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We report the preparation and cytotoxicity of two new eugenol derivatives that contain 1,3,4-oxadiazole, as novel inhibitors of thymidylate synthase; these derivatives are shown to be promising chemotherapeutic agents.

Compounds 10 and 14 arrest the cell cycle at the G1 phase and induce apoptosis without any necrosis in MDA-MB-231 cells.

1,3,4-oxadiazole is an aromatic heterocycle with –N=C=O- linkage. 1,3,4-oxadiazole derivatives possess remarkable biological properties; antimicrobial anti-inflammatory, anti-cancer, antitubercular, antioxidant, antiviral, and anti-diabetic. This scaffold is present in many marketed drugs, such as Raltegravir, Tiodazosin, Nesapidil, and Zibotentan. 1,3,4-oxadiazole derivatives have displayed significant anti-cancer potential with a diverse mode of actions viz. growth factors, enzymes, kinases, etc. The present review gives an overview of the anti-cancer potential of 1,3,4-oxadiazoles derivatives in cancer drug discovery and development from the last ten years.

Background: The frequent use of antimicrobial agents to treat infections in diabetic patients make them more drug resistant than non-diabetic patients, which accounts for a higher mortality rate of diabetic patients. Therefore, it is a necessity today to synthesize new drugs with dual modes of action as antidiabetic and antibacterial agents. In the present work, new derivatives containing thiazolidinedione and 1,3,4-oxadiaozle have been synthesized and screened for PPAR-γ and antibacterial activities. Methods: Compounds 5-12 have been synthesized from 2-methoxy benzaldehyde and thiazolidinedione and characterized using different spectroscopic techniques such as IR, NMR, and mass spectrometry. These compounds were tested for in vitro PPAR-γ transactivation, PPAR-γ gene expression, and antibacterial activities. Finally, molecular docking was carried out to see the binding interactions of molecules with the target protein. Results: All the compounds follow the Lipinski rule suggesting the synthesized derivatives have good drug-likeness properties. Compounds 11 and 12 exhibited promising PPAR-γ transactivation with 73.69% and 76.50%, respectively, as well as showed significant antibacterial activity with comparable MIC of 3.12 μg/disc to standard drug amoxicillin. The docking result was found to be consistent with the in vitro PPAR-γ transactivation results. Conclusion: Compounds 11 and 12 can be further investigated as lead molecules for the development of new and effective antidiabetic and antibacterial agents.

In the present work, a library of fifteen 2-hydroxy benzothiazole-linked 1,3,4 -oxadiazole derivatives have been synthesized and confirmed using different analytical techniques. All of the synthesized compounds have been tested for antibacterial and in silico pharmacokinetic studies for the first time. From the ADME predictions, compound 4 showed the highest in silico absorption percentage (86.77%), while most of the compounds showed more than 70% absorption. All of the compounds comply with the Lipinski rule of 5, suggesting that the compounds possess good drug likeness properties upon administration. Furthermore, all of the compounds follow the Veber rule, indicating good bioavailability and good intestinal absorption. The antibacterial results exhibited excellent to moderate activity. Compounds 5, 9, 12, 14, 15, 16, and 17 were the most active compounds against the tested bacterial strains. Compound 14 showed comparable MIC 6.25 +/- 0.2 mu g/disc to the standard drug amoxicillin against the tested Gram-positive bacterial strains. Compounds 5, 14, 17 exhibited MIC 12.5 +/- 0.8 mu g/disc, which was comparable to the standard drug against E. faecalis. It can be concluded that the synthesized compound could be used as a lead molecule in the development of new antibacterial agents with high efficacy.

