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Journal articles on the topic 'Novel heterocyclic compounds'

Author: Grafiati

Published: 4 June 2021

Last updated: 6 February 2022

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1

Shah, Pranay, R. I. Patel, and P. J. Vyas. "Preparation and Biological Screening of Novel Heterocyclic Compounds." International Journal of Trend in Scientific Research and Development Volume-3, Issue-3 (April 30, 2019): 632–36. http://dx.doi.org/10.31142/ijtsrd22815.

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2

Olšovská, Jana, Karel Štěrba, Martin Slabý, and Tomáš Vrzal. "Novel method for determination of heterocyclic compounds and their impact in brewing technology." KVASNY PRUMYSL 67, no. 2 (April 15, 2021): 417–27. http://dx.doi.org/10.18832/kp2021.67.417.

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A new simultaneous method for determination of 16 heterocyclic compounds using SPE sample preparation and GC-MS determination was developed regarding increasing interest of the role of sensory active compounds in beer. LiChrolut® EN SPE columns proved to be optimal for both, a mixture of analytes with a different polarity and such complicated matrix as beer. Recoveries of individual analytes are about 100% except for three compounds (2-methylpyridine about 30%, maltol and furaneol about 50%); repeatability, uncertainty and LOQ are satisfactory for the method application. The method was used for monitoring of heterocyclic compounds formation during roasting, mashing, hop boiling and fermentation. To summarize, during roasting of malt, the concentration of oxygen heterocycle compounds (OHC) increases more rapidly in comparison with nitrogen heterocycles compounds (NHC) till a critical point where OHC starts to decrease and NHC starts to be formed sharper (with the exception of 2-acetylpyrrole which is similar to OHC). Finally, the total concentration of NHC during fermentation rapidly decreases whilst the OHC concentration is influenced by many factors, e.g., fermentation conditions and yeast strain.

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3

Ābele, E., R. Ābele, Ļ. Golomba, J. Višņevska, T. Beresņeva, and K. Rubina. "Oximes of Seven-Membered Heterocyclic Compounds Containing One Heteroatom." Latvian Journal of Chemistry 50, no. 3-4 (January 1, 2011): 205–22. http://dx.doi.org/10.2478/v10161-011-0071-7.

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Oximes of Seven-Membered Heterocyclic Compounds Containing One Heteroatom Literature data on the synthesis and structure of azepane, oxepane and thiepane oximes were reviewed. Synthesis of novel heterocycles from oximes of seven-membered heterocycles containing one heteroatom were described. Biological activity of oximes of seven-membered heterocycles with one heteroatom was also reviewed.

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4

Ābele, E. "Oximes of Seven-Membered Heterocyclic Compounds Containing Two Heteroatoms." Latvian Journal of Chemistry 51, no. 1-2 (January 1, 2012): 83–92. http://dx.doi.org/10.2478/v10161-012-0005-z.

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Oximes of Seven-Membered Heterocyclic Compounds Containing Two Heteroatoms Literature data concerning the synthesis and structure of diazepane, oxazepane and thiazepane oximes were reviewed. Synthesis of novel heterocycles from the oximes of seven-membered heterocycles containing two heteroatoms was described. Biological activity of oximes of seven-membered heterocycles with two heteroatoms was also reviewed.

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5

Shaikh, Ansar R., Mazahar Farooqui, R. H. Satpute, and Syed Abed. "Overview on Nitrogen containing compounds and their assessment based on ‘International Regulatory Standards’." Journal of Drug Delivery and Therapeutics 8, no. 6-s (December 21, 2018): 424–28. http://dx.doi.org/10.22270/jddt.v8i6-s.2156.

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Heterocyclic compounds have a role in most fields of sciences such as medicinal chemistry, biochemistry also another area of sciences. More than 90% of new drugscontain heterocycles and the interface between chemistry and biology, at which so much new scientific insight, discovery and application is taking place is crossed by heterocyclic compounds. Compounds derived from heterocyclic rings in pharmacy, medicine, agriculture, plastic, polymer and other fields.Most active heterocycles that have shown considerable biological actions as antifungal, anti-inflammatory, antibacterial, anticonvulsant, antiallergic, herbicidal, anticancer activity. There is always a strong need for new and efficient processes in synthesizing of new Heterocycles.Alum have been used as a novel catalyst in the synthesis of Schiff’s bases. Synthesized Schiff’s bases are free from use of ICH class 1 and Class 2 solvents and also free from structural alerts genotoxic impurities. This review highlights on various aspects of heterocyclic compounds with its biological activity & regulatory assessment based on the ‘International Regulatory Standards’. Keywords: Heterocycles. Nitrogen containing compounds Biological activity, History, Regulatory assessment, International Regulatory Standards

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6

Mohareb, Rafat, and Hanaa Hana. "Synthesis of progesterone heterocyclic derivatives of potential antimicrobial activity." Acta Pharmaceutica 58, no. 1 (March 1, 2008): 29–42. http://dx.doi.org/10.2478/v10007-007-0043-3.

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Synthesis of progesterone heterocyclic derivatives of potential antimicrobial activityThe aim of this work was to synthesize steroidal heterocycles and to elucidate the potential role of these compounds as antimicrobial agents. The synthesis of steroidal heterocycles containing the pyrazole, isoxazole, thiazole, pyrane, pyridine, pyridazine, or benzopyrane ring attached to the pregnene nucleus is reported. Progesterone (1) reacts with dimethyl formamide dimethyl acetal to form enamine2. Heterocyclization of2with hydrazines, hydroxylamine, glycine, ethyl acetoacetate or cyanomethylene afforded novel steroidal heterocyclic derivatives. Thein vitroantimicrobial evaluation showed that all synthesized compounds show activity against the used strains of Gram positive bacteria and fungi.

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7

Orzeszko, Barbara, Tomasz Świtaj, Anna B. Jakubowska-Mućka, Witold Lasek, Andrzej Orzeszko, and Zygmunt Kazimierczuk. "Tumor Necrosis Factor-α Production-Enhancing Properties of Novel Adamantylalkylthio Derivatives of Some Heterocyclic Compounds." Zeitschrift für Naturforschung B 60, no. 4 (April 1, 2005): 471–75. http://dx.doi.org/10.1515/znb-2005-0419.

