다중혈관 관상동맥 환자에서 y-문합을 이용하여 양쪽 내흉동맥만을 사용한 우회술의 조기 성적

[신간의 별자리x] 우리/미술, 그리고 ‘슬픔의 박물관’

Assay for lipid peroxides in animal tissues by thiobarbituric acid reaction

A review on anticancer potential of bioactive heterocycle quinoline.

Quinoline (1-azanaphthalene) is a heterocyclic aromatic nitrogen compound characterized by a double-ring structure that contains a benzene ring fused to pyridine at two adjacent carbon atoms. Quinoline compounds are widely used as "parental" compounds to synthesize molecules with medical benefits, especially with anti-malarial and anti-microbial activities. Certain quinoline-based compounds also show effective anticancer activity. This broad spectrum of biological and biochemical activities has been further facilitated by the synthetic versatility of quinoline, which allows the generation of a large number of structurally diverse derivatives. This includes numerous analogues derived from substitution of the quinoline ring system, and derivatization of quinoline ring structure. Quinoline and its analogs have recently been examined for their modes of function in the inhibition of tyrosine kinases, proteasome, tubulin polymerization and DNA repair. In this review, we have summarized our knowledge on quinoline compounds with respect to their anticancer activities, mechanisms of action, structure-activity relationship (SAR), and selective and specific activity against various cancer drug targets. In particular, we focus our review on in vitro and in vivo anticancer activities of quinoline and its analogs in the context of cancer drug development and refinement.

Quinoline as a Privileged Scaffold in Cancer Drug Discovery

Quinoline derivatives have been reported to possess antimicrobial 1 and anti-inflammatory 2 activities besides wide range of pharmacological activities. Moreover fusion of tetrazole, which is considered as planar acidic heterocyclic analogue of carboxylic function 3,4 , have ability to increase potency 5,6 and improve bioavailability 7 . Similarly Schiff’s bases have been reported to possess antimicrobial 8,9 apart from other biological activities. These observations led to the conception that Schiff’s bases of tetrazolo[1,5a]quinoline possess potential antimicrobial and antiinflammatory activities. In the present study a new series of Schiff’s bases of tetrazolo[1,5-a]quinoline has been synthesized successfully. The reaction sequence for the title compound is outlined in Scheme I. Vilsmeier-Haack formylation 10

Synthesis of Schiff′s Bases of 8‐Methyltetrazolo[1,5‐a]quinoline as Potential Antiinflammatory and Antimicrobial Agents.

Synthesis, antidepressant and antifungal evaluation of novel 2-chloro-8-methylquinoline amine derivatives.

Purpose : A series of 2-chloro-6-methylquinoline hydrazones (3a-o) were synthesized by the condensation of substituted acyl hydrazines, semicarbazide, thiosemicarbazide, and INH with 2-chloro-3-formyl-6-methylquinoline in absolute alcohol and were tested for antimicrobial activity. Materials and Methods : The structures of compounds were established using modern analytical technique FT-IR, 1 H and 13 C-NMR, mass spectral data and elemental analysis. All the compounds were evaluated for their antibacterial activity against Escherichia coli (NCTC 10418), Staphylococcus aureus (NCTC 65710), and Pseudomonas aeruginosa (NCTC 10662). The compounds were also tested for antifungal activity aganist Aspergillus niger (MTCC 281), Aspergillus flavus (MTCC 277), Monascus purpureus (MTCC 369) and Penicillium citrinum (NCIM 768) by the cup-plate method. Results : It was observed that maximum antibacterial activity was shown by compounds having the 4-fluoro, 4-chloro, 4-nitro, and 2, 4-dicloro group in the benzoyl ring. Compounds were weakly active against fungal strains. Conclusion : Quinolinyl hydrazone of INH 3o was found to be most active toward the bacterial strains compared to their corresponding benzoyl derivatives.

Synthesis and antimicrobial activity of 2-chloro-6-methylquinoline hydrazone derivatives

Hit to lead optimization of a series of N-[4-(1,3-benzothiazol-2-yl)phenyl]acetamides as monoacylglycerol lipase inhibitors with potential anticancer activity

Epilepsy is a neurological condition which is characterized by unprovoked seizures resulting from abnormal discharge of cerebral neurons and affecting at least 50 million people worldwide. There is continuing demand for new anticonvulsant agents as it has not been possible to control every kind of seizure with existing antiepileptic drugs. Moreover, conventional antiepileptic drugs exhibited unfavorable side effect profile and failure to adequately control seizures (1n3). Searching for compounds with potential anticonvulsant activity we focused our attention on various hydrazones and semicarbazones which have been found to display significant anticonvulsant activity (4n6). These compounds were believed to interact at two locations on a putative binding site designated as hydrogen binding domain and hydrophobic binding area as proposed by Dimmock et al. (Figure 1). In their study it is also reported that replacement of aryl group with other hydrophobic SYNTHESIS AND IN VIVO ANTICONVULSANT EVALUATION OF 2-CHLOROQUINOLINYL HYDRAZONE DERIVATIVES

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Suresh Kumar

Papers

Synthesis of Schiff′s Bases of 8‐Methyltetrazolo[1,5‐a]quinoline as Potential Antiinflammatory and Antimicrobial Agents.

Synthesis, antidepressant and antifungal evaluation of novel 2-chloro-8-methylquinoline amine derivatives.

Synthesis and antimicrobial activity of 2-chloro-6-methylquinoline hydrazone derivatives

Hit to lead optimization of a series of N-[4-(1,3-benzothiazol-2-yl)phenyl]acetamides as monoacylglycerol lipase inhibitors with potential anticancer activity

Synthesis and in vivo anticonvulsant evaluation of 2-chloroquinolinyl hydrazone derivatives.