Eugenol chemically known as 4-allyl-2-methoxyphenol is a major phenolic component of Syzigium aromaticum and associated with significant biological activities. In the present work, new eugenol 1,2,3-triazole derivatives have been synthesized, characterized using NMR, mass spectrometry, IR, and elemental analysis and screened for their anticancer activity against breast cancer cells. Compound 9, namely 3-(4-((4-allyl-2-methoxyphenoxy)methyl)-1H-1,2,3-triazol-1-yl)-N'-(4-methylbenzoyl) benzohydrazide was found to be the most potent candidate and better than eugenol in exhibiting cytotoxicity with IC50 6.91 and 3.15 μM, comparable to Doxorubicin with IC50 6.58 and 3.21 μM against MDA-MB-231 and MCF-7 cells, respectively. Furthermore, compound 9 treated MCF-7 cells as observed by propidium iodide staining significantly increased cell population of S phase and G2 phase to 43.64% and 35.19%, respectively therefore arresting cell cycle at G2 and S phase. These results indicate that eugenol linked 1,2,3-triazole ring could be used as anticancer leads for the treatment of this deadly diseases.

This investigation aimed at evaluating the efficiency of micro and nanoclays as a low-cost material for the removal of crystal violet (CV) dye from an aqueous solution. The impacts of various factors (contact time, pH, adsorbent dosage, temperature, initial dye concentration) on the adsorption process have been taken into consideration. Six micro and nanoclay samples were obtained by treating clay materials collected from different locations in the Albaha region, Saudi Arabia. Out of the six tested micro and nanoclays materials, two (NCQ1 and NCQ3) were selected based on the highest adsorption efficiency for complete experimentation. The morphology and structure of the selected micro and nanoclay adsorbents were characterized by various techniques: SEM-EDX, FTIR, XRF, XRD, and ICP-MS. The XRF showed that the main oxides of both nanoclays were SiO2, Al2O3, Fe2O3, K2O, CaO, and MgO, and the rest were impurities. All the parameters affecting the adsorption of CV dye were optimized in a batch system, and the optimized working conditions were an equilibrium time of 120 min, a dose of 30 mg, a temperature of 25 °C, and an initial CV concentration of 400 mg/L. The equilibrium data were tested using nonlinear isotherm and kinetic models, which showed that the Freundlich isotherm and pseudo-second-order kinetics gave the best fit with the experimental data, indicating a physico-chemical interaction occurred between the CV dye and both selected micro and nanoclay surfaces. The maximum adsorption capacities of NCQ1 and NCQ3 adsorbents were 206.73 and 203.66 mg/g, respectively, at 25 °C. The thermodynamic factors revealed that the CV dye adsorption of both micro and nanoclays was spontaneous and showed an exothermic process. Therefore, the examined natural micro and nanoclays adsorbents are promising effective adsorbents for the elimination of CV dye from an aqueous environment.

Despite the advancements in the development of anticancer agents, more effective and safer anticancer drugs still need to be developed as the current agents cause unwanted side effects and many patients have become drug resistant. 1,2,3-Triazoles, due to their remarkable biological potential, have received considerable attention in drug discovery for the development of anticancer agents. The present review article presents an overview of the recent advances in 1,2,3-triazole hybrids with anticancer potential over the last 2 years, their chemical structures, structure-activity relationships, and mechanisms of action, as well as insights into the docking studies.

Callistemon lanceolatus (Sm.) Sweet grows all over the world and used to treat cough and bronchitis. The air-dried powder of the aerial parts was exhaustively extracted with methanol and the concentrated extract was adsorbed on silica gel for preparation of slurry. It was dried and subjected to silica gel column packed in petroleum ether. The column was eluted with organic solvents in order of increasing polarity to isolate 1-triacosanol (1), n-eicosanyl palmitate (2), n-heptadecanyl arachidate (3), n-tricosanyl palmitate, (4), 4-hydroxyphenethyl carbocerate (5), 4-hydroxyphenethyl gheddate (6), urs-12-en-3α-acetoxy-18β-H-28-oic acid (7) and stigmast-5-en-3β-ol-3β-D-glucuronopyranoside (8). Among them, compound 5 and 6 were new fatty acid ester isolated from this plant. Compound 7 showed MIC 32 µg/mL against E. coli which was comparable to amoxicillin having same MIC 32 µg/mL. Compound 5 and 6 showed significant antioxidant activity by inhibiting DPPH due to the presence of phenolic groups.