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Certain adamantylated heterocycles were previously shown to enhance the secretion of tumor necrosis factor alpha (TNF-α) by murine melanoma cells that have been transduced with the gene for human TNF-α and constitutively expressed this cytokine. The stimulatory potency of those compounds depended, among other factors, on the structure of the linker between the adamantyl residue and the heterocyclic core. In the present study, a series of (1-adamantyl)alkylsulfanyl derivatives of heterocyclic compounds was prepared by alkylation of the corresponding thioheterocyles. Of the novel adamantylalkylthio compounds tested in the aforementioned cell line, 2-(2-adamantan-1-ylethylsulfanyl)- 4-methyl-pyrimidine was found to be the most active

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8

Sharma, Praveen Kumar, Andleeb Amin, and M. Kumar. "Synthetic Methods of Medicinally Important Heterocycles-thiazines: A Review." Open Medicinal Chemistry Journal 14, no. 1 (September 14, 2020): 71–82. http://dx.doi.org/10.2174/1874104502014010071.

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Heterocyclic compounds containing N and S atoms have unique properties so that they can be used as potential reactive materials in pharmacokinetic systems. In medicinal chemistry, the therapeutic applications of nitrogen sulphur heterocycles are well known. Especially, Thiazines attract the attention of chemists due to their great bioactive behavior. The present study is a review of the work carried out by the research community for the synthesis of novel, effective, medicinally important heterocyclic compounds-thiazines.

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9

Doller, Dario, Guiying Li, Robbin M. Brodbeck, and Christian Thomsen. "Novel heterocyclic compounds as mGlu5 antagonists: WO2009015897." Expert Opinion on Therapeutic Patents 20, no. 3 (February 24, 2010): 435–39. http://dx.doi.org/10.1517/13543770903547848.

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10

Wu, Hsien-Jen, Fang-Jung Huang, and Chu-Chung Lin. "Novel heterocyclic cage compounds from 2-methylthiofurans." Journal of the Chemical Society, Chemical Communications, no. 11 (1991): 770. http://dx.doi.org/10.1039/c39910000770.

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11

Górska, Agata, Lidia Chomicz, Justyna Żebrowska, Przemysław Myjak, Ewa Augustynowicz-Kopeć, Zofia Zwolska, Janusz Piekarczyk, Henryk Rebandel, and Zygmunt Kazimierczuk. "Synthesis and Antimycobacterial and Antiprotozoal Activities of Some Novel Nitrobenzylated Heterocycles." Zeitschrift für Naturforschung B 61, no. 1 (January 1, 2006): 101–7. http://dx.doi.org/10.1515/znb-2006-0120.

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A series of N-, S-, and O-mononitro- and dinitrobenzyl derivatives of heterocycles was synthesized by alkylation of heterocyclic bases with the respective nitrobenzyl chlorides. Of the newly synthesized compounds, dinitrobenzylsulfanyl derivatives of 1-methyl-2-mercaptoimidazole (2c) and of 5-nitro- and 5,6-dichloro-2-mercaptobenzimidazole (8b and 8c, and 8e and 8f, respectively) showed considerable antimycobacterial activity. On a molar basis, nine of the novel compounds showed also a considerably higher antiprotozoal efficacy than metronidazole that reduced T. hominis viability to 73.5% at 8 μg/ml.

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12

Lather, Amit, Sunil Sharma, Sarita Khatkar, and Anurag Khatkar. "Docking Related Survey on Heterocyclic Compounds Based on Glucosamine-6- Phosphate Synthase Inhibitors and their Antimicrobial Potential." Current Pharmaceutical Design 26, no. 15 (May 18, 2020): 1650–65. http://dx.doi.org/10.2174/1381612826666200217115211.

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: The synthetic heterocyclic compounds have their importance due to their wide applications in various fields of science. The heterocyclic compounds have been reported for their anticancer, antitubercular, insecticides, analeptics, analgesic, anti-bacterial, anti-viral, anti-fungal, and weedicidal activity. Researchers have tried various newer targets in search of better antimicrobials acting via novel mechanisms. Glucosamine-6-Phosphate synthase is an enzyme present in microbial cells. The inactivation of G-6-P synthase may serve as a novel approach to find better antimicrobials. The increasing demands development of newer and effective antimicrobial drugs has reported in search of newer techniques for the generation of new drugs. Hence, the molecular docking technique shall be explored to find or investigate the newer target finding the novel compounds which can be an active antimicrobial compound. The present review has focused on the reported heterocyclic compounds which have been evaluated for their antimicrobial potential using G-6-P synthase as a target. The results of in silico methods and in vitro methods have been compared and critically discussed.

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13

Liu, Jia-Chun, Suresh Narva, Kang Zhou, and Wen Zhang. "A Review on the Antitumor Activity of Various Nitrogenous-based Heterocyclic Compounds as NSCLC Inhibitors." Mini-Reviews in Medicinal Chemistry 19, no. 18 (November 29, 2019): 1517–30. http://dx.doi.org/10.2174/1389557519666190312152358.

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At present, cancers have been causing deadly fears to humans and previously unpredictable losses to health. Especially, lung cancer is one of the most common causes of cancer-related mortality accounting for approximately 15% of all cancer cases worldwide. While Non-Small Cell Lung Carcinomas (NSCLCs) makes up to 80% of lung cancer cases. The patient compliance has been weakening because of serious drug resistance and adverse drug effects. Therefore, there is an urgent need for the development of novel structural agents to inhibit NSCLCs. Nitrogen-containing heterocyclic compounds exhibit wide range of biological properties, especially antitumor activity. We reviewed some deadly defects of clinical medicines for the lung cancer therapy and importance of nitrogen based heterocyclic derivatives against NSCLCs. Nitrogen heterocycles exhibit significant antitumor activity against NSCLCs. Nitrogen heterocyclic hybrids could be developed as multi-target-directed NSCLC inhibitors and it is believed that the review is significant for rational designs and new ideas in the development of nitrogen heterocyclic-based drugs.

