- Quinoline and 2-nitroimino-1, 3-diazacycloalkane hybrids: Design, synthesis and insecticidal activity
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A library of new hybrid molecules comprising quinoline, 2-nitroimino-1, 3-diazacycloalkane motifs were designed and synthesized as plausible neonicotinoid analogues. These compounds were synthesized from 2-chloro/aryloxy-3-formyl quinolines and guanidine nitrate with the coupling of 2-chloro/aryloxy-3-(chloromethyl)quinolines, 2-nitroimino-1, 3-diazacycloalkanes under phase transfer catalysis (PTC) as crucial step. All the compounds were obtained in excellent yields (80–90%) and were characterized by 1H, 13C NMR and mass spectrometry. The newly generated compounds were screened for insecticidal activity against aphids in safflower field and some of them displayed moderate activity.
- Sowmya, Jonnalagadda,Padma, Banda,Leelavathi, Panaganti
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- RETRACTED ARTICLE: Synthesis, Molecular Properties, and Biological Evaluation of Hybrid 1,2,3-Triazolylpolyaza Heterocyclic Compounds
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In this research article, a highly efficient, cost-effective synthesis of various hybrid molecules possessing 1,2,3-triazolyltetrazoles and evaluation of their biological activity have been addressed. The structure elucidation of these new library hybrid molecules has been carried out by IR, 1H NMR, 13C NMR, and mass spectral analysis. The compounds have been screened for their anticancer activity against human colon cancer cell line Colo-205 and human lung cancer cell line HOP-205, and the results attest that most of the compounds have shown very good therapeutic nature. In particular, compounds 3d, 3j, 6a, and 6e were more cytotoxic than Adriamycin against all tested human cancer cell lines with 68percent, 101.8percent, 94percent, and 104.5percent growth, respectively. In the present investigation, a series of 3a–j and 6a–h were subjected to molecular properties prediction, drug likeness by Molinspiration, and toxicity risks by Molsoft software programs. All the 18 analogues were chosen on the basis of Lipinski “Rule of five” for the synthesis, screening their antibacterial and anticancer as oral bioavailable drugs/leads.
- Dasari, Srinivasa Rao,Tondepu, Subbaiah,Vadali, Lakshmana Rao,Ganivada, Mutyala Naidu,Seelam, Nareshvarma
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p. 195 - 208
(2019/01/04)
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- Design of new hybrid template by linking quinoline, triazole and dihydroquinoline pharmacophoric groups: A greener approach to novel polyazaheterocycles as cytotoxic agents
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A new hybrid template designed by linking three pharmacophoric groups, for example, quinoline, triazole and dihydroquinoline moieties have been used for the generation of a library of molecules as potential cytotoxic agents. Synthesis of these polyazaheterocycles were carried out by using a strategy that involved one-pot sequential azidation and CuAAC in water under mild conditions. A number of 1,4-disubstituted 1,2,3-triazoles possessing quinolinylmethylene at N-1 and 1,2-dihydroquinolinyl methylene at C-4 as different substituents were synthesized and evaluated for their cytotoxic effects against various cancer cells. Some of them showed encouraging activities against lung cancer cells and one of them showed inhibition of PDE4 indicating the potential medicinal value of these novel polyazaheterocycles.
- Praveena, Koduru Sri Shanthi,Shivaji Ramarao, Edupuganti Veera Venkat,Murthy, Nandula Yadagiri Sreenivasa,Akkenapally, Surekha,Ganesh Kumar,Kapavarapu, Ravikumar,Pal, Sarbani
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p. 1063 - 1069
(2015/02/19)
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- New heteroaryl-spaced phosphono α-amino acids are competitive NMDA antagonists with analgesic activity
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The synthesis and the NMDA receptor binding affinities of α-amino-3-(phosphonomethyl)-2-naphthalenepropanoic acid, α-amino-3-(phosphonomethyl)-2-benzofuranpropanoic acid, a series of substituted (R)-α-amino-3-(phosphonomethyl)-2-quinolinepropanoic acids, (R)-α-amino-3-(phosphonomethyl)-1,8-naphthyridine-2-propanoic acid and (R)-α-amino-3-(phosphonomethyl)-1,6-naphthyridine-2-propanoic acid are reported.
- Swahn, Britt-Marie,Claesson, Alf,Pelcman, Benjamin,Besidski, Yevgeni,Molin, Hakan,Sandberg, Mats P.,Berge, Odd-Geir
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p. 1635 - 1640
(2007/10/03)
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