Due to chemotherapy failure, drug resistance, and the advent of multiresistant microbes, new antimicrobial and anticancer agents are needed. The present study has synthesized and screened new 1,3,4-oxadiazole derivatives bearing benzimidazole scaffold for antimicrobial and anticancer activities. The structure of final compounds 8-15 was completely established by NMR (1H, 13C), mass, IR, and elemental analysis. From the antimicrobial study, compounds10 and 15 exhibited promising effects against Gram-positive bacterial strains, S. aureus, and S. epidermidis, with MIC comparable to standard drugs. Also, the same compounds 10 and 15 displayed potent cytotoxicity against MCF-7 breast carcinoma, which was comparable to doxorubicin. Furthermore, docking studies have been performed to explore the binding interaction of the compounds with the target protein.

Natural product produced by plants has been the backbone for numerous anticancer agents. In the present work, natural bioactive thymol based 1,2,3-triazole hybrids have been synthesized and evaluated for anticancer activity in MCF-7 and MDA-MB-231 cancer cells. The synthesized molecules displayed desired pharmacokinetic predictions for an orally available drug. Among the synthesized hybrids, compound 4-((2-isopropyl-5-methylphenoxy)methyl)-1-o-tolyl-1H-1,2,3-triazole (10) was the most potent (IC50 6.17 μM) showing comparable cytotoxity to tamoxifen (IC50 5.62 μM) and 3.2 fold inhibition to 5-fluorouracil (IC50 20.09 μM) against MCF-7 cancer cells. Whereas against MDA-MB-231 cancer cells, compound 10 (IC50 10.52 μM) and 3-(4-((2-isopropyl-5-methylphenoxy)methyl)-1H-1,2,3-triazol-1-yl)benzoic acid (12) (IC50 11.41 μM) displayed 1.42 and 1.3 fold inhibition, respectively to tamoxifen (IC50 15.01 μM) whereas 2.4 fold and 2.2 activity to 5-Florouracil (IC50 25.31 μM). Furthermore, 10 and 12 significantly inhibited thymidylate synthase enzyme with 2.4 and 1.26 fold activity to standard drug, Pemetrexed (IC50 5.39 μM) suggesting their mode of action as thymidylate synthase inhibitors. Cell cycle arrest and annexin V induced apoptosis study of compound 10 showed cell cycle arrest at the G2/M phase and induction of apoptosis in MCF-7 cells. The molecular docking was accomplished onto thymidylate synthase (TS) protein. The active compounds exhibited promising binding interactions and binding affinities into active sites. Finally, density functional theory (DFT) calculations including chemical reactivity and molecular electrostatic potential (MEP) have been performed to confirm the data obtained from docking and biological experiments. The results from this study inferred that compound 10 could be served as a lead molecule for the treatment of breast cancer.

Thymidylate synthase (TS) has been an attention-grabbing area of research for the treatment of cancers due to their role in DNA biosynthesis. In the present study, we have synthesised a library of thiazolidinedione-1,3,4-oxadiazole hybrids as TS inhibitors. All the synthesised hybrids followed Lipinski and Veber rules which indicated good drug likeness properties upon oral administration. Among the synthesised hybrids, compound 9 and 10 displayed 4.5 and 4.4 folds activity of 5-Fluorouracil, respectively against MCF-7 cell line whereas 3.1 and 2.5 folds cytotoxicity against HCT-116 cell line. Furthermore, compound 9 and 10 also inhibited TS enzyme with IC50 = 1.67 and 2.21 µM, respectively. Finally, the docking studies of 9 and 10 were found to be consistent with in vitro TS results. From these studies, compound 9 and 10 has the potential to be developed as TS inhibitors.

