Ethyl 2-(4-benzoyl-2,5-dimethyl­phen­oxy)acetate

The title compound, C19H20O4, was synthesized via a Fries rearrangement of hydr­oxy benzophenone. The dihedral angle between the least-squares planes of the two benzene rings is 69.04 (11)°. The mol­ecular structure displays an intra­molecular non-classical C—H⋯O hydrogen bond

THERAPEUTIC POTENTIAL AND IN VITRO ANTHELMINTIC ACTIVITY OF RIDGE GOURD FRUIT

Objective: The objective of the study was to evaluate the therapeutic potential and in vitro anthelmintic activity of ridge gourd fruit (Luffa acutangula) against Indian earthworms. Methods: For anthelmintic activity against Indian earthworms (Pheretima posthuma, Ascaridia galli, and Raillietina spiralis), various different extracts concentration of L. acutangula fruit have been taken. Five concentrations as 10, 20, 30, 40, and 50 mg/ml of various extracts were tested and results were expressed in terms of time for paralysis and time for the death of worms. Albendazole (20 mg/ml) was used as reference standard and water (0.5%) as a control group. Results: Preliminary phytochemical screening of the different extracts of ridge gourd fruit was shown to produce anthelmintic activities. In the present study, it was observed that all the extracts of ridge gourd fruit have exhibited a positive response to a certain degree of anthelmintic activity. Ethyl acetate extract exhibited more potent activity at the lower concentration of 10 mg/mL against A. galli (Roundworm). The anthelmintic activity of L. acutangula fruit extract has, therefore, been demonstrated

Efficacy of 5-(2-aroyl)aryloxy methyl-2-phenyl-1,3,4-oxadiazoles as antibacterial and antifungal agents

Research and development of potent and effective antimicrobial agents represent one of the most important advances in therapeutics; the main aim of these efforts is not only control the serious infections, but also prevention and treatment of some infectious complications of other therapeutic modalities. A series of 5-(2-aroyl)aryloxy methyl-2-phenyl-1,3,4-oxadiazoles were screened for their antibacterial and antifungal activities. Anti-bacterial activity against B. cereus, S. aureus, B. subtilis, S. aureus (MRSA), E. aerogenes, M. luteus, K. pneumonia, P. aeruginosa, S. typhimurium, E. coli, paratyphi-B, P. vulgaris bacterial strains and anti-fungal activity against C. albicans, A.niger, F.solani, A.flavus, B.cinerea, C.krusei, M. pachydermatis, C.parapsilosis, F.moniliforme, C.gloeosporioides fungal strains were carried out. The bioassays indicated that most of the synthesized compounds showed potential antibacterial and anti-fungal activity

2-Methylxanthen-9-one

In the title compound, C14H10O2, the tricycle is not planar, being bent with a dihedral angle of 4.7 (1)° between the two benzene rings. In the crystal, π–π inter­actions between the six-membered rings of neighbouring mol­ecules [centroid–centroid distances = 3.580 (3) and 3.605 (3) Å] form stacks propagating along [101]

Competent synthesis of biaryl analogs via asymmetric Suzuki–Miyaura cross-coupling for the development of anti-inflammatory and analgesic agents

Based on the core structure of diflunisal drug, herein, we report a resembling series of biaryl analogs (3a–j) containing halogens, nitro, and methoxy substituents. They were designed and synthesized via a Suzuki–Miyaura cross-coupling reaction using Pd (OH)2 as a catalyst at a temperature of 65 °C with an intent to obtain improved and safer anti-inflammatory and analgesic agents. Suzuki–Miyaura transformation is the most significant among the cross-coupling reactions since its practical advantages include the commercially available low toxic reagents, mild reaction conditions, and functional group compatibility. On the other hand, a few conditions can be used to cross-couple aryl boronic acids or esters with aryl halides, especially 2-benzyl halides. Because of this, a novel Suzuki–Miyaura protocol is investigated that facilitates the selective conversion of halo aromatics, with an emphasis on the reaction to convert substituted bromobenzene to conjugated biphenyls. Finally, the obtained biaryl analogs (3a–j) were tested for in vitro and in vivo anti-inflammatory and analgesic applications. The results showed that compound 3b performed better than the standard drug with IC50 values comparable to that of the standard drug for COX-1 and COX-2 inhibition. Finally, molecular docking tests for the effective compound were carried out

