S. A. Abdel-aziz

Bio: S. A. Abdel-aziz is an academic researcher from Ain Shams University. The author has contributed to research in topics: Acetamide & Benzothiazole. The author has an hindex of 5, co-authored 6 publications receiving 88 citations.

Synthesis of Bioactive 4-Oxo-4H-Chromenes Bearing Heterocyclic Systems from Hydrazonecarbodithioic Acid and Thiocarbohydrazone

Abstract: Condensation 4-oxo-4H-chromene-3-carboxaldehydes (1a,b) with acid hydrazine-carbodithioic acid and/or thiocarbohydrazide afforded hydrazonecarbodithioic acid 2, monothiocarbohydrazone 3a,b and bisthiocarbohydrazone 4, respectively. Heterocyclization of 2–4 via reaction with oxygen, sulfur and/or halogen reagents in different media yielded pyridazinethione 5; 1,3-thiazoles 7; pyrazoles 9–12; 1,2,4-thiadiazoles 8,13,14, and 23; 1,2,4-triazolethiones 15–17; 1,2,4-triazinethiones 18–22; imidazolethione 24 and pyrimidinethione 25 derivatives. Antifungal activity was screened for some the new synthesized compounds. Formulations of all products have been deduced by elemental analysis and spectral data (IR, 1H NMR and Mass spectroscopy).

Synthesis of Some New 4-oxo-4H-Chromene Derivatives Bearing Nitrogen Heterocyclic Systems as Antifungal Agents

Abstract: Some new 4-oxo-4H-chromone derivatives bearing nitrogen heterocyclic systems were achieved by treatment of 3-[(4-aminophenylimino) methyl]-6-chloro-4-oxo-4H-chromene (2) with some aldehydes, cyclic oxygen, and halogen compounds, followed by heterocyclization. Significant antifungal activities were observed for some of the prepared compounds. Structures of all products were confirmed by elemental analysis, IR, 1H-NMR, and mass spectra.

Fused cyanopyrimidines: part ii synthesis and reactions of fused cyanopyrimidine derivatives as affecting enzymatic agents

Abstract: Some new fused heterobicyclic systems, such as thiazolo[3,2-a]-pyrimidin-5-one (3), 2,3-tetrahydrothiazolo[3,2-a]pyrimidin-5-one (5), 2,4-tetrahydrothiazino[3,2-a]pyrimidin-3,6-dione (6), 3-dihydrothiazino[3,2-a]pyrimidin-2,4,6-trione (7), 3-arylidenethiazino[3,2-a]pyrimidin-2,4,6-trione (8) and/or the related nitrogen compounds, such as 2,3-tetrahydroimidazolo[3,2-a]-pyrimidin-5-one (9), 1-aryl-2,3-tetra-hydroimidazolo[3,2-a]pyrimidin-5-one (11), quinazolino[3,2-a]-pyrimidin-6,8-dione (12) and 3-mercapto-1,2,4-triazolo[4,3-a]pyrimidin-5-one (14) have been synthesized by the interaction of 2-mercapto-4-arylidene-5-cyanopyrimidin-6(1H)one (1) with α,β-bifunctional nitrogen, oxygen and/or sulfur compounds The structures have been characterized by elemental analyses, IR, UV, 1H NMR and mass spectral data Some newly prepared compounds revealed a moderate effect on the activity of cellobiase produced by Aspergillus nidulans

Synthesis and antimicrobial activities of some new 2-substituted benzoxazole/benzothiazole derivatives.

Abstract: In the search for new antimicrobial compounds, several new sulfur bearing heterobicyclic moieties (4-11) have been synthesized by acylation and alkylation of acetamide, thioacetamide and semicarbazide derivatives. The structure of the products was deduced from elemental analyses as well as spectral data (IR, 1H NMR and MS). Significant antimicrobial activities were obtained for all new compounds especially against Fusarium oxysporum.

Fused cyanopyrimidines: part-i synthesis and reactions of fused cyanopyrimidine derivatives and their effect on cellobiase activity

Abstract: Some new fused heterotricyclic systems containing the cyanopyrimidine moiety have been synthesized from the interaction between 2-mercapto-4-arylidene-5-cyanopyrimidin-6(1H)one (1) with bi-functional halogen and nitrogen compounds. Structures of the new products have been established by elemental analyses and spectral data (UV, IR, 1H NMR and mass). Effect of the newly synthesized compounds on the activity of the cellobiase produced by Aspergillus nidulans was studied.

Substituted heterocyclic compounds and methods of use

Abstract: The present invention relates to compounds having the general formula (I) or a pharmaceutically acceptable salt thereof, wherein Rl is a saturated or unsaturated 5-, 6- or 7-membered, ring containing 0, 1, 2 or 3 atoms selected from N, O and S, wherein the ring may be fused with a benzo group, and is substituted by 0, 1 or 2 oxo groups, and wherein R1 is additionally substituted; and R2 is a substituted C1-6balkyl. Also included is a method of prophylaxis or treatment of inflammation, rheumatoid arthritis, Pagets disease, osteoporosis, multiple myeloma, uveititis, acute or chronic myelogenous leukemia, pancreatic β cell destruction, osteoarthritis, rheumatoid spondylitis, gouty arthritis, inflammatory bowel disease, adult respiratory distress syndrome (ARDS), psoriasis, Crohn's disease, allergic rhinitis, ulcerative colitis, anaphylaxis, contact dermatitis, asthma, muscle degeneration, cachexia, Reiter's syndrome, type I diabetes, type II diabetes, bone resorption diseases, graft vs. host reaction, Alzheimer's disease, stroke, myocardial infarction, ischemia reperfusion injury, atherosclerosis, brain trauma, multiple sclerosis, cerebral malaria, sepsis, septic shock, toxic shock syndrome, fever, myalgias due to HIV-1, HIV-2, HIV-3, cytomegalovirus (CMV), influenza, adenovirus, the herpes viruses or herpes zoster infection in a mammal comprising administering an effective amount a compound as described above.

In Vitro Activities of Position 2 Substitution-Bearing 6-Nitro- and 6-Amino-Benzothiazoles and Their Corresponding Anthranilic Acid Derivatives against Leishmania infantum and Trichomonas vaginalis

Abstract: 6-Nitro- and 6-amino-benzothiazoles bearing different chains in position 2 and their corresponding anthranilic acid derivatives were investigated for their in vitro antiparasitic properties against parasites of the species Leishmania infantum and Trichomonas vaginalis compared to their toxicity towards human monocytes. Biological investigations established that the antiprotozoal properties depended greatly on the chemical structure of the position 2 substitution-bearing group. Compound C1, 2-[(2-chloro-benzothiazol-6-yl) amino] benzoic acid, demonstrated an interesting antiproliferative activity towards parasites of the species T. vaginalis, while compound C11, 2-({2-[(2-hydroxyethyl) amino]-benzothiazol-6-yl} amino) benzoic acid, exhibited a promising activity against parasites of the species L. infantum in their intracellular amastigote form. Additional experiments established that compound C11, which was poorly toxic against the promastigote and the extracellular amastigote forms of the parasite, could improve host-protective mechanisms against Leishmania by preventing parasite internalization by macrophages and stimulating NO production, by means of a mechanism synergistically enhanced by the presence of gamma interferon.