The crude extracts from leaves of Jatropha glauca plant grown naturally at Al-Baha region obtained by extraction with ethanol and fractionated using three solvents: petroleum ether, ethyl acetate and methanol were investigated for their in vitro antimicrobial susceptibility. The antimicrobial activity were evaluated against two bacterial strains S. aureus and E. coli, and two common fungal strains Candida albicans and Candida krusei using disc diffusion assay. The crude ethanolic extract and its fractions methanolic and ethyl acetate showed an inhibitory effect against both bacterial and fungal microorganisms. The petroleum ether fraction had no antimicrobial effect. The ethanolic crude extract and methanolic fraction showed higher zone of inhibition, while the ethyl acetate fraction showed the least activity against both bacterial strains. The methanolic fraction was found to possess lowest MIC ≥250 μgml−1 against both tested bacterial strains. Similarly, the ethanolic crude extract and methanol fraction showed zone of inhibition against tested fungal strains with methanolic fraction showed the highest zone of inhibition. However, these observations indicated that the ethanolic crude extract and its methanolic and ethyl acetate fractions exhibited some antimicrobial potency that proves the leaves contain some gradients that have antibacterial and antifungal potential.

A library of 1,2,3-triazole-incorporated thymol-1,3,4-oxadiazole derivatives (6–18) hasbeen synthesized and tested for anticancer and antimicrobial activities. Compounds 7, 8, 9, 10, and 11 exhibited significant antiproliferative activity. Among these active derivatives, compound 2-(4-((5-((2-isopropyl-5-methylphenoxy)methyl)-1,3,4-oxadiazol-2-ylthio)methyl)-1H-1,2,3-triazol-1-yl)phenol (9) was the best compound against all three tested cell lines, MCF-7 (IC50 1.1 μM), HCT-116 (IC50 2.6 μM), and HepG2 (IC50 1.4 μM). Compound 9 was found to be better than the standard drugs, doxorubicin and 5-fluorouracil. These compounds showed anticancer activity through thymidylate synthase inhibition as they displayed significant TS inhibitory activity with IC50 in the range 1.95–4.24 μM, whereas the standard drug, Pemetrexed, showed IC50 7.26 μM. The antimicrobial results showed that some of the compounds (6, 7, 9, 16, and 17) exhibited good inhibition on Escherichia coli (E. coli) and Staphylococcus aureus (S. aureus). The molecular docking and simulation studies supported the anticancer and antimicrobial data. It can be concluded that the synthesized 1,2,3-triazole tethered thymol-1,3,4-oxadiazole conjugates have both antiproliferative and antimicrobial potential.

Thymidylate synthase (TS) has emerged as a hot spot in cancer treatment, as it is directly involved in DNA synthesis. In the present article, nine hybrids containing 1,2,3-triazole and 1,3,4-oxadiazole moieties (6&ndash, 14) were synthesized and evaluated for anticancer and in vitro thymidylate synthase activities. According to in silico pharmacokinetic studies, the synthesized hybrids exhibited good drug likeness properties and bioavailability. The cytotoxicity results indicated that compounds 12 and 13 exhibited remarkable inhibition on the tested Michigan Cancer Foundation (MCF-7) and Human colorectal Carcinoma (HCT-116) cell lines. Compound 12 showed four-fold inhibition to a standard drug, 5-fluoruracil, and comparable inhibition to tamoxifen, whereas compound 13 exerted five-fold activity of tamoxifen and 24-fold activity of 5-fluorouracil for MCF-7 cells. Compounds 12 and 13 inhibited thymidylate synthase enzyme, with an half maximal inhibitory concentration, IC50 of 2.52 &micro, M and 4.38 &micro, M, while a standard drug, pemetrexed, showed IC50 = 6.75 &micro, M. The molecular docking data of compounds 12 and 13 were found to be in support of biological activities data. In conclusion, hybrids (12 and 13) may inhibit thymidylate synthase enzyme, which could play a significant role as a chemotherapeutic agent.

