• This compound belongs to the class of organic compounds known as naphthyridine carboxylic acids and derivatives. (drugbank.com)
  • These are compounds containing a naphthyridine moiety, where one of the ring atoms bears a carboxylic acid group. (drugbank.com)
  • Naphthyridine is a class of aromatic heterocyclic compounds whose chemical formula is C8H6N2. (chemenu.com)
  • Novel pyrrolo[1',5'-a]-1,8-naphthyridine compounds (L1-L4) have been synthesized through a facile one-pot process by the reaction of the corresponding 1,8-naphthyridines with aliphatic anhydride. (ias.ac.in)
  • Since most of the pyrazole derivatives show anti-microbial activity, the synthesized compounds are also expected to show antimicrobial activity. (biomedcentral.com)
  • 1 H NMR spectroscopy revealed that in our preparation of pyrazolyl triazole derivative 3 , a mixture of two compounds was obtained (Figure 5). (wuxibiology.com)
  • It is a derivative of the class of compounds k. (benchchem.com)
  • The present invention covers a method for preparing 2-[(3R)-3-methylmorpholin-4-yl]-4-(1-methyl-1H-pyrazol-5-yl)-8-(1H-pyrazol-5-yl)-1,7-naphthyridine ("the compound of formula (I)" in the following) as well as intermediate compounds useful in the preparation of the compound of formula (I). The invention also addresses the polymorphic form B of the substance of formula (I) that has a high quality. (lifechempharma.com)
  • The cycloaddition of nitrile oxides, nitrones, and nitrile imines to 3-arylidenechromanone ( 1 ), -flavonone ( 5 ), -1-thiochromanone ( 2 ) and -1-tetralone ( 3 ) proceeds regio- and stereoselectively under the formation of spiro-substituted isoxazole and pyrazole derivatives. (heterocycles.jp)
  • Hence, our plan is to synthesize some substituted pyrazole derivatives and subsequently screen for their antimicrobial activity. (biomedcentral.com)
  • In a technical sense, it is a naphthyridone, not a quinolone: its ring structure is a 1,8-naphthyridine nucleus that contains two nitrogen atoms, unlike quinoline, which has a single nitrogen atom. (wikipedia.org)
  • Trovafloxacin mesylate differs from other quinolone derivatives by having a 1,8-naphthyridine nucleus. (nih.gov)
  • Many derivatives containing pyrazole nucleus have been commercialized as herbicides, insecticides and fungicides for plant protection [ 3 ]. (biomedcentral.com)
  • 1,8]-Naphthyridine derivatives (1a-1l) were evaluated for inhibitory potential for isozymes of carbonic anhydrase (CA) and alkaline phosphatase (ALP). (bvsalud.org)
  • Shown on Figure 1 are 2D structure of two drug molecules, in which naphthyridine amide 1 has excellent inhibitory activity, while quinoline amide 2 exhibits much lower biological activity. (wuxibiology.com)
  • 2010. Novel huprine derivatives with inhibitory activity toward beta-amyloid aggregation and formation as disease-modifying anti-Alzheimer drug candidates . (ub.edu)
  • The design, synthesis, and ability to inhibit p38α MAP kinase by a novel series of naphthyridine N-oxides will be described. (rcsb.org)
  • The synthesis of 5-formyl-6-aryl-6H-indolo[3,2,1-de][1,5] naphthyridine-2-carboxylates by way of response between 1-formyl-9H-b-carbolines and cinnamaldehydes within the presence of pyrrolidine in water beneath microwave irradiation is described. (topigen.com)
  • Pyrazol-5-one derivative 2 was exploited as a key intermediate for the synthesis of hitherto unknown fused pyrazole. (biomedcentral.com)
  • 2014. 1,2,3,4-Tetrahydrobenzo[h][1,6]naphthyridines as a new family of potent peripheral-to-midgorge-site inhibitors of acetylcholinesterase: Synthesis, pharmacological evaluation and mechanistic studies . (ub.edu)
  • 2014. Synthesis and multitarget biological profiling of a novel family of rhein derivatives as disease-modifying anti-Alzheimer agents . (ub.edu)
  • The invention provides novel coumarin derivatives as specific mitochondrial RNA polymerase inhibitors for the treatment of cancer. (justia.com)
  • The invention provides novel 4-phenyl-coumarin derivatives, processes for their preparation and uses thereof as specific mitochondrial RNA polymerase inhibitors for the treatment of cancer. (justia.com)
  • Furthermore, the present invention relates to the use of said disubstituted pyridine derivatives as inhibitors for a protein kinase. (justia.com)
  • Thus, synthesized derivatives proved to be 100 to 800 times more potent as compared to standard inhibitors of b-TNAP and c-IAP (Levamisole and L-phenyl alanine, respectively). (bvsalud.org)
  • In addition, selectivity and dual inhibition of [1,8]-Naphthyridine derivatives confer precedence over known inhibitors. (bvsalud.org)
  • In this conformation, the amide group is coplanar with the naphthyridine ring and its N10-H is hydrogen bonding with the N6 of the naphthyridine. (wuxibiology.com)