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14

González-González, Carlos A., Juan Javier Mejía Vega, Ricardo García Monroy, Davir González-Calderón, David Corona-Becerril, Aydeé Fuentes-Benítes, Joaquín Tamariz Mascarúa, and Carlos González-Romero. "A Novel and Chemoselective Process ofN-Alkylation of Aromatic Nitrogen Compounds Using Quaternary Ammonium Salts as Starting Material." Journal of Chemistry 2017 (2017): 1–6. http://dx.doi.org/10.1155/2017/4586463.

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The process ofN-alkylation of several pyrroles, indoles, and derivative heterocycles is herein described, using quaternary ammonium salts as the source of an alkylating agent. These reactions were carried out on several heterocyclic rings with triethylbenzylammonium chloride or tetradecyltrimethylammonium bromide and an NaOH solution at 50%, leading to a chemoselectiveN-alkylated product and an average yield of 73%. This is an alternative process to the traditional benzylation and methylation ofN-heterocycles with direct handling of alkyl halides.

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15

TANAKA, Satoko, and Kazuyoshi SEGUCHI. "Syntheses of Novel Heterocyclic Compounds Utilizing Active Urazoles." Journal of Synthetic Organic Chemistry, Japan 54, no. 3 (1996): 212–19. http://dx.doi.org/10.5059/yukigoseikyokaishi.54.212.

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16

Matsumoto, Kiyoshi, Mitsuo Toda, Yukio Ikemi, Akikazu Kakehi, Shiro Hashimoto, Motoo Shiro, and Shinichi Otani. "Molecular Inclusion Crystals of Novel Heterocyclic Host Compounds." Molecular Crystals and Liquid Crystals Science and Technology. Section A. Molecular Crystals and Liquid Crystals 276, no. 1-2 (February 1996): 173–84. http://dx.doi.org/10.1080/10587259608039375.

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17

Missaoui, B. E., M. R. Ouahrani, Y. Kouadri, F. Chebrouk, and N. Gherraf. "Synthesis of Novel Heterocyclic Compounds Containing 1,5-Benzodiazepine." Asian Journal of Chemistry 27, no. 6 (2015): 2175–77. http://dx.doi.org/10.14233/ajchem.2015.18011.

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18

Liu, Xiaoju, Guoyu Ren, Xiangruo Ma, Long Yan, Yurong Jiao, Yajun Ma, and Bingqin Yang. "Synthesis and characterization of novel ferrocenyl heterocyclic compounds." Russian Journal of General Chemistry 85, no. 1 (January 2015): 144–47. http://dx.doi.org/10.1134/s1070363215010247.

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19

Liu, Ying, Xiao‐Hong Zhang, Jun Ren, and Gui‐Yu Jin. "Convenient Preparation of Novel Fused Tri‐heterocyclic Compounds." Synthetic Communications 34, no. 1 (December 31, 2004): 151–57. http://dx.doi.org/10.1081/scc-120027248.

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20

Nair, Vijay, K. C. Sheela, K. V. Radhakrishnan, A. U. Vinod, J. Somarajan Nair, C. Rajesh, and P. M. Treesa. "Novel heterocyclic constructionviadipolar cycloadditions to 1,2-dicarbonyl compounds." Journal of Heterocyclic Chemistry 37, no. 3 (May 2000): 659–68. http://dx.doi.org/10.1002/jhet.5570370323.

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21

Bauer, Adriano, Eszter Borsos, and Nuno Maulide. "A Novel Class of 7-Membered Heterocyclic Compounds." European Journal of Organic Chemistry 2020, no. 26 (May 6, 2020): 3971–74. http://dx.doi.org/10.1002/ejoc.202000363.

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22

Rajkumar, Kommera, Pathi Suman, and Bhimapaka China Raju. "Facile construction of novel heterocyclic compounds: three-component, one-pot synthesis of 2-hydroxybenzoyl-1,2-dihydropyridine-3-carboxylates, ketones, pyridone-3-carboxylates and benzopyrido-1,3-oxazole-4-carboxylates." RSC Advances 5, no. 90 (2015): 73850–58. http://dx.doi.org/10.1039/c5ra10185a.

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A facile method has been developed for the preparation of novel heterocyclic compounds facilitated by 3-oxobutanoates and 1,3-diketones possessing a trihalo group. This three-component, one-pot protocol provided heterocyclic compounds without a catalyst.

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23

Randić, Milan, Sonja Nikolić, and Nenad Trinajstić. "Aromaticity in heterocyclic molecules containing divalent sulfur." Collection of Czechoslovak Chemical Communications 53, no. 9 (1988): 2023–54. http://dx.doi.org/10.1135/cccc19882023.

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The conjugated circuits model is applied to heterocycles containing divalent sulfur. A novel parametrization is introduced for 4n + 2 and 4n conjugated circuits containing a single sulfur atom. The relative aromatic stabilities of a number of heterocyclic systems containing divalent sulfur are studied. Comparison is made whenever possible with earlier reported resonance energies of these compounds, obtained by using Huckel MO and SCF π-MO models, and appropriate reference structures. Special attention is given to positional isomers. An explanation of the differences amongst such isomers is given.

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24

Houbrechts, Stephan, Carlo Boutton, Koen Clays, André Persoons, Ian R. Whittall, Raina H. Naulty, Marie P. Cifuentes, and Mark G. Humphrey. "Novel Organometallic Compounds for Nonlinear Optics." Journal of Nonlinear Optical Physics & Materials 07, no. 01 (March 1998): 113–20. http://dx.doi.org/10.1142/s0218863598000090.

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Hyper-Rayleigh scattering is used to investigate the nonlinear optical properties of novel metal (ruthenium, nickel and gold) σ-arylacetylide complexes. The influence of the organometallic donor group and conjugating bridge on the quadratic hyperpolarizability is studied. For all organic ligands, the addition of the metal (donor) group is shown to increase the static hyperpolarizability by a factor of 2, 4 and 7 for gold, nickel and ruthenium complexes, respectively. Moreover, replacement of phenyl with a heterocyclic ring is demonstrated to enlarge the hyperpolarizability in the case of gold and ruthenium compounds.