A library of synthesized conjugates of phenoxy acetic acid and thiazolidinedione 5a-m showed potent peroxisome proliferator activated receptor-γ (PPAR-γ) transactivation as well as significant blood glucose lowering effect comparable to the standard drugs pioglitazone and rosiglitazone. Most of the compounds showed higher docking scores than the standard drug rosiglitazone in the molecular docking study. Compounds 5l and 5m exhibited PPAR-γ transactivation of 54.21 and 55.41%, respectively, in comparison to the standard drugs pioglitazone and rosiglitazone, which showed 65.94 and 82.21% activation, respectively. Compounds 5l and 5m significantly lowered the blood glucose level of STZ-induced diabetic rats. Compounds 5l and 5m lowered the AST, ALT, and ALP levels more than the standard drug pioglitazone. PPAR-γ gene expression was significantly increased by compound 5m (2.00-fold) in comparison to the standard drugs pioglitazone (1.5-fold) and rosiglitazone (1.0-fold). Compounds 5l and 5m did not cause any damage to the liver and could be considered as promising candidates for the development of new antidiabetic agents.

A library of novel 1,3,4-oxadiazole and 2-4-thiazolidinedione based bis-heterocycles 7 (a-r) has been synthesized which exhibited significant PPAR-γ transactivation and blood glucose lowering effect comparable with the standard drugs Pioglitazone and Rosiglitazone. Compounds 7m and 7r did not cause body weight gain and were found to be free from hepatotoxic and cardiotoxic side effects. Compounds 7m and 7r increased PPAR-γ gene expression by 2.10 and 2.00 folds, respectively in comparison to the standard drugs Pioglitazone (1.5 fold) and Rosiglitazone (1.0 fold). Therefore the compounds 7m and 7r may be considered as potential candidates for development of new antidiabetic agents.

A library of conjugates of chromones and 2,4-thiazolidinedione has been synthesized by Knoevenagel condensation followed by reduction using hydrogen gas and Pd/C as a catalyst. Compounds 5c and 5e were most effective in lowering the blood glucose level comparable to standard drug pioglitazone. Compound 5e exhibited potent PPAR-γ transactivation of 48.72% in comparison to pioglitazone (62.48%). All the molecules showed good glide score against the PPAR-γ target in molecular docking study. PPAR-γ gene expression was significantly increased by compound 5e (2.56-fold) in comparison to standard drug pioglitazone. Compounds 5e and 5c did not cause any damage to the liver and may be considered as promising candidates for the development of new antidiabetic agents.

A series of 1-(4-methoxyphenyl)-2-[5-{(biphenyl-4-yloxy)methyl}4-(substituted phenyl)-3-mercapto-(4H)-1,2,4-triazol-3-ylthio)] ethanones (6a-6s) and 4-(substituted phenyl)-3-(morpholin/pyrrolidin-4-ylmethylthio)-5-(4-phenylphenoxymethyl)-4H-1,2,4-triazoles (7a-7e) were synthesized in order to obtain new compounds with potent anti-inflammatory and analgesic activity with insignificant ulceration. Among the synthesized compounds, (6c), (6e), (6g) and (6l) from triazole series and (7b) and (7e) from Mannich base series were found to exhibit significant anti-inflammatory activity with 59.69, 59.69, 64.69, 79.84, 54.54, 79.69% and 52.55, 57.50, 72.52, 83.03, 60.06, 84.08% inhibition of paw edema at 3 h and 5 h respectively, in comparison to the standard drug ibuprofen (78.93 and 82.58% at 3 h and 5 h). The active compounds were further tested for their analgesic activity and gastric ulceration study. Compounds 6g, 7b and 7e exhibited significant analgesic activity with reaction time (3.60, 3.22, 3.88 s) respectively at 60 min. without causing any gastric irritation. These compounds were also screened for their in vitro antimicrobial activity, Compounds 6f, 6g, 6h, 6l, 6o, 6p, 7a, 7b and 7c showed significant zone of inhibition against various antimicrobial stains. It is concluded that the compounds 6g, 7b and 7e possess a good spectrum of activities. Compound 7e may be considered potent for development of better anti-inflammatory agent. The antimicrobial activity revealed that most of the compounds showed moderate to significant activity. Compounds containing nitro, chloro, bromo and fluoro group showing better activity. All the compounds from 7a, 7b and 7e were active against gram positive bacteria (S. aureus).

