5-(un)-substituted isatin-3-semicarbazones were screened for anticonvulsant and sedative-hypnotic activities. The results revealed that protection was obtained in all the screens i.e., Maximal electroshock, (MES) subcutaneous pentylene tetrazole (scPTZ) and subcutaneous strychnine (scSTY) screens. Three compounds (2a,2e and 2i) possessed anti-MES activity and all the compounds were less neurotoxic than phenytoin, carbamazepine and phenobarbital. All the compounds were completely non-toxic at 4h when compared to phenytoin, carbamazepine and phenobarbital, which were toxic at 100 and 300 mg/kg respectively. Compounds 2a, 2b, 2e, 2g and 2i emerged as the active compounds in oral MES screen. Selected compounds were evaluated for quantification studies in MES, scPTZ and neurotoxicity screens after i. p (2b, 2i) and oral administration (2a, 2g) in rats. Among all the compounds 2a, 2b and 2g emerged as broad-spectrum compounds as indicated by their protection in MES, scSTY and scPTZ screens. All the compounds except compound 2b showed significant sedative-hypnotic activity

Exploring the effect of workplace spirituality on job embeddedness among higher secondary school teachers in Ernakulam district

The quality of education is determined by the quality of the teachers. As teachers are entrusted with the responsibility of shaping and guiding the future citizens of a nation, it is essential for them to be involved and committed toward their job. This brings out the importance of retaining teachers in their job. The concept of workplace spirituality (WPS) brings in the very feeling of being connected to the workplace, which, undoubtedly helps them to remain attached to the job. The study tries to understand the relationship between WPS and job embeddedness (JE) among the higher secondary school teachers in Ernakulam District. WPS was measured using the scale adapted from Milliman et al. and JE was measured using the scale developed by Mitchell et al. A sample size of 105 was selected using simple random sampling method. The study found a satisfactorily good level of WPS and JE among the respondents. The result of the study also shows a significant positive relationship between WPS and JE

IoT: Effective Authentication System (EAS) using Hash based Encryption on RFID Attacks

Internet of Things (IoT) is undoubtedly a well-known research area. Security on IoT communication services is the major challenge with advanced technology and devices. This paper mainly focusing on Perceptron layer based attacks and counter measures based on Effective Authentication System (EAS). This paper is ordered as outlining IoT Architecture, Types of Threats ,Perceptron Layer  based attacks, sensor based communication services ,RFID mechanism ,Tag identify and verification by back end server and Hash based Effective Authentication System (EAS)  to avoid pseudonym attacks .This paper proposes EAS as security measure by preventing   privacy attack, pseudonym attack, location tracking and asynchronous attack