Current Research in Pharmaceutical Sciences

108-113

Authors: Neha Sahu, Jagdish K Sahu and Atul Kaushik

Triazole is an entity which is being synthesized in many of its derivative form from past few years; the entity is major source of interest for many of medicinal chemist to explore its various pharmacological potentials. Various methods for synthesizing triazoles are discussed with their chemistry. Studying this chemistry different substituted and fused compounds of triazole are analyzed here for varying pharmacological activities. In present article we review the chemistry of triazole and its pharmacological actions as antihelmintics, anticancer, antifungal and anti-inflammatory agent by studying its various synthesized derivatives.

122-131

Authors: H K Sharma and V Alagarsamy

In this study we aimed to fix Rungia repens (L) Nees botanical identity, macroscopical, microscopical diagnostic characters and to isolate the bio-active principle responsible for biological actions shown by ethyl acetate and methanol extracts. Bioactive compounds were isolated by running column chromatography, characterized and percentage of activity of bioactive principle was calculated. Microscopical study reveals the characteristic nature of stomata, trichome, leaf mid rib and stem. The extracts were found to be non toxic upto the dose of 3000 mg/kg of Rungia repens ethyl acetate extract (RREAE) and methanolic extract (RRME) respectively. RREAE and RRME produced a significant and dose dependent inhibition of analgesic, anti inflammatory and antipyretic activity. Bioactive principle isolated was a flavonoid luteolin shows maximum activity equal to that of standard drug. We believe that the antipyretic, analgesic, and anti-inflammatory activity of the RREAE and RRME were due to its bioactive principle flavonoid luteolin present in the extract.

138-143

Authors: Asheesh Singh, Amit Jain and Bhawna Mishra

A QSAR study on 4-benzylideneamino-benzenesulfonamide & 4-phenyliminomethyl-benzenesulfonamides derivatives as selective cyclooxygenase-2 (COX-2) & COX-1 inhibitors was performed with 21 (16 training + 5 test) compounds. Molecular modeling studies were performed using Chemoffice 6.0 supplied by cambridgesoft. The sketched structures were subjected to energy minimization and the lowest energy structure was used to calculate the physiochemical properties. The regression analysis was carried out using a computer program called VALSTAT. The best models were selected from the various statistically significant equations. The substitution Different monosubstituents preferably at the 3- or 4-position of the phenyl ring had the greatest influence on selectivity (COX-1 & COX-2). Replacement of the 4-hydroxy moiety with an electron withdrawing group such as 4-fluoro, 4-methoxycarbonyl, or 4-nitro substituents increased inhibitory potency and selectivity. However, 3-nitro substituent resulted in loss of inhibitory potency. On the other hand, the 4-N, N-dimethylamino substituent exhibited potent and selective inhibition of cyclooxygenase. Among these compounds with monosubstituted at the para-position, cyclooxygenase the inhibitory selectivity order was 4-F > 4-CO2Me > 4-NMe2 > 4-NO2 > 4-OH > unselective 3-NO2. The analysis resulted in QSAR equation, which suggests that, n=16, r=0.880, r2=0.774, adjusted squared multiple R=0.713, Standard error of estimate(s) = 0.106 & validated r2 (q2) =0.671. This study can help in rational drug design of new cyclooxygenase-2 inhibitor with predetermined affinity.

148-153

Authors: Veerendra Sharma, Pooja Sinoriya and S C Mehta

To investigate the anticonvulsant and CNS depressant activity of methanolic extracts of whole plant of Sida acuta and Sida rhombifolia in mice. The methanolic extract of whole plant of Sida acuta (MESA) and Sida rhombifolia (MESR) (100, 200 and 400 mg/kg, p.o.) was studied for its anticonvulsant effect on maximal electroshock (MES) induced seizures and Pentylenetetrazole (PTZ) induced seizures and CNS depressant activity at the same dose level using traction test, rota rod and locomoter activity in mice. MESA and MESR at dose 100, 200 and 400 mg/kg significantly reduced the duration of the seizures as compared to control group. In CNS depressant activity and the mean time duration on rotating rod was significantly decreased (P<0.0001) and decline in motor co-ordination.