Synthesis and biological evaluation of some new 1,4-dihydropyridines containing different ester substitute and diethyl carbamoyl group as anti-tubercular agents

Tuberculosis is a leading infectious cause of death worldwide. Because of the concern of the resistance to most of the commonly used drugs displayed by the considered mycobacteria, most efforts have been done to introduce new anti-tubercular agents. Recent studies showed that 1,4-dihydropyridine-3,5-dicarbamoyl derivatives with lipophilic groups have significant anti-tubercular activity. In this study, we synthesized new derivatives of 1,4-dihydropyridines in which different alkyl and aryl esters and diethyl carbamoyl are substituted in C-3 and C-5 of the DHP ring. In addition nitroimidazole ring is substitutes at C-4 position. These asymmetric analogues were synthesized by a modified Hantzsh reaction using procedure reported by Meyer. The in vitro anti-tubercular activity of compounds against Mycobacterium tuberculosis was evaluated. The results indicate that the compounds containing aromatic esters are more potent than alkyl ones. The most potent aromatic compound (R = 3-phenylpropyl) exhibits comparable anti-tubercular activity (MIC = 1 μmol/ml) with reference compound isoniazide (INH) (MIC = 1 μmol/ml). Conformational analysis, SAR studies of these compounds showed that increasing in lipophilicity and rotable bonds of these compounds resulted in increasing anti-tubercular activity.     

Harvesting fat from the infratemporal fossa

As part of forehead rejuvenation and surgical treatment of migraine headaches, the mass of the corrugator supercilii, the procerus, and the depressor supercilii muscles is replaced with fat for optimal aesthetic contouring of this region and to help prevent recurrence of the glabellar lines. The authors propose a new fat graft donor site that is convenient and safe and that adds only minutes to the total operating time. This fat is located between the deep layer of deep temporal fascia and the temporalis muscle as it approaches the zygomatic arch. The temporal musculofascial anatomy as it relates to the available fat donor sites is described. This source has been used on 74 occasions at 128 sites, from July 1, 2002, to December 31, 2002, with no complications attributable to the technique.     

Effects of chlorpromazine on mechanical properties of the outer hair cell plasma membrane

An optical tweezers system was used to characterize the effects of chlorpromazine (CPZ) on the mechanical properties of the mammalian outer hair cell (OHC) through the formation of plasma membrane tethers. Such tethers exhibited force relaxation when held at a constant length for several minutes. We used a second-order generalized Kelvin body to model tether-force behavior from which several mechanical parameters were then calculated including stiffness, viscosity-associated measures, and force relaxation time constants. The results of the analysis portray a two-part relaxation process characterized by significantly different rates of force decay, which we propose is due to the local reorganization of lipids within the tether and the flow of external lipid into the tether. We found that CPZ's effect was limited to the latter phenomenon since only the second phase of relaxation was significantly affected by the drug. This finding coupled with an observed large reduction in overall tether forces implies a common basis for the drug's effects, the plasma membrane-cytoskeleton interaction. The CPZ-induced changes in tether viscoelastic behavior suggest that alterations in the mechanical properties of the OHC lateral wall could play a role in the modulation of OHC electromotility by CPZ.     

Modified temporal incision for facial rhytidectomy: an 18-year experience

An 18-year experience with the senior author's temporal incision is expounded. First, the existing sideburn is outlined with a marking pen. A sideburn is designed approximately 2 cm wide and 2 cm long, regardless of the extent of the existing sideburn providing the minimum sideburn. The posterocaudal portions of the newly designed sideburn will correspond to that of the existing dense portion of the sideburn. After dissection and removal of excess skin, the entire vertical portion of the scar will remain within the hair-bearing skin, eliminating the potential for visibility unless preoperatively the sideburn is less that 2 cm wide. There are several advantages to this approach. First, the configuration of the sideburn remains essentially unaltered. Second, the length of distribution for the redundant redraped facial skin is increased in comparison with most other incisions, thus avoiding a dog-ear regardless of the extent of the excess facial skin. Rhytidectomy is more effective because the distance from the incision to the nasolabial crease and the oral commissure is reduced, thereby effectively transmitting the traction forces to these sites compared with the conventional temporal incision that is placed above the ear. In addition, exposure of the surgical field is significantly enhanced by the added ability to rotate the skin flap medially. The potential disadvantage is that the operative time is increased to accommodate meticulous repair of the temporal incision. A slight modification of this incision has been implemented over the past 18 years, placing the anterior vertical incision farther posterior compared with the original report. The horizontal and posterior vertical portions of the incision are positioned at the hairline, resulting in an inconspicuous scar. None of the 125 patients in this latter group required a scar revision compared with 37 (4.28 percent) of 865 patients before this modification. This technique effectively achieves the goal of facial rhytidectomy and maintains a natural appearance without discernible scars for most patients. Patient and surgeon satisfaction with this method has been very high, and consequently, it has been used for almost all patients in the senior author's (Guyuron's) practice.     

The zygomaticotemporal branch of the trigeminal nerve: an anatomical study

This study was conducted to determine the site of emergence of the zygomaticotemporal branch of the trigeminal nerve from the temporalis muscle and to identify the number of its accessory branches and their locations. A pilot study, conducted on the same number of patients, concluded that the main zygomaticotemporal branch emerges from the deep temporal fascia at a point on average 17 mm lateral and 6 mm cephalad to the lateral palpebral commissure, commonly referred to as the lateral canthus. These measurements, however, were obtained after dissection of the temporal area, rendering the findings less reliable. The current study included 20 consecutive patients, 19 women and one man, between the ages of 26 and 85 years, with an average age of 47.6 years. Those who had a history of previous trauma or surgery in the temple area were excluded. Before the start of the endoscopic forehead procedure, the likely topographic site of the zygomaticotemporal branch was marked 17 mm lateral and 6 mm cephalad to the lateral orbital commissure on the basis of the information extrapolated from the pilot study. The surface mark was then transferred to the deeper layers using a 25-gauge needle stained with brilliant green. After endoscopic exposure of the marked site, the distance between the main branch of the trigeminal nerve or its accessory branches and the tattoo mark was measured in posterolateral and cephalocaudal directions. In addition, the number and locations of the accessory branches of the trigeminal nerve were recorded. On the left side, the average distance of the emergence site of the main zygomaticotemporal branch of the trigeminal nerve from the palpebral fissure was 16.8 mm (range, 12 to 31 mm) in the posterolateral direction and an average of 6.4 mm (range, 4 to 11 mm) in the cephalad direction. On the right side, the average measurements for the main branch were 17.1 mm (range, 15 to 21 mm) in the lateral direction and 6.65 mm (range, 5 to 11 mm) in the cephalic direction. Three types of accessory branches were found in relation to the main branch: (1) accessory branch cephalad, (2) accessory branch lateral, and (3) accessory branches in the immediate vicinity of the main branch. This anatomical information has proven colossally helpful in injection of botulinum toxin A in the temporalis muscle to eliminate the trigger sites in the parietotemporal region and surgical management of migraine headaches triggered from this zone.