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25

Khudheyer Jawad Kadem. "Synthesis of Heterocyclic Compounds Containing Sulphur From Ethylene Diamine Tetra Acetic acid Derivatives." International Journal of Research in Pharmaceutical Sciences 11, SPL4 (December 21, 2020): 1006–11. http://dx.doi.org/10.26452/ijrps.v11ispl4.4236.

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In this work, three novel Schiff's bases subsidiaries were set up from Ethylene Diamine Tetra Acetic corrosive Derivatives(K1, K2 and K3); (K1) which was blend from response of EDTA with 4-hydroxybenzaldehyde and 2,4-dintrophenyl hydrazine. (K2) which was union from response of EDTA with vinilline and 2,4-dintrophenyl hydrazine. (K3) which was amalgamation from response of EDTA with 4-aminoacetophenone and 2,4-dintrophenyl hydrazine after that combination three novel hetrocyclic compound Containing Sulfur molecule; Derivative with compounds containing carbonyl group (aldehyde or ketone) the carbonyl group of aldehyde or ketone react with primary amine to produce mine compounds (Schiff bases), Reaction of produced Schiff base compounds with mercaptoacetic acid (thioglycolic acid) to synthesized new heterocyclic compounds Compounds with heterogeneous ring are characterized by having many biological activities Which attracts the attention of researchers, and accordingly various derivatives containing sulfur were prepared for heterocyclic compounds, these prepared compounds can have inhibitory activity for some bacteria, fungi, and viruses. (M1,M2 and M3)which were union from response of (K1,K2 and K3) individually with marcaptoacetic acid. All of the Schiff’s bases derivatives and hetrocyclic compound Containing Sulphur atom were characterized and identified by spectroscopic methods ( FT-IR and 1H-NMR) spectroscopies.

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26

Mistry, K. M., and K. R. Desai. "Synthesis of Novel Heterocyclic 4-Thiazolidinone Derivatives and their Antibacterial Activity." E-Journal of Chemistry 1, no. 4 (2004): 189–93. http://dx.doi.org/10.1155/2004/590439.

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4-Thiazolidinones have been prepared by the reaction of various substituted Schiff bases 3 with Thioglycolic acid and Thiolactic acid. The intermediate Schiff bases 3 were synthesized by the condensation of various substituted 2-amino benzothiazole 1 with 1-(4'-methyl Phenyl)-3-methyl-5-pyrazolone 2. The starting compound substituted 2-amino benzothiazoles were prepared from various substituted amines via substituted phenyl thiourea. The structures of the compounds have been confirmed by elemental analysis and spectral analysis. The antibacterial activity of the compounds has also been screened againstStaphylococcus aureusandEscherichia coli.

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27

Kaddouri, Y., B. Bouchal, F. Abrigach, M. El Kodadi, M. Bellaoui, and R. Touzani. "Synthesis, Molecular Docking, MEP and SAR Analysis, ADME-Tox Predictions, and Antimicrobial Evaluation of Novel Mono- and Tetra-Alkylated Pyrazole and Triazole Ligands." Journal of Chemistry 2021 (February 23, 2021): 1–11. http://dx.doi.org/10.1155/2021/6663245.

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Newly synthesized compounds of N-alkylated heterocyclic compounds were prepared by condensation of amine with alcohol which undergoes a reaction of SN2. These newly synthesized derivatives were characterized by spectral analysis. The objective is to prepare new potent nontoxic antimicrobial agents which are easy to synthesize and could be scaled up in pharmaceutical industries. Thirteen new heterocyclic compounds containing a pyrazole moiety were synthesized with good yields (29.79 to 99.6%) and were characterized by FTIR, 1H NMR, 13C NMR, and CG-MS techniques. The compounds were divided into two series—monoalkylated compounds (1–11) and tetra-alkylated compounds (12 and 13)—and then evaluated for their in vitro antifungal and antibacterial activities against several fungal and bacterial strains. None of the monoalkylated compounds had antibacterial or antifungal activity. However, the two tetra-alkylated pyrazole ligands displayed strong antibacterial potential. Moreover, compound 12 was more potent against all tested bacterial strains than compound 13. Interestingly, compounds 12 and 13 acted as weak antifungal agents against Saccharomyces cerevisiae. ADME-Tox studies suggested that compounds 12 and 13 exhibit better toxicity profiles than the commercial antibiotic streptomycin. MEP studies suggested that compounds 12 and 13 have the same charge locations but differ in their values which are due to the condensed geometry of compound 13 that make it more polarizable than compound 12. Of particular interest, these different MEPs were evident in ligand protein docking, suggesting that compound 12 has better affinity with MGL enzyme than compound 13. All these findings suggested that these novel compounds represent promising antibacterial lead compounds.

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28

Sharma, Piush, and Charanjeet Singh. "Synthesis, characterization and biological evaluation of some novel N-Mannich bases of heterocyclic 1,3,4-thiadiazole." Journal of Drug Delivery and Therapeutics 9, no. 4-A (August 30, 2019): 220–28. http://dx.doi.org/10.22270/jddt.v9i4-a.3332.

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A series of some novel N-Mannich bases of heterocyclic 1,3,4-thiadiazole were synthesized through the condensation reaction of 1,3,4-thiadiazole containing a aromatic secondary amine, aromatic aldehydes and cyclic compounds employing Mannich reaction and using conventional synthesis. All the synthesized compounds were obtained in the range of 57.41-83.3 % yield. The structures of synthesized compounds were confirmed by UV, IR, 1H NMR spectroscopy. the essential structural features responsible for interaction with receptor site are established within a suggested pharmacophore. The in vitro antibacterial activity of the synthesized compounds was determined, against two Gram-positive bacteria, viz. S. aureus & B. subtilis and Gram-negative, viz. E. coli and K. pneumoniae, by cup-plate method using the standard drug ciprofloxacin. Minimum inhibitory concentrations (MIC) changed in the range of 1.56_ _ 200 mg mL_1. Compound 3b exhibited excellent activity against both bacteria. The in vitro antifungal activity of the synthesized compound was also evaluated by cup-plate method against the fungi A. niger and C. albicans compared with the standard drug Fluconazole. Compound 4a, 8a exhibited excellent activity against both fungi. The result has shown that the compounds are quite active against pathogens under study and were nontoxic. The anti-inflammatory activity of the compound was evaluated, on albino rats, by carageenan induced rat paw oedema method using the standard drug diclofenac sodium. Compound 7b and 8c exhibited excellent anti-inflammatory and analgesic pharmacological activities. Structurally the compound 7b has a greater number of unsaturated hydrocarbons in schiff base, which shows good lipophilic properties within electron rich morpholine ring in Mannich base. Statistical significance of differences between group was determined by one-way analysis of variance (ANOVA). Among the synthesized compounds 3a, 4b, 5c, 7b, 8a and 8c were found be the most active. All the synthesized compounds were found to be low lethal as ascertained by LD50 test. Keywords: N- Mannich bases of heterocyclic 1,3,4-thiadiazole derivatives; Mannich reaction; antimicrobial agents; anti-inflammatory activity;

