Focus on the synthesis and reactions of some new pyridine carbonitrile derivatives as antimicrobial and antioxidant agents

3-[4-CHLOROPHENYL]-1-[2, 4-dichlorophenyl]-propen-1-one [1] was prepared and reacted with active methylene compound, ethyl cyanoacetate in the presence of ammonium acetate 10 give the corresponding pyridine carbonitrile [2]. The behavior of compound 2 towards phosphorous pentasulfide, phosphorous oxychloride and some acyclic-sugars has been investigated and afforded compounds 3, 4 and 5a-d, respectively. The thioxo-pyridine carbonitrile [3] reacted with different halo compounds namely: methyl iodide, ethyl chloroacetate, some acyclic sugars to afford 6, 7 and 8a-c, respectively. Treatment of compound 3 with acrylonitrile afforded compound 9. Reaction of the thiosulfanyl 6 with hydrazine hydrate gave the hydrazine derivative 10 while reaction of 7 with the same reagents gave the acid hydrazide 11. Also, compound 4 reacted with different nucleophiles to afford compounds 10, 12-14. Condensation of compound 10 with ethyl acetoacetate, acetyl acetone, acetic anhydride, p-chlorobenzaldehyde afforded compounds 15-18, respectively. Moreover, compound 10 reacted with carbon disulfide to afford compound 19. Finally, condensation of compound 10 with aldehydo-sugar namely: D-glucose gave the corresponding acyclic nucleoside 20. Furthermore, biological evaluation of some prepared compounds has been assessed and some of them revealed promising antimicrobial and antioxidant activity

Production and characterization of milk-clotting enzymes by Bacillus circulans NRC-3

The production of Milk-clotting enzyme was investigated using seven bacterial isolates. Bacillus circulans NRC-3 proved to be the most potent and produced a highly active milk-clotting enzyme with negligible proteolytic activity on wheat bran medium as a food byproduct. The milk- clotting enzyme activity was optimal at 50°C and CaC12 of final concentration of 0.3 mM. The enzyme was highly stable at elevated temperatures [70°C] and retained more than 60% of the original activity by heating for 5min.at 70°C. Partial purification of the enzyme was achieved by fractional precipitation with acetone or ethanol. The 40% acetone fraction was the most promising and possessed rennin properties with no proteolytic activity. It reached about 4.3-fold that of the culture filtrate. The partial purified B.circulans NRC-3 milk-coltting enzyme was applied on three buffalo fresh milk specimens, i.e. full- cream, half- cream and skimmed fresh. The enzyme exhibited the maximum relative activity [100%] with both half- cream and skimmed fresh milk specimens and dropped to 67.1% with the full- cream specimen

Reactions with 6-substituted-2-thiouracil-5-carbonitrites, synthesis of tetrazolo [1,5-c] and ditetrazolo [1,5 -a: 1,5-c] pyrimidines

Heating a ternary mixture of 6-furyl or 6-thienyl-4- oxo- 1, 2, 3, 4 - tetrahydro-2- thioxopyrimidine-5-carbonitrile [I a, b], chloroacetic acid and a suitable aromatic or heterocyclic aldehyde, led to the formation of 2- arylmethylene-2, 3- dihydro-3, 5 - dioxo-7- substituted- 5H- thiazolo [3, 2 - a] pyrimidine-6-carbonitriles [II a- i]. Alkylation of Ia, gave the s-alkyl derivatives IVa, b. Compounds IV and the thienyl analogue V reacted with benzylamine to give the 2- benzylamino derivatives. Heating IVa and V with phosphorus oxychloride gave the corresponding 4- chloropyrimidine derivatives [VIIa, b]. The 4- phenylthio-, 4-phenylhydrazino-, 4-benzylamino and 4- anilino-2- ethylthio-6- thienylpyrimidine-5- carbonitriles [VIIIa- d] were prepared from VIIb. Whereas compound VIIa gave, on heating with hydrazine hydrate, the 4-hydrazino-2-ethylthio and the 2, 4-dihydrazino derivatives IXa and X, respectively, compound VIIb gave only the 4-hydrazine derivative IXb. The latter compound reacted with nitrous acid to give 5-ethylthio-7-thienyltetrazolo [1, 5-c] pyrimidine-8-carbonitril XI. Diazotization of X led to the formation of 5-furyl ditetrazolo [1, 5-a, 1, 5-c] pyrimidine-6-carbonitrile [XII]

