Synthesis and hypotensive activity of some 6-(substituted aryl)-4-methyl-2,3- dihydropyridazin-3-ones

1574-15796-(Substituted aryl)-4-methyl-2, 3-dihydropyridazin-3-ones are synthesized by cyclisation of appropriate β-(substituted aroyl)-2-methylene propionate with hydrazine hydrate in the presence of sodium acetate. The title compounds are tested for hypotensive activity, non-invasively, by tail-cuff method and are found to possess significant hypotensive activity in normotensive rats

Synthesis of some 1,2,4-triazoles as potential antifungal agents

838-841 Some new 3-(p-substituted anilinoethyl)-4-(p-substituted phenyl)-5-thioxo-1,2,4-triazoles 3a-p are synthesized and evaluated for antifungal activity against Candida albicans and Aspergillus niger. </smarttagtype

<span style="font-size:14.0pt;line-height: 115%;font-family:"Times New Roman";mso-fareast-font-family:"Times New Roman"; color:#131313;mso-ansi-language:EN-IN;mso-fareast-language:EN-US;mso-bidi-language: HI;mso-bidi-font-weight:bold" lang="EN-IN">Syntheses and antiinflammatory activity of some 6-aryl-2,3,4,5-tetrahydro-3-pyridazinones</span>

614-619<span style="font-size:14.0pt;line-height: 115%;font-family:" times="" new="" roman";mso-fareast-font-family:"times="" roman";="" color:#262626;mso-ansi-language:en-in;mso-fareast-language:en-us;mso-bidi-language:="" hi"="" lang="EN-IN">6-Aryl-2<span style="font-size:14.0pt;line-height:115%; font-family:" times="" new="" roman";mso-fareast-font-family:"times="" roman";="" color:#515151;mso-ansi-language:en-in;mso-fareast-language:en-us;mso-bidi-language:="" hi"="" lang="EN-IN">, <span style="font-size:14.0pt;line-height:115%; font-family:" times="" new="" roman";mso-fareast-font-family:"times="" roman";="" color:#262626;mso-ansi-language:en-in;mso-fareast-language:en-us;mso-bidi-language:="" hi"="" lang="EN-IN">3<span style="font-size:14.0pt;line-height:115%; font-family:" times="" new="" roman";mso-fareast-font-family:"times="" roman";="" color:#515151;mso-ansi-language:en-in;mso-fareast-language:en-us;mso-bidi-language:="" hi"="" lang="EN-IN">, <span style="font-size:14.0pt;line-height:115%; font-family:" times="" new="" roman";mso-fareast-font-family:"times="" roman";="" color:#262626;mso-ansi-language:en-in;mso-fareast-language:en-us;mso-bidi-language:="" hi"="" lang="EN-IN">4<span style="font-size:14.0pt;line-height:115%; font-family:" times="" new="" roman";mso-fareast-font-family:"times="" roman";="" color:#515151;mso-ansi-language:en-in;mso-fareast-language:en-us;mso-bidi-language:="" hi"="" lang="EN-IN">, <span style="font-size:14.0pt;line-height:115%; font-family:" times="" new="" roman";mso-fareast-font-family:"times="" roman";="" color:#262626;mso-ansi-language:en-in;mso-fareast-language:en-us;mso-bidi-language:="" hi"="" lang="EN-IN">5-tetrahydro-3-pyridazinones <span style="font-size:14.0pt; line-height:115%;font-family:" times="" new="" roman";mso-fareast-font-family:"times="" roman";="" color:#131313;mso-ansi-language:en-in;mso-fareast-language:en-us;mso-bidi-language:="" hi"="" lang="EN-IN">(2c-22c) <span style="font-size:14.0pt;line-height: 115%;font-family:" times="" new="" roman";mso-fareast-font-family:"times="" roman";="" color:#262626;mso-ansi-language:en-in;mso-fareast-language:en-us;mso-bidi-language:="" hi"="" lang="EN-IN">are