IMIDES POSSESS A DIVERSE CHEMISTRY AND UNDERGO A VARIETY OF INTER- AND INTRAMOLECULAR ADDITION REACTIONS AT ACARBONYL GROUP [1]. THE MALEIMIDE MOTIF HAS FOUND WIDESPREAD USE IN A RANGE OF FIELDS DUE ITS DIVERSE REACTIVITY PROFILE. IT IS A HIGHLY REACTIVE CONJUGATE ACCEPTOR AND AS SUCH CAN BE EMPLOYED EFFECTIVELY IN SELECTIVE REACTIONS WITH NUCLEOPHILS, SUCH AS THIOLS. AS A RESULT IT IS ONE OF THE MOST WIDELY USED FUNCTIONAL GROUPS IN BIOCONJUGATION [2].THE REACTION OF MALEIMIDE OR N-ALKYLMALEIMIDE IN THE PRESENCE OF ZINC AND ACETIC ANHYDRIDE PROCEEDS SMOOTHLY IN TOLUENE TO PRODUCE THE SUCCINIMIDE OR N-ALKYLSUCCINIMIDE COMPOUNDS IN FAIRLY GOOD YIELDS. ALTHOUGH NUMEROUS EXAMPLES OF METAL REDUCTIONS METHODS APPEAR IN THE LITERATURE [3], NO BROAD STUDY OF THE SCOPE OF THIS METHOD FOR THE PREPARATION OF N-ALKYL SUCCINIMIDES HAS BEEN REPORTED. THE STRUCTURES OF THE PRODUCTS WERE DETERMINED ON THE BASIS OF ITS ELEMENTAL ANALYSES, 1H AND 13C NMR AND IR SPECTRAL DATA.

POTASSIUM HYDROGEN SULFATE (KHSO4) WAS USED AS AN EFFICIENT CATALYST FOR A SERIES OF NEW POLY-FUNCTIONALIZED INDOLE DERIVATIVES THAT WERE SYNTHESIZED VIA REACTION OF ALLOXAN MONOHYDRATE AND N-ARYL SUBSTITUTED ENAMINONES IN ETOH/H2O IN ROOM TEMPERATURE (SCHEME 1)....

SANDWICH AND HALF-SANDWICH COMPOUNDS CONTAINING PENDANT BORYL (-BX2) FUNCTIONS HAVE RECEIVED A GREAT DEAL OF ATTENTION IN RECENT YEARS AND HAVE BEEN EXTENSIVELY STUDIED. BORON COMPOUNDS DUE TO THEIR SPECIFIC CHEMICAL PROPERTIES REACT WITH FERROCENE AND LEAD TO COMPOUNDS WITH UNIQUE CAPABILITIES. BECAUSE OF THE BASICITY PROPERTY OF FERROCENE, ELECTROPHILIC SUBSTITUTION REACTION OCCURS WITH LEWIS ACIDS SUCH AS TRIHALOBORANE (BX3), AND ESPECIALLY TRIBROMOBORANE (BBR3). THE PRODUCTS OF THIS REACTION (FCBX2, FC = FERROCENE) COULD BE USED AS THE PRECURSORS FOR THE SYNTHESIS OF OTHER DERIVATIVES OF BORYLFERROCENE [1-3].IN THIS RESEARCH WE PRESENT THE SYNTHESIS OF TWO NEW COMPOUNDS OF FERROCENYLBORANE 2 AND 3, WHICH HAVE DIFFERENT LEWIS ACIDITY PROPERTIES. THE COMPOUNDS (DIBROMOBORYL) FERROCENE 1, LITHIUM-DIMETHYLAMID (LINME2) AND POTASSIUM-TRIS (TRIMETHYLSILYL)SILAN K[SI(SIME3)3] ARE VERY SENSITIVE TO AIR AND MOISTURE AND WERE FRESHLY SYNTHESIZED IN OUR LABORATORY. ALL REACTIONS MUST BE CARRIED OUT UNDER ARGON ATMOSPHERE. THE 11B-NMR RESONANCE OF COMPOUNDS 2 AND 3 APPEAR AT 36 AND 50 PPM, RESPECTIVELY, AS EXPECTED FOR SUCH COMPOUNDS.

PYRANOPYRAZOLES ARE AN IMPORTANT CLASS OF BIOLOGICALLY ACTIVE HETEROCYCLES. THEY ARE REPORTED TO POSSESS A MULTIPLICITY OF PHARMACOLOGICAL PROPERTIES INCLUDING ANTICANCER, ANTIMICROBIAL, ANTI-INFLAMMATORY, INSECTICIDAL, AND MOLLUSCICIDAL ACTIVITIES. THEY ARE ALSO POTENTIAL INHIBITORS OF HUMAN CHK1 KINASE [1, 2]. THEY ALSO FIND APPLICATIONS AS PHARMACEUTICAL INGREDIENTS AND BIODEGRADABLE AGROCHEMICALS [3].IN THIS WORK, WE FIRSTLY DESCRIBE THE GREEN AND MULTI-COMPONENT SYNTHESIS OF PYRANOPYRAZOLE DERIVATIVES AND THEN USING THEM FOR SYNTHESIS OF NOVEL HYBRID HETEROCYCLES CONTAINING PYRAZOLE, PYRANE AND PYRIMIDINE MOIETIES [SHEME 1].

3-Isothiazolone DERIVATIVES have shown antibacterial, antimycotic, antialgual and pesticidal activity and have been used as preservatives for the control of living organisms in cosmetics, paints, soaps, fabrics, leather, swimming pools, etc. for many years. Considering the limited number of reports on the mechanism of action and toxicity of 3-isothiazolones some reported and novel N-phenyl 3-isothiazolones with or without chlorine atom at the 5-position and having substituents at the 4-position of the phenyl moiety with different physicochemical properties were prepared and their antibacterial and antifungal activity were determined.The majority of compounds displayed moderate to high activity against some tested pathogenic bacteria and had MICs in the range of ciprofloxacin as the most active reference drugs and some compounds had either equal or higher antifungal activity in comparison with Itraconazole and Ketoconazole as standard drugs against the most tested fungi. These findings prompted us to determine the cytotoxicity of the most potent compounds of this investigation. Cytotoxicity of compounds XXVIII, XXXIII, XXXV, XXXVII, LXIX, LXXI was determined by the MTT test on HFFFp-16 cells, in comparison with Itraconazole as the reference drug.5-Chloro-2(4-chlorophenyl)-4-isothiazoline-3-one XXXV which had highest activity against gram positive and gram negative bacteria and was one of the most active compounds of this study against tested fungi, had lower toxicity than Itraconazole and other synthsized compounds.Preparation of 3-isothiazolones having biological activity comparable to the widely used antibacterial and antifungal drug encourage further investigation on these compounds.

1, 3, 4-OXADIAZOLES AN IMPORTANT CLASS OF HETEROCYCLIC COMPOUNDS THAT HAVE A WIDE RANGE OF PHARMACEUTICAL AND BIOLOGICAL ACTIVITIES INCLUDING ANTIMICROBIAL, ANTI-FUNGAL, ANTI-INFLAMMATORY, ANTIHYPERTENSIVE, ANALGESIC, ANTIBACTERIAL, HYPOGLYCEMIC, ANTIMALARIAL, ANTITUBERCULAR AND ANTIDEPRESSANT [1]...