Trazodone and dexamethasone suppression in major depressive illness

This study is a clinical investigation for the effects of trazodone on the dexamethasone suppression response of 23 patients with major depressive episode. Assessment of the clinical response to four weeks treatment period was done by applying the Hamilton scale of depression [H.S.D.] before and after the treatment period. Analysis of the HSD results, the presence of 12 responders to trazodone treatment with a mean score of 12.2 +/- 2 and 11 non-responders with a mean score of 27 +/- 3.4. Responders were considered to be those who achieved 50% [or more] reducation in their post-treatment HSD score. The Dexamethasone Suppression Test [D.S.T] done before and after the four weeks treatment, revealed that before trazodone treatment, only four patients out of the 12 responders were suppression [showed lowering of Cortisol level after dexamethasone treatment]. The rest were non-suppressors. After trazodone treatment 9 patients were suppressors and 3 were non-suppressors. All the [HSD] non-responders [11 patients] were [DST] non-suppressors before trazodone treatment and only one of them became a suppressor after treatment

Reactions with alpha-substituted cinnamonitriles: synthesis of benzo [h] quinolines and naphthol [1,2, b] pyrans

Alpha-substituted cinnamonitrile derivatives [1a-i] reacted with alpha-tetralone [2] in the presence of ammonium acetate to yield 5, 6-dihydrobenzo [h] quinoline derivatives with different substituents at 2,3, and 4 positions [3,7-9]. Substituting sodium acetate for ammonium acetate led to the formation of the 5, 6-dihydro-2-imino-4-phenylnaphtho [1, 2-b] pyran-3-carbonitrile [5]

Synthesis of some benzothiazole derivatives of expected biological activity

Denzothiazole was long known to be effective as bacteriostatic, tuberculostatic, fungistatic and molluscidal agents [1-6]. The present work describes the synthesis of new 2-methyl and 2-thiobenzothiazole derivatives which is expected to posses bacteriostatic activity

Reactions with 4,5-diphenyl 2-mercaptoimidazole: synthesis of 2-substituted thiazolo [3,2-a] imidazoles

The potassium salt of 4,5-diphenyl-2-mercaptoimidazole [I] was reacted with 3-chloro-2,4-pentaneaione to give the S-alkyl derivative II. Compound II coupled with arenediazonium salts to give the azo derivatives [III]. On heating II and III with poly-phosphoric acid, cyclization took place and 2-substituted thiazolo [3,2-a] imidazoles V and VI were obtained. V Condensed with aromatic aldehydes to yield the cinnamoyl derivatives VII, which reacted with phenylhydrazine and hydroxylamine to give 2-pyr-azolinyl-and 2-isoxazolinyl-thiazolo [3,2-a] imidazole derivatives IX and X respectively

Reconstruction of full thickness defects of ala nasi by one-stage procedure

One-stage reconstruction of full-thickness defects of the ala nasi, of traumatic origin [3 cases] and following excision of basal cell carcinoma [11 cases], is presented in this paper. The superiorly pedicled nasolabial cheek flap has been used in the reconstruction. The flap has been designed long enough to allow folding of its terminal part as an inner lining. The nasolabial flaps, in general, are supplied with the angular branch of the anterior facial artery and its free anastomosis with and infra-orbital arteries. The latter anastomosis is the main supply for the superiorly pedicled nasolabial flap. The tremendous blood supply allows for raising flaps of 4 to 1 length to breadth ratio without need for prior delay. This technique saves the trouble of the traditional multiple-stage reconstruction techniques, and, at the same time, gives very satisfactory cosmetic results

Cross-leg flaps in children

Ten children of ages ranging between 4 and 11 years sustaining road traffic accidents that resulted into crushing and devitalizing injury to the shin of the foot, with exposure of and variable degree of damage to underlying structures, were treated by cross-leg flaps. The flaps were transferred immediately without any prior very much than delay. The paper exposes three new findings: First, the children can tolerate the immobilization without any adverse effects be used during the period of transfer and, third, flaps of slightly bigger than width could be transferred immediately in such young age

Surgical treatment of epithelioma of the lower lip

Thirty-five cases of epithelioma of the lower lip were treated surgically. The clinical diagnosis was confirmed by wedge biopsy. After radical excision, the edges were pathologically examined and were clear of any malignancy. Reconstruction was made by naso-labial flap[s] very much less than 21 cases, rectangular flap [4 cases], forehead shin graft lined-flap [5 cases] and cross-lip flap [5 cases]. Unilateral therapeutic neck dissection was needed for three cases only. The results are discussed