obtained <span style="font-size:14.0pt;line-height: 115%;font-family:" times="" new="" roman";mso-fareast-font-family:"times="" roman";="" color:#131313;mso-ansi-language:en-in;mso-fareast-language:en-us;mso-bidi-language:="" hi"="" lang="EN-IN">by dehydrocyclisation <span style="font-size:14.0pt; line-height:115%;font-family:" times="" new="" roman";mso-fareast-font-family:"times="" roman";="" color:#262626;mso-ansi-language:en-in;mso-fareast-language:en-us;mso-bidi-language:="" hi"="" lang="EN-IN">of various <span style="font-size:14.0pt;line-height: 115%;font-family:" times="" new="" roman";mso-fareast-font-family:"times="" roman";="" color:#131313;mso-ansi-language:en-in;mso-fareast-language:en-us;mso-bidi-language:="" hi"="" lang="EN-IN">h<span style="font-size:14.0pt;line-height:115%; font-family:" times="" new="" roman";mso-fareast-font-family:"times="" roman";="" color:#3a3a3a;mso-ansi-language:en-in;mso-fareast-language:en-us;mso-bidi-language:="" hi"="" lang="EN-IN">yd<span style="font-size:14.0pt;line-height:115%; font-family:" times="" new="" roman";mso-fareast-font-family:"times="" roman";="" color:#131313;mso-ansi-language:en-in;mso-fareast-language:en-us;mso-bidi-language:="" hi"="" lang="EN-IN">r<span style="font-size:14.0pt;line-height:115%; font-family:" times="" new="" roman";mso-fareast-font-family:"times="" roman";="" color:#3a3a3a;mso-ansi-language:en-in;mso-fareast-language:en-us;mso-bidi-language:="" hi"="" lang="EN-IN">azides <span style="font-size:14.0pt;line-height:115%; font-family:" times="" new="" roman";mso-fareast-font-family:"times="" roman";="" color:#131313;mso-ansi-language:en-in;mso-fareast-language:en-us;mso-bidi-language:="" hi"="" lang="EN-IN">formed <span style="font-size:14.0pt;line-height:115%; font-family:" times="" new="" roman";mso-fareast-font-family:"times="" roman";="" color:#262626;mso-ansi-language:en-in;mso-fareast-language:en-us;mso-bidi-language:="" hi"="" lang="EN-IN">by <span style="font-size:14.0pt;line-height:115%; font-family:" times="" new="" roman";mso-fareast-font-family:"times="" roman";="" color:#131313;mso-ansi-language:en-in;mso-fareast-language:en-us;mso-bidi-language:="" hi"="" lang="EN-IN">the <span style="font-size:14.0pt;line-height:115%; font-family:" times="" new="" roman";mso-fareast-font-family:"times="" roman";="" color:#262626;mso-ansi-language:en-in;mso-fareast-language:en-us;mso-bidi-language:="" hi"="" lang="EN-IN">reaction of appropriate methyl β-aroylpropionate and hydrazine hydrate in the presence of anhydrous sodium acetate.They show promising antiinflammatory activity during their evaluation by carrageenin induced paw edema test in <span style="font-size: 14.0pt;line-height:115%;font-family:" times="" new="" roman";mso-fareast-font-family:="" "times="" roman";color:#515151;mso-ansi-language:en-in;mso-fareast-language:="" en-us;mso-bidi-language:hi"="" lang="EN-IN">ra<span style="font-size:14.0pt; line-height:115%;font-family:" times="" new="" roman";mso-fareast-font-family:"times="" roman";="" color:#131313;mso-ansi-language:en-in;mso-fareast-language:en-us;mso-bidi-language:="" hi"="" lang="EN-IN">ts.</span

