AN EFFICIENT MICROWAVE ASSISTED MULTICOMPONENT SYNTHESIS OF SOME 7-AMINO-3-(SUBSTITUTED PHENYL)-5-(SUBSTITUTED PHENYL)-[1,2,4]TRIAZOLO[4,3A]PYRIMIDINE-6-CARBONITRILE DERIVATIVES

A series of 7-amino-3-(substituted phenyl)-5-(substituted phenyl)-[1,2,4]triazolo [4,3a] pyrimidine-6-carbonitrile derivatives were synthesized from 4-amino-2-hydroxy (OR mercapto)-6-(substituted phenyl)-pyrimidine-5-carbonitrile, hydrazine hydrate and aromatic aldehydes. The derivatives were obtained in good yields by the microwave-assisted one-pot protocol in very short reaction time. The synthesized compounds were studied for QSAR by subjecting to a prediction of biological activities applying computer programme PASS. It is found that 7-Amino-3-(4-chloro-phenyl)-5-(2,4-dichloro-phenyl)-[1,2,4]triazolo[4,3-a]pyrimidine-6-carbonitrile is a promising anticonvulsant agent; which can be synthesized by an efficient, promising, and green synthetic method with high yield

Synthesis and QSAR Study of Some HDL Cholesterol Increasing Quinazolinone Derivatives

We describe here an easy and efficient method to obtain S-alkylated derivatives of thio-quinazolinone using different alkylating agents via a solvent-free microwave-assisted method. The alkylated thio quinazolinones were further sequentially condensed with hydrazine hydrate and different aromatic aldehydes to get the hydrazones, which were studied for QSAR. The synthesized compounds were subjected to a prediction of biological activities. A software application (PASS) was used for this purpose. The relationship between structure and different biological activities was studied and the different derivatives were recommended for the screening of some specific activities like anti-tuberculosic, anti-mycobacterial and HDL cholesterol increasing activities

Synthesis and QSAR Study of (4-Oxo-3-aryl-3,4-dihydro-quinazolin-2-ylsulfanyl)-propionic Acid arylidene/aryl-ethylidene-hydrazides via Microwave Assisted Solvent Free Reations

In the present work, s-alkylated derivatives of thio-quinazolinone were obtained using Methyl 2-chloro propionate via a solvent-free microwave-assisted method. The alkylated thio quinazolinones were further sequentially condensed with hydrazine hydrate and different aromatic aldehydes to get the hydrazides, which were studied for QSAR. The synthesized compounds were subjected to a prediction of biological activities. A software application (PASS) was used for this purpose. . The relationship between structure and different biological activities was studied and the different derivatives were recommended for the screening of some specific activities like anti-tuberculosic, anti-mycobacterial & HDL cholesterol increasing activities

Synthesis, X-ray diffraction study and biological activity of 7-hydroxy-4-methylquinolin-2(1<i>H</i>)-one

1659-1662The compound 7-hydroxy-4-methylquinolin-2(1H)-one (HMQ) has been synthesized by an easy and efficient microwave-assisted method.The structure of the compound has been confirmed on the basis of its IR, 1H NMR spectral data and elemental analyses. The sample has been subjected to X-ray diffractometry to elucidate structural information. The structure of the compound has been found to be orthorhombic belonging to base centered system. The accountability of strain broadening effects with respect to natural particle size is also examined and discussed. The compound has been screened for the antibacterial and antifungal activities. </i

Synthesis of Some New 2-Methyl -1,4-benzothiazine-3(1H)- one Derivatives as Potential Vasodilators

The increase in the internal diameter of a blood vessel that results from relaxation of smooth muscle within the wall of the vessel is vasodilation. This causes an increase in blood flow and a decrease in systemic vascular resistance. Some substances produced by tissue deprived of fresh blood seem to be responsible for the dilation. Many products of metabolism bring about the action, CO2 and acids are among them. Dilation of vessels is necessary to restore local environment of tissues and normal metabolism. It may prove to be potential in the treatment of different cardiac disorders like atherosclerosis, where, the blood vessels are narrowed due to deposition of plaque of substances like cholesterol etc. 1,4-benzothiazines have been reported to possess wide range of pharmacological and biological activities. Here, we report the synthesis and biological activity of some new arylidenehydrazino-(1H)-1,4-benzothiazines. The synthesized compounds were subjected to a prediction of biological activities. A software application (PASS) was used for this purpose. The relationship between structure and different biological activities was studied and it was found that the arylidenehydrazino-(1H)-1,4-benzothiazines are expected to be potential vasodilators