Phytochemical investigation of the antidiabetic chloroform fraction of the ethanolic extract obtained from the aerial parts of Callistemon lanceolatus DC led to the isolation of three new phytoconstituents, one flavone, 8-(1″-hydroxyisopranyl)-5,6-dihydroxy-7,4′-dimethoxy flavone (1) and two phenolic esters, 2,3,4-trihydroxyphenethyl tetracontanoate (2) and 2,3,4-trihydroxyphenethyl tetracontanoate-4-β-xylopyranoside (3). The isolated compound 1 exhibited significant in vivo blood glucose lowering effect comparable to the standard drugs Pioglitazone and Rosiglitazone in streptozotocin induced diabetic rats without causing any toxic effect on the pancreas and liver. Compound 1 showed a glide score of −7.89 against PPAR-γ target in molecular docking studies which is significantly higher than the glide score of reference molecule Rosiglitazone (glide score of −5.77). Compound 1 also exhibited moderate in vitro PPAR-γ transactivation activity of 48.52% in comparison with standard drugs rosiglitazone and pioglitazone, which showed a transactivation activity of 80.47% and 65.27%, respectively. Keywords: Callistemon lanceolatus, Flavone, Phenolic esters, PPAR-γ, Antidiabetic

A library of synthesized conjugates of phenoxy acetic acid and thiazolidinedione 5a-m showed potent peroxisome proliferator activated receptor-γ (PPAR-γ) transactivation as well as significant blood glucose lowering effect comparable to the standard drugs pioglitazone and rosiglitazone. Most of the compounds showed higher docking scores than the standard drug rosiglitazone in the molecular docking study. Compounds 5l and 5m exhibited PPAR-γ transactivation of 54.21 and 55.41%, respectively, in comparison to the standard drugs pioglitazone and rosiglitazone, which showed 65.94 and 82.21% activation, respectively. Compounds 5l and 5m significantly lowered the blood glucose level of STZ-induced diabetic rats. Compounds 5l and 5m lowered the AST, ALT, and ALP levels more than the standard drug pioglitazone. PPAR-γ gene expression was significantly increased by compound 5m (2.00-fold) in comparison to the standard drugs pioglitazone (1.5-fold) and rosiglitazone (1.0-fold). Compounds 5l and 5m did not cause any damage to the liver and could be considered as promising candidates for the development of new antidiabetic agents.

A library of novel bis-heterocycles (III) encompassing 2-mercapto benzothiazole and 1,2,3-triazoles are synthesized using click chemistry approach.

A variety of new S-alkylated triazoles (IX) (19 examples) and related Mannich bases (XII) are synthesized and evaluated for their pharmacological activities.

Phytochemical investigation of the aerial parts of Callistemon lanceolatus DC (Myrtaceae) led to the isolation of two new flavones characterized as 5,7-dihydroxy-6,8-dimethyl- 4′ -methoxy flavone ( 1 ) and 8-(2-hydroxypropan-2-yl)-5-hydroxy-7-methoxy-6-methyl-4′-methoxy flavone ( 2 ) along with the seven known phytoconstituents. The structures of new compounds have been established on the basis of chemical and spectral studies and known compounds were compared with the published literature data. The isolated flavones exhibited blood glucose lowering effect in streptozotocin induced diabetic rats.