A phyto-pharmacological overview on <i style="mso-bidi-font-style:normal">Salvadora oleoides</i> Decne

209-214<span style="mso-fareast-font-family:Calibri; mso-ansi-language:EN-US" lang="EN-US">Salvadora oleoides <span style="mso-fareast-font-family:Calibri;mso-ansi-language:EN-US;mso-bidi-font-style: italic" lang="EN-US">Decne belonging to the family Salvadoraceae is a small, multipurpose tree commonly grown in western Rajasthan and Gujarat states of India. It is also known as Jhal and Badapilu. Many chemical constituents such as carbohydrates, alkaloids, steroids, glycosides, saponins, tannins, triterpenes, mucilage, fats and oils have been reported from its leaves and stems extracts. Because of the presence of these active chemical constituents it possesses anti-inflammatory, analgesic, anti-ulcer, anthelmintic, antibacterial, antifungal and diuretic activities. This review summarizes the traditional claims, phytochemistry and pharmacology of S. oleoides reported so far in scientific literature. </span

Establishment of inherent stability on piracetam by UPLC/HPLC and development of a validated stability-indicating method

A novel comparative force degradation UPLC assay method was developed and validated for Piracetam and its degradation products. Piracetam was subjected to acid (5 M HCl), neutral (water) and alkaline (0.5 M NaOH) hydrolytic conditions at 80 °C, as well as to oxidative decomposition (H2O2) at room temperature. Photolytic studies were carried out by exposing this drug into sunlight (60,000–70,000 lux) for 2 d. Additionally, the solid drug was subjected to 50 °C for 60 days in a hot air oven for thermal degradation. The UPLC chromatographic separation was performed on Acquity UPLC BEH C18 column (1.7 μm, 2.1 mm × 150 mm) using isocratic mode (ACN:water, 25:75 v/v) at a flow rate of 0.15 mL min−1 and HPLC chromatographic separation was achieved on phenomenex C18 using isocratic mode (ACN:10 mM ammonium acetate, pH 5.0, 20:80 v/v) at a flow rate of 0.9 mL/min. Piracetam was found to degrade only in the base and shows stable behavior under all stress conditions. The UPLC and HPLC linearity of the proposed method was investigated in the range of 10–50 μg mL−1. The r2 value of UPLC and HPLC was found to be 0.999 and 0.999, respectively. Method detection limit (MDL) and Method quantification limit (MQL) were found to be 0.180 μg mL−1and 1.10 μg mL−1 for UPLC and 0.500 μg mL−1and 1.700 μg mL−1 for HPLC respectively. The %RSD values for intra-day and inter-day precision were <1.2%, confirming that the method was sufficiently precise. The validation studies were carried out fulfilling ICH requirements. The developed method was simple, fast, accurate and precise and hence could be applied for routine quality control analysis of Piracetam in solid dosage forms

A phyto-pharmacological overview on Salvadora oleoides Decne

Salvadora oleoides Decne belonging to the family Salvadoraceae is a small, multipurpose tree commonly grown in western Rajasthan and Gujarat states of India. It is also known as Jhal and Badapilu. Many chemical constituents such as carbohydrates, alkaloids, steroids, glycosides, saponins, tannins, triterpenes, mucilage, fats and oils have been reported from its leaves and stems extracts. Because of the presence of these active chemical constituents it possesses anti-inflammatory, analgesic, anti-ulcer, anthelmintic, antibacterial, antifungal and diuretic activities. This review summarizes the traditional claims, phytochemistry and pharmacology of S. oleoides reported so far in scientific literature

Isolation and hypotensive activity of five new phytoconstituents from chloroform extract of flowers of <i>H</i><i style="">ibiscus rosasinensis</i> Linn.

806-811Three extracts of Hibiscus rosasinensis Linn have been prepared and studied for their hypotensive activity. Hydroalcoholic extract is found to exhibit prominent activity when compared to the reference standard minoxidil followed by chloroform extract. In an attempt to isolate the active constituents responsible for this activity, five new phytoconstituents have been isolated and their structures are elucidated from spectral evidence (IR, NMR and mass spectra). Hypotensive activity of these compounds is also studied

Synthesis, spectral characterization, and pharmacological screening of some 4-[{1-(aryl)methylidene}-amino]-3-(4-pyridyl)-5-mercapto-4H-1,2,4-triazole derivatives

Background : Pain is an unpleasant and subjective sensation that results from a harmful sensorial stimulation, which alerts the body about current or potential damage to its tissues and organs. Fever is a complex physiological response triggered by infections or aseptic stimuli. Elevation in body temperature occurs when the concentration of prostaglandin E 2 (PGE 2 ) increases within parts of the brain. Triazole derivatives have been found to possess various pharmacological and biological activities, such as, anti-inflammatory, analgesics, antipyretic, and antifungal. Materials and Methods : Various 4-[{1-(aryl)methylidene}-amino]-3-(4-pyridyl)-5-mercapto-4H-1,2,4-triazole derivatives were synthesized by a sequence of reactions starting from isonicotinic acid hydrazide. The synthesized compounds were screened for in-vivo analgesic by the tail-flick method and anti-pyretic activities at a dose of 25 and 100 mg/kg body weight respectively. The antipyretic activity was evaluated using Brewer′s yeast induced pyrexia in rats. Fever was induced by subcutaneously injecting 20 ml/kg of 20% aqueous suspension of Brewer′s yeast in normal saline. Results and Discussion : The analgesic screening results revealed that the compounds 3b, 3c, and 3d exhibited excellent analgesic activity at 60 and 90 minutes compared to the standard drug (Analgin). Results revealed that the compounds 3a, 3e, and 3f significantly decreased the temperature of pyretic (P<0.001) rats at one, three and six hours after compound administration as compared to Aspirin (standard drug). Conclusion : Compounds 3b, 3c, and 3d exhibited significant analgesic activity comparable with the standard drug analgin, using the tail flick model. Compounds 3a, 3e, and 3f showed significant anti-pyretic activities comparable with the standard drug aspirin using the yeast-induced pyrexia model