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29

Xia, Liang, Yan Zhang, Jingbo Zhang, Songwen Lin, Kehui Zhang, Hua Tian, Yi Dong, and Heng Xu. "Identification of Novel Thiazolo[5,4-b]Pyridine Derivatives as Potent Phosphoinositide 3-Kinase Inhibitors." Molecules 25, no. 20 (October 12, 2020): 4630. http://dx.doi.org/10.3390/molecules25204630.

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A series of novel 2-pyridyl, 4-morpholinyl substituted thiazolo[5,4-b]pyridine analogues have been designed and synthesized in this paper. These thiazolo[5,4-b]pyridines were efficiently prepared in seven steps from commercially available substances in moderate to good yields. All of these N-heterocyclic compounds were characterized by nuclear magnetic resonance (NMR) and high-resolution mass spectrometry (HRMS) analysis and tested for phosphoinositide 3-kinase (PI3K) enzymatic assay. The results indicated that these N-heterocyclic compounds showed potent PI3K inhibitory activity, and the IC50 of a representative compound (19a) could reach to 3.6 nm. The structure−activity relationships (SAR) study showed that sulfonamide functionality was important for PI3Kα inhibitory activity, and 2-chloro-4-florophenyl sulfonamide (19b), or 5-chlorothiophene-2-sulfonamide (19c) showed potent inhibitory activity with a nanomolar IC50 value. The pyridyl attached to thiazolo[5,4-b]pyridine was another key structural unit for PI3Kα inhibitory potency, and replacement by phenyl lead to a significant decrease in activity. Enzymatic Inhibition results showed that compound 19a inhibited PI3Kα, PI3Kγ, or PI3Kδ with a nanomolar IC50 value, but its inhibitory activity on PI3Kβ was approximately 10-fold reduced. Further docking analysis revealed that the N-heterocyclic core of compound 19a was directly involved in the binding to the kinase through the key hydrogen bonds interaction.

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30

Muslim, Rasim Farraj, and Suheb Eaid Saleh. "Synthesis, Characterization and Evaluate the Biological Activity of Novel Heterocyclic Derivatives from Azomethine Compounds." Oriental Journal Of Chemistry 35, no. 4 (August 16, 2019): 1360–67. http://dx.doi.org/10.13005/ojc/350416.

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This research includes synthesis of new seventh-membered heterocyclic derivatives as 1,3-oxazepine-dione derived from azomethine compounds. Azomethine compounds R1-R4 were synthesized by the reaction of aromatic aldehydes with primary aromatic amines. The novel of 1,3-oxazepine-dione derivatives R5-R9 were obtained from the treatment of azomethine compounds with anhydrides. The synthesized compounds were checked by TLC technique, spectral methods (FT-IR, H1-NMR) and measurements of some its physical properties. The biological activity of the heterocyclic derivatives was investigated against bacteria and fungi in vitro.

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31

Khwaza, Vuyolwethu, Sithenkosi Mlala, Opeoluwa O. Oyedeji, and Blessing A. Aderibigbe. "Pentacyclic Triterpenoids with Nitrogen-Containing Heterocyclic Moiety, Privileged Hybrids in Anticancer Drug Discovery." Molecules 26, no. 9 (April 21, 2021): 2401. http://dx.doi.org/10.3390/molecules26092401.

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Pentacyclic triterpenoids are well-known phytochemicals with various biological activities commonly found in plants as secondary metabolites. The wide range of biological activities exhibited by triterpenoids has made them the most valuable sources of pharmacological agents. A number of novel triterpenoid derivatives with many skeletal modifications have been developed. The most important modifications are the formation of analogues or derivatives with nitrogen-containing heterocyclic scaffolds. The derivatives with nitrogen-containing heterocyclic compounds are among the most promising candidate for the development of novel therapeutic drugs. About 75% of FDA-approved drugs are nitrogen-containing heterocyclic moieties. The unique properties of heterocyclic compounds have encouraged many researchers to develop new triterpenoid analogous with pharmacological activities. In this review, we discuss recent advances of nitrogen-containing heterocyclic triterpenoids as potential therapeutic agents. This comprehensive review will assist medicinal chemists to understand new strategies that can result in the development of compounds with potential therapeutic efficacy.

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32

Su, Biyun, Yaning Li, Dandan Pan, Paison Faida, Tingyu Yan, and Zhan Qu. "Microwave Irradiation Syntheses and Crystal Structures of Two Series of Novel Fivemembered Heterocyclic Mono-Imine Compounds." Current Organic Synthesis 16, no. 3 (June 17, 2019): 444–48. http://dx.doi.org/10.2174/1570179416666181207125604.