Leaves of Platanus orientalis Linn. are used in folk medicine as a wound-healer and ophthalmologic agent. Phytol derivatives from the leaves of plane-tree show anti-ulcer activity. Its analgesic and anti-inflammatory effects for knee pain were known to Persian scientists and hakims.The ethanolic extract of Platanus orientalis Linn. and its various fractions were given at a dose of 100mg/kg po and 200mg/kg po for testing their anti-inflammatory activity by carrageenan induced hind paw edema. The analgesic activity of the ethanolic extract and its fractions has been carried out by tail-flick method and writhing test at a dosage of 200mg/kg po. Gastric ulceration studies have been further carried out to study the ulcerogenic risk evaluation of the ethanolic extract and its various fractions at a dose of 600mg/kg body weight.Among the tested fractions, chloroform fraction exhibited better inhibition (68.33%) at 200mg/kg po dosage when compared to the standard drug Ibuprofen (66.66%) after 3h in the carrageenan induced hind paw edema. The ethanolic extract and all its fractions especially the chloroform (p0.01) showed significant analgesic activity with insignificant ulceration as compared to the standard drug i.e. Ibuprofen. The histopathological study of ethanolic extract and its fractions revealed that none of them cause ulcer.The present study indicates that Platanus orientalis Linn. has significant anti-inflammatory and analgesic effect.

A focused library of novel bis-heterocycles encompassing 2-mercapto benzothiazole and 1,2,3-triazoles were synthesized using click chemistry approach. The synthesized compounds have been tested for their anti-inflammatory activity by using biochemical cyclooxygenase (COX) activity assays and carrageenan-induced hind paw edema. Among the tested compounds, compound 4d demonstrated a potent selective COX-2 inhibition with COX-2/COX-1 ratio of 0.44. Results from carrageenan-induced hind paw edema showed that compounds 4a, 4d, 4e and 4f posses significant anti-inflammatory activity as compared to the standard drug Ibuprofen. The compounds showing significant activity were further subjected to anti-nociceptive activity by writhing test. These four compounds have shown comparable activity with the standard Ibuprofen. Further ulcerogenic studies shows that none of these compounds causing gastric ulceration.

To investigate the anti-inflammatory and anti-nociceptive activities of the crude ethanolic extract of Adiantum capillus veneris Linn. (Adiantaceae) and its various fractions.The ethanolic extract and its fractions were given at a dose of 200 mg/kg po and 300 mg/kg po for testing their anti-inflammatory activity by carrageenan induced hind paw edema. The analgesic activity of the ethanolic extract and its fractions has been carried out by tail-flick method and writhing test at a dosage of 300 mg/kg po. Gastric ulceration studies have been further carried out to study the antiulcer effect of the ethanolic extract and its various fractions at dose of 900 mg/kg body weight.Amongst the tested fractions, the ethyl acetate fraction exhibited better inhibition (67.27%) at 300 mg/kg po dosage when compared to the standard drug Indomethacin (63.63%) after 3h in the carrageenan induced hind paw edema. The anti-inflammatory activity of the ethanolic extract and its various fractions appear to be related to the inhibition of NO release, and the decreasing TNF-α level. The ethanolic extract and all its fractions especially the ethyl acetate (p0.01) showed significant analgesic activity with insignificant ulceration as compared to the standard drug, i.e. ibuprofen. The histopathological study of ethanolic extract and its fractions reveals that none of them cause ulcer.The present study indicates that Adiantum capillus veneris Linn. has significant anti-inflammatory and analgesic effect.

A series of novel 2-[4-aryl-5-{(quinolin-8-yloxy)methyl}-4H-1,2,4-triazol-3-ylthio]-1-arylethanones (6a-6j) and 8-{(5-aryl-1,3,4-oxadiazol-2-yl)methoxy}quinolines (7a-7d) were synthesized from the corresponding 4-arnyl-1-(2- quinolin-8-yloxy)acetyl) thiosemicarbazides (4a-4d) and hydrazides (3) respectively. The prepared compounds were screened for their anti-inflammatory, analgesic, ulcerogenic and antimicrobial activities. The anti-inflammatory activities were determined by carrageenan induced rat paw edema method. Compounds 6c, 6d, 6f 6j, 7b and 7e significantly inhibited the rat paw edema depending upon the dose employed. These compounds exhibited insignificant ulceration compared to the standard drug Indomethacin. The compounds were also evaluated for their in vitro antimicrobial activity. Some compounds have shown moderate to good activity whereas compound 7b has shown significant zone of inhibition compared to the standard drug Ampicillin against gram negative microorganisms.