  • Quinoline amide 2 , with the N6 atom on the naphthyridine ring replaced with a C atom, loses the intramolecular hydrogen bonding, as shown in Figure 4, conformation 2B . (wuxibiology.com)
  • Since naphthyridine 1 is more biologically active, we can speculate that its coplanar structure is likely to be the dominant conformation for target binding, and that the orientation of the carbonyl group and/or the amino group in the amide might also be biased for specific hydrogen bonding with the target. (wuxibiology.com)
  • Chemically, trovafloxacin mesylate, a fluoronaphthyridone related to the fluoroquinolone antibacterials, is (1α, 5α, 6α)-7-(6-amino-3-azabicyclo[3.1.0]hex-3-yl)-1-(2,4-difluorophenyl)-6-fluoro-1,4-dihydro-4-oxo-1,8-naphthyridine-3-carboxylic acid, monomethanesulfonate. (nih.gov)
  • Objective: In the efforts to develop suitable antimicrobia drugs, medicinal chemists have focused on thiazole derivatives. (dntb.gov.ua)
  • Thus cyclocondensation of 2 with active methylene reagent such as malononitrile in ethanol under reflux in the presence catalytic amount of piperidine afforded indazole derivative 3 on the basis of analytical and spectral data (Scheme 1 ). (biomedcentral.com)
  • 1. Indazole and indolizine-3-carboxylic acid derivatives. (chemchart.com)
  • To adopt the ground state conformation as naphthyridine 1A , the quinoline conformation 2B will be 2 kcal/mol higher than its ground state 2A . (wuxibiology.com)
  • 1,8]-Naphthyridine derivatives have been reported to possess important biological activities and may serve as attractive pharmacophores in the drug discovery process. (bvsalud.org)
  • Derivatives of ethylene, a simple organic gas of biological origin with many industrial and biological use. (lookformedical.com)
  • 1,8]-Naphthyridine derivatives (1a-1l) were approximately 4 folds more potent than standard CA inhibitor acetazolamide. (bvsalud.org)
  • Further, X-ray crystal analysis of 7-diacetamino-2,4-dimethy-1,8-naphthyridine (L1) identifies its molecular structure and reveals π-π stacking. (ias.ac.in)
  • The reactivity of methyl group in pyrazolone 2 toward aryl diazonium salts was also investigated aiming at preparation of new pyridazine derivatives. (biomedcentral.com)
  • Title: 7-(4H-1,2,4-Triazol-3-yl)benzo[c][2,6]naphthyridines: a novel class of Pim kinase inhibitors with potent cell antiproliferative activity. (aablocks.com)
  • Title: Discovery and SAR of 5-(3-chlorophenylamino)benzo[c][2,6]naphthyridine-8-carboxylic acid (CX-4945), the first clinical stage inhibitor of protein kinase CK2 for the treatment of cancer. (aablocks.com)
  • Nitrogen-containing heterocyclic compounds such as 1,4-thiazine and its benzo derivatives are important compounds in many different research fields due to their remarkable biological properties. (chemenu.com)
  • In international patent applications WO98/42707, W098/54188, WO00/17200 and WO00/26217, as well as in international patent applications WO00/63211, WO01/72756, WO01/72754, WO01/72755 and WO01/72757, tricyclic imidazopyridine derivatives having a very specific substitution pattern are disclosed, which should likewise be suitable for the treatment of gastric and intestinal diseases. (allindianpatents.com)
  • 16. 1,8-Naphthyridine-3-carboxamide derivatives with anticancer and anti-inflammatory activity. (nih.gov)
  • Naphthyridine is a class of aromatic heterocyclic compounds whose chemical formula is C8H6N2. (chemenu.com)
  • Chemically, trovafloxacin mesylate, a fluoronaphthyridone related to the fluoroquinolone antibacterials, is (1α, 5α, 6α)-7-(6-amino-3-azabicyclo[3.1.0]hex-3-yl)-1-(2,4-difluorophenyl)-6-fluoro-1,4-dihydro-4-oxo-1,8-naphthyridine-3-carboxylic acid, monomethanesulfonate. (nih.gov)
  • 2006. 4-Amino derivatives of the Hsp90 inhibitor CCT018159 . (ub.edu)
  • There are ten isomers of naphthyridine, because naphthyridine has two benzene rings, has strong π-π conjugation, and has better luminescence properties. (chemenu.com)
  • Jan 10, 2008 a series of carbazole derivatives with promising pharmacological properties has been prepared using either an ironmediated or a palladiumcatalyzed synthetic approach. (web.app)
  • 18. Biological activity of bis-benzimidazole derivatives on DNA topoisomerase I and HeLa, MCF7 and A431 cells. (nih.gov)
  • Pharmacophoric modification of the formyl group provided a number of new fused-b-carboline derivatives which have been investigated for his or her k-opioid receptor (KOR) agonistic exercise. (topigen.com)
  • HN - 2019 MH - Afatinib UI - D000077716 MN - D2.65.132 MN - D3.633.100.786.188 MS - A quinazoline and butenamide derivative that acts as a tyrosine kinase inhibitor of epidermal growth factor receptors (ERBB RECEPTORS) and is used in the treatment of metastatic NON-SMALL CELL LUNG CANCER. (nih.gov)
  • 1,8-Naphthyridine Derivatives: A Privileged Scaffold for Versatile Biological Activities. (nih.gov)