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Aim and Objective: The late transition metal complexes with five-membered heterocyclic mono-imine ligands have attracted much attention because of their potential application in olefin polymerization catalysis. In order to increase the coordination ability of heteroatom N and S to center metals, CH3 group was introduced into the side arm of pyrrole imine and thiophene imine respectively, to get two series of novel five-membered heterocyclic imine compounds, mono(imino)pyrroles and mono(imino)thiophenes Materials and Methods: Two series of novel five-membered heterocyclic compounds with the mono-imine group were synthesized from the p-toluene sulfonic acid catalyzed Schiff base condensation of aromatic amines and 2-acetylpyrrole/ 2-acetylthiophene respectively, using CH3 group to substitute the common H atom on the side arm of pyrrole imine/ thiophene imine. Results: All the heterocyclic mono-imine compounds were characterized adequately by means of 1H NMR, 13C NMR, FT-IR, elementary analysis, as well as X-ray crystallographic diffraction. The reactivity differences between two precursor 2-acetylpyrrole and 2-acetylthiophene with aromatic amines were compared and discussed in detail. Conclusion: Compared to traditional heating methods, the solvent-free microwave irradiation seemed more efficient to prepare these series of five-membered heterocyclic mono-imine compounds, which resulted in a higher yield and cleaner product.

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M, Bhagavaan Raju, A. Ramesh A, and A. Raghuram Rao. "Synthesis and Evaluation of 2, 3, 4, 6-Tetra-Substituted-2, 3-Dihydropyridine Derivatives as Novel Antimicrobial Agents." International Journal of Pharmaceutical Sciences and Nanotechnology 11, no. 5 (September 30, 2018): 4268–74. http://dx.doi.org/10.37285/ijpsn.2018.11.5.7.

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The present study has been carried out to synthesize and screen certain heterocyclic antimicrobial compounds with clues from the biologically potent activities of heterocyclic compounds containing pyridine. With a view to synthesize some biologically active compounds, it has been felt worthwhile to study the synthesis of 2, 3, 4, 6-tetra-substituted-2,3-dihydro pyridine derivatives (7a-t). They were synthesized by the condensation of respective 2-amino-2,3-dihydropyridines with different aromatic aldehydes. 7a-t were purified and characterized by physical and spectral methods (IR, 1HNMR & MS). All the compounds were evaluated for their antimicrobial activity by the agar diffusion method against Bacillus subtilis, Staphylococcus aureus, Escherichia coli, Proteus vulgaris, Candida albicans and Saccharomyces cerevisiae. All the compounds exhibited mild to moderate antibacterial & antifungal activity. Among these compounds, compound 7h (R= Cl, R1=Cl) showing greater inhibitory activity against all tested organisms employed with zones inhibition of 20 to 15 mm at a concentration of 150 μ g/mL. Compounds 7g, 7c, 7i and 7j have been found as the next in the order of its antimicrobial potency. These compounds have the potential as novel antimicrobial agents.

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Honavar, Premanand M., Vasantha Kumar, P. Nikhil, Naveen Kumar, S. Sreenivasa, P. Vishwanatha, Boja Poojary, and B. Shivarama Holla. "Synthesis, Anti-inflammatory Activity and in silico Studies of Some Novel Morpholine Based Carboxamides." Asian Journal of Chemistry 32, no. 4 (February 25, 2020): 901–6. http://dx.doi.org/10.14233/ajchem.2020.22488.

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Two series of carboxamides were synthesized from 3-fluoro-4-morpholinoaniline and different substituted aromatic/heterocyclic carboxylic acids. All the compounds were characterized by IR, 1H NMR, 13C NMR and mass spectral data. The newly synthesized amide derivatives were screened for anti-inflammatory activity by following carrageenan induced rat paw edema method. Among the compounds screened, compound 6e was found to be highly potent. Molecular docking interaction of active compounds revealed that effective binding was observed in the pocket of COX-I and COX-II proteins.

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Elsayed, Galal A., Naglaa F. H. Mahmoud, and Sameh A. Rizk. "Solvent-free Synthesis and Antimicrobial Properties of Some Novel Furanone and Spiropyrimidone Derivatives." Current Organic Synthesis 15, no. 3 (April 27, 2018): 404–13. http://dx.doi.org/10.2174/1570179414666170830124447.

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Background: The regioselective synthesis of spiro-heterocyclic compounds is intriguing since those compounds have unique non-planar structures and great potential for binding to biomolecules because of their inherent rigid chiral structure. A novel class of furanone and spiro-heterocyclic derivatives were synthesized and evaluated for antifungal activities to establish structure-activity relationship (SAR). Results: The synthesis was carried out through one-pot multicomponent reaction (MCR) of 4-aryl-4-oxo-2- butenoic acids, camphor, urea, and hydrogen peroxide in the presence of sodium ethoxide as a catalyst using a microwave irradiation method and / or a traditional thermal method. They are used as key starting materials to synthesize some heterocyclic compounds. Structures of all synthesized compounds were elucidated by elemental analyses and spectroscopic data. Conclusion: A facile and efficient method for the preparation of a new furanone, chalcone and spiropyrimidone derivatives via the one-pot MCR with the microwave-assisted irradiation was established.

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Zaki, Remon M., Adel M. Kamal El Dean, Maisa I. Abd El Monem, and Mohamed A. Seddik. "Novel synthesis and reactions of pyrazolyl-substituted tetrahydrothieno[2,3-c]isoquinoline derivatives." Heterocyclic Communications 22, no. 2 (April 1, 2016): 103–9. http://dx.doi.org/10.1515/hc-2015-0204.

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AbstractTreatment of isoquinolinecarboxamide 4a with triethyl orthoformate, chloroacetyl chloride or carbon disulfide afforded the pyrimidinone 7, oxopyrimidinethione 12 and chloromethylpyrimidinone 18, respectively. These products were used as versatile starting materials for synthesis of other heterocyclic compounds. The heterocyclic hydrazide 6 was also obtained.

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Godge, Rahul K., and Rahul Kunkulol. "Synthesis of novel heterocyclic Quinolone compound for anti -tubercular activity." International Journal of Clinical and Biomedical Research 4, no. 3 (July 31, 2018): 44–49. http://dx.doi.org/10.31878/ijcbr.2018.43.10.

