Home > Aromatic/ Heterocyclic Sulfonamides Containing Chromone Moieties and Their Transition Metal Complexes: Synthesis, Structural Elucidation and Evaluation of Biological Activities
Aromatic/ Heterocyclic Sulfonamides Containing Chromone Moieties and Their Transition Metal Complexes: Synthesis, Structural Elucidation and Evaluation of Biological Activities
Carbonic anhydrases (CA E.C. 4.2.1.1) are zinc containing metalloenzymes found in both prokaryotes and eukaryotes where they perform important physiological functions. CA has at least 16 different isozymes many of which are important drug targets. Sulfonamides and its metal derivatives are well established inhibitors of CA. The task of developing a new class of chromone containing sulfonamide CA inhibitors was taken up in this research/thesis. Consequently cobalt (II), nickel (II) and copper (II) transition metal complexes were also synthesized and tested as inhibitors of CA. An assortment of structurally diverse aromatic/heterocyclic sulfonamides containing chromone moieties were synthesized by condensation of various substituted and un-substituted 4-oxo-4H-1-benzopyran-3-carboxaldehydes with different aminobenzenesulfonamides. Compounds L1, L4, L7 and L10 were prepared by reacting 4-oxo-4H-1-benzopyran-3-carboxaldehyde (C10H6O3) and substituted 4- oxo-4H-1-benzopyran-3-carboxaldehydes (R1R2-C10H4O3, R1 = F, Br; R2 = H, Br) with 4-aminobenzenesulfonamide (4-ABS). Compounds L2, L5, L8 and L11 were prepared by reacting above chromone-3-carboxaldehydes with 3- aminobenzenesulfonamide (3-ABS). Similarly compounds L3, L6, L9 and L12 were obtained by reaction with 2-aminobenzenesulfonamide (2-ABS). Compounds L13- L17 were prepared by reaction of 4-oxo-4H-1-benzopyran-3-carboxaldehyde and 4- oxo-6-fluoro -4H-1-benzopyran-3-carboxaldehydes with N-(heteroaryl)substituted sulfonamides. In case of reactions with 3-ABS and 4-ABS, enamine products of type and 4-[{(2-ethoxy-6-(un)substituted-4-oxo-chroman)3-ylidene}methylamino] xv benzenesulfonamides were obtained. However, on reaction with 2-ABS, a benzothiadiazine product containing chromone moiety at 3-position resulted due to cyclization. Only 4-oxo-6,8-dibromo-4H-1-benzopyran-3-carboxaldehyde proved to be the only exception giving an enamine product, 2-[{(2-ethoxy-6,8-dibromo-4-oxo- chroman)3-ylidene}methylamino]benzenesulfonamide. Stable, non electrolyte, non polymeric metal complexes were obtained in good yields by reacting Co (II), Ni (II) and Cu (II) acetates with above compounds under basic conditions. Molecular structure of all fifty three compounds (both ligands and their complexes) was ascertained by means of IR, 1H-NMR, 13C-NMR, MS and elemental (C, H, N) analysis. The metal content of the metal complexes was determined by AAS. In case where suitable crystals were available, single crystal X-ray diffraction was carried out. In view of CA inhibitory role of sulfonamides and their metal complexes, CA inhibitions activity of all the compounds and their metal complexes was evaluated against bovine cytosolic enzyme containing CA-I and CA-II. All compounds containing free sulfonamide group showed excellent CAI activity (IC50values are in the range 4.31 to 29.12 μmoles). Compounds containing substituted sulfonamide group were found to be inactive as CAIs. Among metal complexes copper complexes were most active followed by some nickel complexes; cobalt complexes were not very active as CAIs. DPPH radical scavenging activity for all the compounds was also evaluated. Only compounds L12 and L14 showed moderate activity (67 and 41 % inhibition respectively). None of the other compounds showed outstanding radical scavenging activity.
The word "Ikhthilaf" refers to such an approach and way of conversation in which one scholar disagrees with another scholar. Islam being a perfect religion bars its followers from developing mutual conflicts. Islam has clearly stated that Muslim Ummah should not have differences on the basis of opinions in vivid injunctions. Such dissension has been placed nowhere in Islam. Disputes may only arise in case of secondary and vague injunctions. In such situations, each jurist considers himself as right. Such divergence, in the secondary issues based on argumentation and within the ambit of Qur’ān and Ḥadith, is not contemptible one but is the source of blessings due to the depth of knowledge of the jurists. Because of such conflicting opinions, jurisprudence and religious injunctions have the power of adaptability in accordance with the demands of the changing times. In the matters of jurisprudence, establishing consensus on the basis of argumentation must not lead to sectarianism, prejudice and hatred. True jurists have tried their level best to protect Muslim Ummah from sectarian disputes. Among such jurists we have Allama Alusī, the author of Tafsīr Rūḥ al Ma’ānī, as one big contributor. Tafsīr Rūḥ al Ma’ānī is the solid proof of his authentic and deep knowledge. It has a combination of reported sayings and exegesis of consents.
Present study was designed to find out the relationship between emotional intelligence and self esteem
among sighted and visually impaired school students. The main objectives of this study were to measure self
esteem of sighted and visually impaired students, to measure emotional intelligence level of sighted and
visually impaired students, to compare self esteem and emotional intelligence of sighted and visually impaired
students, to compare emotional intelligence and self esteem of sighted and visually impaired students
studying in private and public sectors institutions and to investigate the role of students' demographic
variations of gender, age, grade, family socioeconomic status, number of siblings, birth order, parental
professions and qualification in determining their self esteem and emotional intelligence levels.
In this study standardized questionnaires were used to measure emotional intelligence and self esteem,
emotional intelligence was measured by using Emotional Intelligence Scale (EIS) and Self Esteem
Questionnaire (SEQ) was used to measure students' self esteem. EIS contained 33 items comprised seven
subscales i.e. Appraisal of Emotions in Self, Appraisal of Emotions in Others, Emotional Expression, Emotional
Regulation of others, Utilization of Emotions in Problem Solving and Uncategorized. SEQ contained 36 items
comprised five subscales i.e. self — Regard, Social Confidence, School Abilities, Physical Appearance and
Physical Abilities. Cronbach's Alpha reliability of EIS and SEQ were .843 and .696. A sample comprising of 200
students was taken from sighted and visually impaired students studying at secondary schools from
Islamabad, Rawalpindi, Sargodha District and Attock. Stratified random sampling technique was used to
collect data for the study.
Research findings revealed that there is significant difference in responses between sighted and visually
impaired school students regarding emotional intelligence and self esteem, this study also reveals that there
is significant positive relationship between emotional intelligence and self esteem.