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A new series of pyridine-2-one and pyrazole derivatives were designed and synthesized based on cyanoacrylamide derivatives containing 2,4-dichlro aniline and 6-methyl 2-amino pyridine as an aryl group. Condensation of cyanoacrylamide derivatives 3a–d with different active methylene (malononitrile, ethyl cyanoacetate cyanoacetamide, and ethyl acetoacetate) in the presence of piperidine as basic catalyst afforded the corresponding pyridinone derivatives 4a–c, 5, 9, and 13. Furthermore, the reaction of cyanoacrylamide derivatives 3a–d with bi-nucleophile as hydrazine hydrate and thiosemicarbazide afforded the corresponding pyrazole derivatives 14a,b and 16. The newly designed derivatives were confirmed and established based on the elemental analysis and spectra data (IR, 1H NMR, 13C NMR, and mass). The in vitro antibacterial activity was evaluated against four bacterial strains with weak to good antibacterial activity. Moreover, the results indicated that the most active derivatives 3a, 4a, 4b, 9, and 16 might lead to antibacterial agents, especially against B. subtilis and P. vulgaris. The DFT calculations were performed to estimate its geometric structure and electronic properties. In addition, the most active pyridinone and pyrazole derivatives were further evaluated for in silico physicochemical, drug-likeness, and toxicity prediction. These derivatives obeyed all Lipinski’s and Veber’s rules without any violation and displayed non-immunotoxin, non-mutagenic, and non-cytotoxic. Molecular docking simulation was performed inside the active site of Topoisomerase IV (PDB:3FV5). It displayed binding energy ranging from -14.97 kcal/mol to -18.86 kcal/mol with hydrogen bonding and arene–cation interaction. Therefore, these derivatives were suggested to be good antibacterial agents via topoisomerase IV inhibitor. Graphical abstract

I . The changes in serum levels of uric acid and lipids during I month of starvation-refeeding were 2. Uric acid levels increased linearly with the duration of the experiment. The increase was positively 3. Triglycerides increased at a faster rate than uric acid implying that the increase in uric acid was secon-4. It was concluded that the purine and lipid synthetic pathways are linked through a common smallmeasured in sixteen male volunteers. correlated with the increase in serum triglycerides but not with cholesterol or phospholipids. dary to that of the lipid. molecular-weight effector rather than through the sharing of a common enzyme.Throughout the holy lunar month of Ramadan, moslems are expected to abstain from food and drink daily between dawn and sunset. The incidence of renal colic or of angina pectoris increases noticeably during this Islamic month especially when the latter coincides with the hot, dry summer in the Sudan. The question whether these complaints are due to increases of risk factors predisposing to renal calculi and to coronary vascular disease consequent upon the dietary pattern during Ramadan remained to be answered.When breaking their fast at sunset, Sudanese moslems consume large volumes of sugarsweetened juices to quench thirst, and foods rich in carbohydrates are eaten from sunset till dawn. Nicholls & Scott (1972) reported that energy restriction leads to a decrease in the plasma level of uric acid and attributed this partly to the relative hydration state associated with weight loss. Increased carbohydrate intake, especially sucrose, is known to increase the triglyceride concentration in serum (Anderson, Grande, Matsumoto & Keys, I 963 ; Nestel, Carrol & Haverstein, 1970; Fry, Spector, Connor & Connor, 1973; Roberts, 1973; Sacks, Castelli, Donner & Kass, 19-75),The present study reports the changes in the serum levels of uric acid and lipids during daily starvation-refeeding over a period of 28 d in an attempt to test their relationship to the associated complaints of renal colic or angina. Correlation studies were used to test the relation between uric acid and lipid metabolism during periods of maximal dehydration and rehydration throughout the 28 d. M A T E R I A L S A N D M E T H O D SThe present investigation took place in the Facuty of Medicine, University of Khartoum, Sudan. Sixteen male students aged between 20 and 22 years volunteered for the study, which was to span the one month of Ramadan. All volunteers were healthy as evident from a general medical examination and none was receiving any medication.Venous blood was collected into clean tubes and allowed to clot at room temperature.

I. Fluid intake, urine output and evaporative water loss were measured and fluid balance calculated in sixteen subjects for I d before Ramadan, during weeks 1-5 of fasting and on the 10th day after the end of Ramadan.2. Plasma osmolality at 06.00 hours, the beginning of the fast, at 18.00 hours, before breaking the fast and at 19.00 hours, I h after breaking the fast, and urine osmolality during the day and night were measured before, during and after Ramadan.3. All subjects developed an initial negative fluid balance which was maximum at the beginning of week 3 of fasting and that deficit was compensated for during the later weeks.4. Compensation was brought about by an increase in urine concentration, a decrease in urine volume by day, and salt retention.5. No significant changes were observed in plasma osmolality during the days of fasting and the 'setting' of plasma osmolality during Ramadan also was not changed.6. It was concluded that healthy young adults maintain good control of fluid and electroytes during Ramadan.During the Islamic lunar month of Ramadan millions of moslems in the tropics abstain, among other things, from drinking and eating from dawn to sunset. At night they take fluids and meals rich in carbohydrates.McCance & Widdowson (1937) described the responses of human volunteers-to dehydration during salt depletion. Haberner, Dashe & Solomon (1964) investigated1the responses of normal subjects to prolonged high fluid intake. Veverbrants & Arky (1969) and Chinn, Brown, Fraser, Heron, Lever, Murchison & Robertson (1970) studied the effects of energy deprivation and refeeding on water and electrolyte excretion in subjects maintained on a constant electrolyte and fluid intake. As far as we know, the pattern in Ramadan of 12 h energy deprivation and dehydration followed by 12 h of refeeding and rehydration, over a period of 30 d, has not been studied before.In this paper we will report on the fluid and electrolyte homoeostasis; effects of fasting Ramadan on plasma lipids and uric acid have been reported separately (Gumaa, Mustafa, Mahmoud & Gader, 1978).Sixteen male Sudanese students aged 20-22 years, all healthy as evident by medical history and clinical examination, volunteered for this study. They were all conscientious moslems who observed fasting rigidly. They were all studied on the day before Ramadan (week 0) and then divided into two groups, one studied on the 1st day and the other on the 3rd day of every week of fasting. Because of the small number of subjects investigated the results * Present address:

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A pilot survey was designed to define incidence, rotation period, rotation direction and cycle of shiftwork plans in the production and service units in Kuwait. Preliminary results from the Ministry of Interior showed that four different shift plans are widely used. Forty policemen, ten from each shift plan, volunteered to fill in a diary for a period of two or more cycles. The diary was comprised of a set of questions planned to reveal disturbances in sleep duration, sleep quality, food intake and appetite. The daily questionnaire also covered psychosomatic complaints and subjective judgement of recovery. A control group, on permanent day work, volunteered to fill in the diary for the same period. The results indicated that one of the four shift plans was quite satisfactory and least harmful to the policemen. Two plans were associated with excessive strain during working days, but the number of free days was sufficient to achieve complete recovery. The fourth plan was associated with excessive strain during working days and recovery was not achieved after 24 h of rest at the end of the shift cycle.

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