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In last few decades, though significant progress has been made in the treatment and control strategies of tubercular infections by introducing new diagnostic and monitoring tools and combination therapy, it still continues to be severe problem. The need of study was only because of there are many drugs in market to treat infection but most of the drugs are showing resistance because of the same it is difficult to treat the infection. In this study we chosen quinolone nucleus for study and over it. Thus with the aim of developing novel molecule with improved potency for treating Mycobacterium tuberculosis H37Rv strain infections and with decreased probability of developing drug resistance. Methodology: The synthesis of Quinolone derivatives, starting from substituted aniline and ethyl acetoacetate, by conventional organic reaction and results of investigations of their anti-mycobacterial activity. Results: MICs of the synthesized compounds are compared with existing drugs Cytotoxicity. The substituted quinolones are synthesized by taking mixture of 7-substituted-2-(3-chloro-2-oxopropyl) quinolin-4(1H)-one and different secondary amines. Many compounds have shown promising activity while some were inactive. Conclusion: It was found that Compound A1, A3, B1, B3, have shown promising anti tubercular activity whereas compound A2, A4,B2,B4 were showing moderate anti tubercular activity against std. Streptomycin.

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Sethi, Arun, Akriti Bhatia, Ranvijay Pratap Singh, and Atul Srivastava. "Synthesis and Evaluation of Some Novel Pregnane Derivatives as Anti-Hyperlipidemic and Anti-Oxidant Agents." Letters in Organic Chemistry 16, no. 1 (December 4, 2018): 40–49. http://dx.doi.org/10.2174/1570178615666180806123719.

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In the present paper, synthesis of few novel pregnane derivatives and their evaluation as potential anti-hyperlipidemic and anti-oxidant agents has been reported. The synthesis of 3β-hydroxy- 16α-methoxy pregn-5-en-20-one (4) was achieved by reaction of 3β-hydroxy-5,16-pregnadiene-20-one (3) with KOH/MeOH under reflux. Compound 4 on treatment with succinic and phthalic anhydride afforded compound 6 and 7, respectively. The reaction of the C-20-oxime-pregnadiene (8) with 1,5- dibromohexane yielded 20-(O-6-bromo hexyl)-oximino-3β-hydroxy-pregn-5, 16-diene (9). A novel heterocyclic derivative 3β-hydroxy-androst-5-en [17,16-c]-2′-methyl-7′ bromo-3′,4′-dihydro quinoline (16) was synthesized by reaction of 3 with 3-bromoaniline. However, attempted synthesis of other heterocyclic derivatives by reaction of (3) with other halogenated amine led to Aza-Michael addition products (10-14). The synthesized compounds were also evaluated for their anti-hyperlipidemic and anti-oxidant activities. Compounds 6 and 14 were found to exhibit more lipid lowering and antioxidant activities in comparison to other compounds.

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Alho, Daniela, Jorge Salvador, Marta Cascante, and Silvia Marin. "Synthesis and Antiproliferative Activity of Novel Heterocyclic Glycyrrhetinic Acid Derivatives." Molecules 24, no. 4 (February 20, 2019): 766. http://dx.doi.org/10.3390/molecules24040766.

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A new series of glycyrrhetinic acid derivatives has been synthesized via the introduction of different heterocyclic rings conjugated with an α,β-unsaturated ketone in its ring A. These new compounds were screened for their antiproliferative activity in a panel of nine human cancer cell lines. Compound 10 was the most active derivative, with an IC50 of 1.1 µM on Jurkat cells, which is 96-fold more potent than that of glycyrrhetinic acid, and was 4-fold more selective toward that cancer cell line. Further biological studies performed in Jurkat cells showed that compound 10 is a potent inducer of apoptosis that activates both the intrinsic and extrinsic pathways.

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Jayanna, N. D., H. M. Vagdevi, J. C. Dharshan, T. R. Prashith Kekuda, B. C. Hanumanthappa, and B. C. Gowdarshivannanavar. "Synthesis and Biological Evaluation of Novel 5,7-Dichloro-1,3-benzoxazole Derivatives." Journal of Chemistry 2013 (2013): 1–9. http://dx.doi.org/10.1155/2013/864385.

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A new class of 5,7-dichloro-1,3-benzoxazole derivatives4–11were synthesized by fusing 5,7-dichloro-2-hydrazino-1,3-benzoxazole3nucleus with aliphatic acids, active methylene compounds, and with selected esters to form heterocyclic ring systems like 1,2,4-triazoles, pyrazoles, and triazine moieties. The compound3on diazotization reaction affords the tetrazole compound. The synthesized compounds were characterized by1H NMR, IR, Mass, and13C NMR spectral data and screened for cytotoxic, antimicrobial, antioxidant, and antilipase activities. The compounds4,5, and8have shown significant antimicrobial activities, whereas compounds6and8have been emerged as leading cytotoxic agents. The compounds9,10, and11were found to be strong enzyme inhibitors.

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Potapov, Vladimir A., Roman S. Ishigeev, Lyudmila A. Belovezhets, and Svetlana V. Amosova. "A Novel Family of [1,4]Thiazino[2,3,4-ij]quinolin-4-ium Derivatives: Regioselective Synthesis Based on Unsaturated Heteroatom and Heterocyclic Compounds and Antibacterial Activity." Molecules 26, no. 18 (September 14, 2021): 5579. http://dx.doi.org/10.3390/molecules26185579.

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A novel family of [1,4]thiazino[2,3,4-ij]quinolin-4-ium derivatives was synthesized by annulation reactions of 8-quinolinesulfenyl chloride with unsaturated heteroatom and heterocyclic compounds. It was found that the reactions with 4-pentenoic and 5-hexenoic acids, allyl chloride and bromide, allyl cyanate and vinyl heterocyclic compounds (N-vinyl pyrrolidin-2-one and 1-vinylimidazole) proceeded in a regioselective mode but with the opposite regiochemistry. The reactions with vinyl heterocyclic compounds included electrophilic addition of the sulfur atom of 8-quinolinesulfenyl chloride to the β-carbon atom of the vinyl group. In the case of other substrates, the annulation proceeded with the attachment of the sulfur atom to the α-carbon atom of the vinyl group. The antibacterial activity of novel water-soluble compounds against Enterococcus durans, Bacillus subtilis and Escherichia coli was evaluated. Compounds with high antibacterial activity were found.

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Korem, Maya, Sarah Kagan, and Itzhack Polacheck. "The Effect of Novel Heterocyclic Compounds on Cryptococcal Biofilm." Journal of Fungi 3, no. 3 (July 20, 2017): 42. http://dx.doi.org/10.3390/jof3030042.