Synthesis, characterization and biological applications of mononuclear azamacrocyclic metal complexes

A novel series of mononuclear azamacrocyclic metal complexes using the cobalt (II) chlorides were synthesized by the reaction of 2, 6 dibenzoyl-4-chloro phenols with ethylene diamine by adopting template method. The complexes have been characterized on the basis of micro analytical, IR, and magnetic measurement studies. Spectral studies suggested octahedral geometry around the cobalt .The antimicrobial activity of the complexes has been screened in vitro against bacteria and fungi to access their inhibiting potential. Metal complexes exhibited enhanced antimicrobial activity in comparison to their fragments. In vitro antioxidant activities of these compounds were evaluated and compared with commercial antioxidant ascorbic acid. The results showed good antioxidant activities of these compounds

Synthesis and anti-inflammatory activity of 2-aryloxy methyl oxazolines

A series of potential biologically active 2-aryloxy methyl oxazolines 3a–n have been synthesized from substituted hydroxybenzenes 1a–n with good chemical yield. The compounds 3a–n were screened for their anti-inflammatory, ulcerogenic, cyclooxygenase activities and also for their acute toxicity. The potency of the compounds was compared with that of the standard drugs, aspirin and phenyl butazone. The outcome indicates that compounds 3b (48.2), 3h (48.5) and 3l (46.5) offered significant anti-inflammatory activity with low ulcerogenic activity than the standard drugs

Synthesis of 2-(2-aroylaryloxy)methyl-oxazolines as potent analgesic and anti-inflammatory agents

The synthetic strategies and characterization of some novel benzophenone derivatives carrying oxazoline ring are described using microwave irradiation technique. The compounds 2a-h, 3a-h and 4a-h were screened for their analgesic, anti-inflammatory, ulcerogenic, cyclooxygenase activities and acute toxicity. The results revealed that halo compounds 4a (48.3%), 4c (45.4%) and 4f (40.2%) displayed significant anti-inflammatory activity with low ulcerogenic activity in comparison with that of the standard drugs, aspirin (35.3%) and phenyl butazone (35.5%

Benzophenone-N-ethyl piperidine ether analogues-synthesis and efficacy as anti-inflammatory agent

A sequence of substituted benzophenone-N-ethyl piperidine ether analogues has been synthesized and evaluated as orally active anti-inflammatory agents with reduced side effects. The anti-inflammatory and ulcerogenic activities of the compounds were compared with naproxen, indomethacin, and phenylbutazone. These analogues showed an interesting anti-inflammatory activity in carrageenan-induced foot pad edema assay. In the air-pouch test, some of the analogues reduced the total number of leukocytes of the exudate, which indicates inhibition of prostaglandin production. Side effects of the compounds were examined on gastric mucosa, in the liver and stomach. None of the compounds illustrated significant side effects compared with standard drugs like indomethacin and naproxen. (C) 2009 Elsevier Ltd. All rights reserved

Synthesis and antimicrobial activity of 5-[(4-aroyl) aryloxymethyl]-2-(4- methylphenylamino)-1 ,3,4-thiadiazoles and 5-[(4-aroyl) aryloxy methyl]-4- (4-methylphenyl)-3-mercapto-4<i>H</i>-1,2,4-triazoles

2652-2656Aroyl aryloxyaeetic thiosemicarbazides 4a-d have been synthesized by the reaction of acid hydrazides 3a-d with p-tolyl isothiocyanate. The aroyl aryloxyacetic thiosemicarbazides 4a-d on intramolecular cyclization using cone. H2SO4 and 2N NaOH give 1,3,4-thiadiazoles 5a-d and 3-mercapto-4H-1,2,4-triazoles 6a-d, respectively. The structures of the synthesised compounds have been determined by their elemental analysis and spectral data. The synthesized compounds are evaluated for their antibacterial activity