Reactivity of Hydrazine, Some Hydrazine derivatives and Diamines toward Ethyl 2,2-Dicyano-1-aryl (or alkyl)vinylcarbamate

A series of pyrimidinone and dipyrimidinone derivatives 2a-c, 4a-e and 6a-f has been synthesized via the reaction between ethyl 2,2-dicyano-1-aryl(or alkyl)vinylcarbamate derivatives 1a-d and hydrazine derivatives or  diamines. The reactivity of compounds 1a-d toward hydrazine is studied. The result is the formation of triazolones 5a-d rather than pyrimidinone derivatives

A Novel Synthesis of (Z)-ethyl 3-amino-2-cyano-3-phenyl(or alkyl)acrylate and ethyl- 2-cyano-3-phenyl-3-propionylimino-propanoate

Reaction between ethyl cyanoacetate and imidate, N-acetyl imidate and N-ethoxycarbonyl imidate in basic medium are student. The structure and geometrically configuration of (Z)-ethyl 3-amino-2-cyano-4-phenylbut-2-enoate 3c was established by X-ray diffraction. The functionality in ethyl 2-cyano-3-(ethoxycarbonyl)-3-p-tolylacrylate 7b was exploited to get the desired heterocycle. Â

A Facile Synthesis of Pyrimidoquinazoline Derivatives

A series of pyrimidoquinazoline are prepared via the reaction of ethyl 2,2-dicyano-1-arylvinylcarbamate derivatives 1a-b with methyl 2-aminobenzoate, 1-(2-aminophenyl)ethanone and 2-aminobenzonitrile. The reactivity of compounds 1a-b toward 3-amino-4,6-diphénylnicotinonitrile are studied. The structures of the synthesized compounds are elucidated by X-ray diffraction, IR spectroscopy and nuclear magnetic resonance.Â

Synthesis of aminocyanopyrazoles via a multi-component reaction and anti-carbonic anhydrase inhibitory activity of their sulfamide derivatives against cytosolic and transmembrane isoforms

A convenient protocol for the multicomponent reaction (MCRs) between malononitrile with an orthoester and hydrazine derivatives, under acid catalyst is described. A series of aminocyanopyrazoles 4 was prepared, isolated and characterized. These pyrazoles reacted with sodium nitrite followed by secondary amine reagent and with formic acid to lead pyrazolotriazines 6 and pyrazolopyrimidinones 7. Some of the aminopyrazoles were converted to the corresponding sulfamides by reaction with sulfamoyl chloride. The aminopyrazoles incorporating phenyl and tosyl moieties were tested as inhibitors of four carbonic anhydrase (CA, EC 4.2.1.1) isoforms, the human (h) hCA I, II, IX and XII. Many of them showed low micromolar or submicromolar inhibition of these enzymes. The corresponding sulfamides were low nanomolar CA inhibitors

Synthesis and Antitubercular Evaluation of Some Novel 1,2,3,6-tetrahydropyrimidine-5-carbonitrile

         In an attempt to find a new class of antitubercular agents, a series of 1,2,3,6-tetrahydropyrimidine-5-carbonitrile were prepared via the reaction  of ethyl N-ethoxycarbonylbenzimidate 2a-b with cyanoacetanilide derivatives 1a-c. These compounds were screened for their antitubercular activity against M. tuberculosis. Several analogues, such as 2,6-dioxo-1-phenyl-4-p-tolyl-1,2,3,6-tetrahydropyrimidine-5-carbonitrile 3a, 1-benzyl-2, 6-dioxo-4-p-tolyl-1,2,3,6-tetrahydropyrimidine-5-carbonitrile 3c and 1-benzyl-2, 6-dioxo-4-phenyl-1,2,3,6-tetrahydropyrimidine-5-carbonitrile 3d exhibited a potent antitubercular activity with an MIC values ranging from 10-35 µg/ml. Structures of the newly synthesized compounds were established by spectral data and HRMS

A Proposal to Mitigate Energy Consumption through the Sustainable Design Process in Tunis

The main objective of this paper is to assess the energy efficiency of residential buildings in Tunis. To this end, three complementary studies were carried out at different levels. Initially, a diagnosis of the building’s adaptability to climate change at urban and architectural scales was established. The methodology adopted was based on indicators obtained following a cross-reference of environmental assessment tools. This made it possible to highlight the lacunary factors related to thermal comfort. According to this finding, the second research was set up to focus on outdoor thermal comfort. The methodology adopted is based on numerical simulations and calculations of comfort indices. The results demonstrated the importance of specific morphological indicators at the urban scale. Finally, the third research is interested in the architectural scale to assess the building’s thermal comfort and energy consumption. It was performed through numerical simulations. The results demonstrated the impact of specific physical indicators on buildings’ thermal comfort and energy behavior. Ultimately, this research highlighted the gap factors in urban and architectural design in Tunis. It detected the most significant physical and morphological indicators to be considered for sustainable urban design

5-Amino-3-methyl-1-phenyl-1H-1,2,4-triazole

In the title compound, C9H10N4, the phenyl and triazole rings make a dihedral angle of 38.80 (2)°. N—H⋯N hydrogen bonds link the mol­ecules, forming centrosymmetric R 2 2(8) rings; these rings are inter­connected through a C(5) chain, building up a zigzag layer parallel to the (100) plane

Ethyl 6-amino-5-cyano-4-isopropyl-2-methyl-4H-pyran-3-carboxyl­ate

In the title compound, C13H18N2O3, the two H atoms of the NH2 group are engaged in hydrogen bonding with the N atom of the cyano group and with one O atom of the ethoxy­carbonyl group, building a chain parallel to the [100] direction. The N—H⋯N hydrogen bonds assemble the mol­ecules around inversion centres, forming dimers with an R 2 2(12) graph-set motif

Exploring the Potential of Sulfonamide-Dihydropyridine Hybrids as Multitargeted Ligands for Alzheimer’s Disease Treatment

Alzheimer’s disease (AD) is a multifactorial neurodegenerative disease that has a heavy social and economic impact on all societies and for which there is still no cure. Multitarget-directed ligands (MTDLs) seem to be a promising therapeutic strategy for finding an effective treatment for this disease. For this purpose, new MTDLs were designed and synthesized in three steps by simple and cost-efficient procedures targeting calcium channel blockade, cholinesterase inhibition, and antioxidant activity. The biological and physicochemical results collected in this study allowed us the identification two sulfonamide-dihydropyridine hybrids showing simultaneous cholinesterase inhibition, calcium channel blockade, antioxidant capacity and Nrf2-ARE activating effect, that deserve to be further investigated for AD therapy.This work was supported by the Regional Council of Franche-Comté (2022Y-13659 and 13660 Accurate Project).Peer reviewe

Synthesis and biological evaluation of benzochromenopyrimidinones as cholinesterase inhibitors and potent antioxidant, non-hepatotoxic agents for Alzheimer’s disease

We report herein the straightforward two-step synthesis and biological assessment of novel racemic benzochromenopyrimidinones as non-hepatotoxic, acetylcholinesterase inhibitors with antioxidative properties. Among them, compound 3Bb displayed a mixed-type inhibition of human acetylcholinesterase (IC50 = 1.28 ± 0.03 μM), good antioxidant activity, and also proved to be non-hepatotoxic on human HepG2 cell line.JMC thanks Government of Spain for support (SAF2016-65586-R), JJ and OS thank MH CZ- DRO (UHHK 00179906).We acknowledge support by the CSIC Open Access Publication Initiative through its Unit of Information Resources for Research (URICI)