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Kagan, S., A. Jabbour, E. Sionov, A. A. Alquntar, D. Steinberg, M. Srebnik, R. Nir-Paz, A. Weiss, and I. Polacheck. "Anti-Candida albicans biofilm effect of novel heterocyclic compounds." Journal of Antimicrobial Chemotherapy 69, no. 2 (September 26, 2013): 416–27. http://dx.doi.org/10.1093/jac/dkt365.

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WU, H. J., F. J. HUANG, and C. C. LIN. "ChemInform Abstract: Novel Heterocyclic Cage Compounds from 2-Methylthiofurans." ChemInform 23, no. 10 (August 22, 2010): no. http://dx.doi.org/10.1002/chin.199210216.

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Shailaja, K. M., Dipukakoty Dipukakoty, B. Shivakumar, and E. Jayachandran. "ChemInform Abstract: Synthesis and Characterization of Novel Heterocyclic Compounds." ChemInform 45, no. 1 (December 12, 2013): no. http://dx.doi.org/10.1002/chin.201401249.

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BUTIN, B. M., and A. D. SALIMBAEVA. "ChemInform Abstract: Synthesis of Novel Selenium-Containing Heterocyclic Compounds." ChemInform 22, no. 29 (August 23, 2010): no. http://dx.doi.org/10.1002/chin.199129231.

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47

Khairwar, Rekha, Diwa Mishra, and Arun Singh. "PREPARATION AND ANTIMICROBIAL STUDIES OF NOVEL FUSED HETEROCYCLIC COMPOUNDS." Rasayan Journal of chemistry 14, no. 03 (2021): 1947–52. http://dx.doi.org/10.31788/rjc.2021.1436365.

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de Andrade, Vitor, and Marcio de Mattos. "N-Halo Reagents: Modern Synthetic Approaches for Heterocyclic Synthesis." Synthesis 51, no. 09 (March 27, 2019): 1841–70. http://dx.doi.org/10.1055/s-0037-1611746.

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Heterocyclic chemistry is an essential frontier in science and a source of novel biologically active compounds. The development of innovative synthetic methodologies that allows access to different heterocyclic rings is of critical interest to the scientific community. This review will focus on recent applications of N-halo compounds (e.g., N-halosuccinimides, trihaloisocyanuric acids, N-halosulfonamides, etc.) in heterocyclic construction via electrophilic cyclization, asymmetric halocyclization, oxidative cyclization, and radical processes.1 Introduction2 N-Halo Reagent Mediated Heterocyclic Construction and Functionalization2.1 Electrophilic Halocyclizations2.1.1 Asymmetric Halocyclizations2.2 Radical Halocyclizations2.3 Oxidative Halocyclizations2.4 Miscellaneous Halocyclization Reactions3 Summary and Outlook

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Neha, Ashish Ranjan Dwivedi, Rakesh Kumar, and Vinod Kumar. "Recent Synthetic Strategies for Monocyclic Azole Nucleus and Its Role in Drug Discovery and Development." Current Organic Synthesis 15, no. 3 (April 27, 2018): 321–40. http://dx.doi.org/10.2174/1570179414666171013154337.

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Background: In recent years, the development and diversification of heterocyclic compounds has become central to the discovery of bioactive compounds with novel or improved pharmacological properties. In particular, N-containing heterocycles are proved to be promising leads and drug candidates, and received huge attention of the medicinal chemists. Objective: Many drugs especially antibiotics are becoming obsolete due to the development of multidrug resistance. Moreover, toxicity and other side effects of some drugs necessitated the quest for safer and more potent drug candidates. The current review article described biological potential of various monocyclic azoles. Recent developments in the synthesis of azole derivatives have been also reviewed. Conclusion: The presence of N-heterocyclic rings can influence the pharmacokinetics, pharmacodynamics, pKa and bioavailability profile of the drug molecules. Compounds containing monocyclic azole rings showed various biological activities and number of molecules are in clinical practice. A number of important leads and potential drug candidates containing azole nucleus are in advance stages of drug developments. Thus, simple, atom economic and more efficient synthetic strategies are desired for the synthesis of new libraries of the compounds.

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M. Mohareb, R., M. M. Kamel, and Y. R. Milad. "Uses of -diketones for the synthesis of novel heterocyclic compounds and their antitumor evaluations." Bulletin of the Chemical Society of Ethiopia 34, no. 2 (October 28, 2020): 385–405. http://dx.doi.org/10.4314/bcse.v34i2.15.

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The reaction of the 3-oxo-N,3-diphenylpropan-amide (3) with either malononitrile or ethyl cyanoacetate in ammonium acetate gave the 1,2-dihydropyridine derivatives 6a or 6b, respectively. On the other hand, carrying the same reaction in the presence of triethylamine gave the 1,6-dihydropyridine derivatives 7a and 7b, respectively. Moreover, compound 3 reacted with 2-aminoprop-1-ene-1,1,3-tricarbonitrile to give the pyridine derivative 9. Compound 7b reacted with the active methylene derivatives 10a,b and 4a,b to give the naphthyridine derivatives 11a,b and 12a,b; respectively. Compound 3 was also used for the synthesis of thiophene derivatives 13a,b and 16a,b. In addition, the reaction of ethyl benzoylacetate (1) with o-phenylene diamine gave the benzimidazole derivative 18. The reactivity of the latter product towards different reagents was studied to give different products. The cytotoxicity of the newly synthesized products was studied towards some cancer and normal cell lines, in addition toxicity of compounds was measured and docking of the most active compounds was done. Compounds 6b, 7b, 9, 13a, 13b, 16a, 20b, 20c, 24b, 25 and 26b exhibited optimal cytotoxic effect against cancer tested cell lines. These active compounds were evaluated against c-Met kinase using foretinib as the reference drug where all compounds expressed higher activity than the reference drug. KEY WORDS: Ethyl benzoylacetate, Pyridine, Benzimidazole, Cytotoxicity Bull. Chem. Soc. Ethiop. 2020, 34(2), 385-405 DOI: https://dx.doi.org/10.4314/bcse.v34i2.15

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